-
2
-
-
0021343377
-
Effectiveness of Amodiaquine as a Treatment for Chloroquine Resistant Plasmodium falciparum
-
(a) Watkins, W. M.; Sixsmith, D. G.; Spencer, H. G.; Boriga, D. A.; Karjuki, D. M.; Kipingor, T.; Koech, D. K. Effectiveness of Amodiaquine as a Treatment for Chloroquine Resistant Plasmodium falciparum. Lancet I, 1984, 357-359.
-
(1984)
Lancet I
, pp. 357-359
-
-
Watkins, W.M.1
Sixsmith, D.G.2
Spencer, H.G.3
Boriga, D.A.4
Karjuki, D.M.5
Kipingor, T.6
Koech, D.K.7
-
3
-
-
0029852248
-
Can Amodiaquine be Resurrected?
-
(b) White, N. J. Can Amodiaquine be Resurrected? Lancet, 1996, 348, 1184-1185.
-
(1996)
Lancet
, vol.348
, pp. 1184-1185
-
-
White, N.J.1
-
4
-
-
0029807475
-
Systematic Review of Amodiaquine Treatment in Uncomplicated Malaria
-
(c) Olliaro, P.; Nevill, C.; Lebras, J.; Ringwald, P.; Mussano, P.; Garner, P.; Brasseur, P. Systematic Review of Amodiaquine Treatment in Uncomplicated Malaria. Lancet 1996, 348, 1196-1201.
-
(1996)
Lancet
, vol.348
, pp. 1196-1201
-
-
Olliaro, P.1
Nevill, C.2
Lebras, J.3
Ringwald, P.4
Mussano, P.5
Garner, P.6
Brasseur, P.7
-
5
-
-
0022655075
-
Amodiaquine Induced Agranulocytosis and Liver Damage
-
Neftel, K. A.; Woodtly, W.; Schmid, M. Amodiaquine Induced Agranulocytosis and Liver Damage. Br. Med. J. 1986, 292, 721-723.
-
(1986)
Br. Med. J.
, vol.292
, pp. 721-723
-
-
Neftel, K.A.1
Woodtly, W.2
Schmid, M.3
-
6
-
-
0015934337
-
Amodiaquine Induced Agranulocytosis; Toxic Effects of Amodiaquine in Bone Marrow Culture In vitro
-
Lind, D. E.; Levi, J. A.; Vincent, P. C. Amodiaquine Induced Agranulocytosis; Toxic Effects of Amodiaquine in Bone Marrow Culture In vitro. Br. Med. J. 1973, 1, 458-460.
-
(1973)
Br. Med. J.
, vol.1
, pp. 458-460
-
-
Lind, D.E.1
Levi, J.A.2
Vincent, P.C.3
-
7
-
-
0026546128
-
The Mechanism of Bioactivation and Antigen Formation of Amodiaquine in the Rat
-
Harrison, A. C.; Kitteringham, N. R.; Clarke, J. B.; Park, B. K. The Mechanism of Bioactivation and Antigen Formation of Amodiaquine in the Rat. Biochem. Pharmacol. 1992, 43, 1421-1430.
-
(1992)
Biochem. Pharmacol.
, vol.43
, pp. 1421-1430
-
-
Harrison, A.C.1
Kitteringham, N.R.2
Clarke, J.B.3
Park, B.K.4
-
8
-
-
0023855476
-
Drug Protein Conjugates-XIV. Mechanism of Formation of Protein Arylating Intermediates From Amodiaquine a Myelotoxin and Hepatotoxin in Man
-
Maggs, J. L.; Kitteringham, N. R.; Park, B. K. Drug Protein Conjugates-XIV. Mechanism of Formation of Protein Arylating Intermediates From Amodiaquine a Myelotoxin and Hepatotoxin in Man. Biochem. Pharmacol. 1988, 37, 303-311.
-
(1988)
Biochem. Pharmacol.
, vol.37
, pp. 303-311
-
-
Maggs, J.L.1
Kitteringham, N.R.2
Park, B.K.3
-
9
-
-
0001349941
-
Detection of IgG Antibodies in Patients with Adverse Drug Reactions to Amodiaquine
-
Clarke, J. B.; Maggs, J. L.; Kitteringham, N. R.; Park, B. K. Detection of IgG Antibodies in Patients with Adverse Drug Reactions to Amodiaquine. Int. Arch. Allergy Immunol. 1990, 1335-1342.
-
(1990)
Int. Arch. Allergy Immunol.
, pp. 1335-1342
-
-
Clarke, J.B.1
Maggs, J.L.2
Kitteringham, N.R.3
Park, B.K.4
-
10
-
-
0027328976
-
The Effect of Fluorine Substitution On the Hepatotoxicity and Metabolism of Paracetamol in the Mouse
-
(a) Barnard, S.; Kelly, D. F.; Storr, R. C.; Park, B. K. The Effect of Fluorine Substitution On the Hepatotoxicity and Metabolism of Paracetamol in the Mouse. Biochem. Pharmacol. 1993, 46, 841-849
-
(1993)
Biochem. Pharmacol.
, vol.46
, pp. 841-849
-
-
Barnard, S.1
Kelly, D.F.2
Storr, R.C.3
Park, B.K.4
-
11
-
-
0027305369
-
The Effect of Fluorine Substitution on the Physicochemical Properties and the Analgesic Activity of Paracetamol
-
(b) Barnard, S.; Storr, R. C.; O'Neill, P. M.; Park, B. K. The Effect of Fluorine Substitution on the Physicochemical Properties and the Analgesic Activity of Paracetamol. J. Pharm. Pharmacol. 1993, 45, 736-744.
-
(1993)
J. Pharm. Pharmacol.
, vol.45
, pp. 736-744
-
-
Barnard, S.1
Storr, R.C.2
O'Neill, P.M.3
Park, B.K.4
-
12
-
-
0028307644
-
The Effect of Fluorine Substitution on the Metabolism and Antimalarial Activity of Amodiaquine
-
O'Neill, P. M.; Harrison, A. C.; Storr, R. C.; Hawley, S. R.; Ward, S. A.; Park, B. K. The Effect of Fluorine Substitution on the Metabolism and Antimalarial Activity of Amodiaquine. J. Med. Chem. 1994, 37, 1362-1370.
-
(1994)
J. Med. Chem.
, vol.37
, pp. 1362-1370
-
-
O'Neill, P.M.1
Harrison, A.C.2
Storr, R.C.3
Hawley, S.R.4
Ward, S.A.5
Park, B.K.6
-
13
-
-
0031965067
-
The 4-Aminoquinolines-Past, Present and Future-A Chemical Perspective
-
(a) O'Neill, P. M.; Hawley, S. R.; Bray, P. G.; Ward, S. A.; Park, B. K. The 4-Aminoquinolines-Past, Present and Future-A Chemical Perspective. Pharmacol. Ther. 1998, 77, 29-58.
-
(1998)
Pharmacol. Ther.
, vol.77
, pp. 29-58
-
-
O'Neill, P.M.1
Hawley, S.R.2
Bray, P.G.3
Ward, S.A.4
Park, B.K.5
-
14
-
-
0035899179
-
Synthesis and in Vitro and in Vivo Antimalarial Activity of New 4-Anilinoquinolines
-
(b) For a very recent approach to amodiaquine analogues designed to be less toxic than amodiaquine see; Delarue, S.; Girault, S.; Maes, L.; et al. Synthesis and in Vitro and in Vivo Antimalarial Activity of New 4-Anilinoquinolines. J. Med. Chem. 2001, 44, 2827-2833.
-
(2001)
J. Med. Chem.
, vol.44
, pp. 2827-2833
-
-
Delarue, S.1
Girault, S.2
Maes, L.3
-
15
-
-
0031055744
-
Synthesis, Antimalarial Activity, and Molecular Modeling of Tebuquine Analogues
-
(a) O'Neill, P. M.; Willock, D. J.; Hawley, S. R.; Bray, P. G.; Storr, R. C.; Ward, S. A.; B. K. Park. Synthesis, Antimalarial Activity, and Molecular Modeling of Tebuquine Analogues. J. Med. Chem. 1997, 40, 437-448.
-
(1997)
J. Med. Chem.
, vol.40
, pp. 437-448
-
-
O'Neill, P.M.1
Willock, D.J.2
Hawley, S.R.3
Bray, P.G.4
Storr, R.C.5
Ward, S.A.6
Park, B.K.7
-
16
-
-
85039608960
-
-
note
-
(b) ClogP values were calculated using the MacLogP 4 programme, Biobyte Corp.201 W. 4th St. Suite #204, Claremont, CA 91711.
-
-
-
-
17
-
-
33947445299
-
Aminoalkylphenols as Antimalarials II (Heterocyclic-amino)-α -amino-o-cresols; The Synthesis of Camoquine
-
Burckhalter, J. H.; Tendwick, J. H.; Jones, F. H.; Jones, P. A.; Holcombe, W. F.; Rawlins, A. L. Aminoalkylphenols as Antimalarials II (Heterocyclic-amino)-α-amino-o-cresols; The Synthesis of Camoquine. J. Am. Chem. Soc. 1948, 70, 1363-1373.
-
(1948)
J. Am. Chem. Soc.
, vol.70
, pp. 1363-1373
-
-
Burckhalter, J.H.1
Tendwick, J.H.2
Jones, F.H.3
Jones, P.A.4
Holcombe, W.F.5
Rawlins, A.L.6
-
18
-
-
33947449429
-
The Role of Phenol in the Reaction of 4,7-Dichloroquinoline with Novol Diamine
-
A byproduct in this process is the 4-ethoxy-7-chloroquinoline that arises via nucleophilic aromatic substitution of the 4-chloro atom by solvent. That 4-ethoxy-7-chloroquinoline is an intermediate en route to the desired product remains to be established. By analogy, it has been shown that for reactions involving 4-chloroquinolines with alkylamines in phenol as solvent, the intermediate 4-phenoxyquinoline is an intermdiate. For examples, see: Surrey, A. R.; Cutler, R. A. The Role of Phenol in the Reaction of 4,7-Dichloroquinoline with Novol Diamine. J. Am. Chem. Soc. 1951, 73, 2623-2626.
-
(1951)
J. Am. Chem. Soc.
, vol.73
, pp. 2623-2626
-
-
Surrey, A.R.1
Cutler, R.A.2
-
19
-
-
0025071113
-
Immunogenicity of Amodiaquine in the Rat
-
(a) Clarke, J. B.; Maggs, J. L.; Kitteringham, N. R.; Park, B. K. Immunogenicity of Amodiaquine in the Rat. Int. Arch. Allergy Appl. Immunol. 1990, 91, 335-342.
-
(1990)
Int. Arch. Allergy Appl. Immunol.
, vol.91
, pp. 335-342
-
-
Clarke, J.B.1
Maggs, J.L.2
Kitteringham, N.R.3
Park, B.K.4
-
20
-
-
0036154008
-
Amodiaquine Clearance And Its Metabolism To N-Desethylamodiaquine Is Mediated By CYP2C8: A New High Affinity And Turnover Enzyme-Specific Probe Substrate
-
(b) Li, X. Q.; Bjorkman, A.; Andersson, T. B. et al. Amodiaquine Clearance And Its Metabolism To N-Desethylamodiaquine Is Mediated By CYP2C8: A New High Affinity And Turnover Enzyme-Specific Probe Substrate. J. Pharmacol. Exp. Ther. 2002, 300, 399-407.
-
(2002)
J. Pharmacol. Exp. Ther.
, vol.300
, pp. 399-407
-
-
Li, X.Q.1
Bjorkman, A.2
Andersson, T.B.3
-
21
-
-
0036178106
-
Glucuronidation of Acetaminophen Catalyzed by Multiple Rat phenol UDP-Glucuronosyl-transferases
-
Kessler, F. K.; Kessler, M. R.; Auyeung, D. J. et al. Glucuronidation of Acetaminophen Catalyzed by Multiple Rat phenol UDP-Glucuronosyl-transferases. Drug Metab. Dispos. 2002, 30, 324-330.
-
(2002)
Drug Metab. Dispos.
, vol.30
, pp. 324-330
-
-
Kessler, F.K.1
Kessler, M.R.2
Auyeung, D.J.3
-
22
-
-
0022006971
-
Amodiaquine as a Prodrug: Importance of Metabolite(s) in the Antimalarial Effect of Amodiaquine in Humans
-
(a) Churchill, F. C.; Patchen, L. C.; Campbell, C. C.; Schwartz, I. K.; Nguyen-Dinh, P.; Dickinson, C. M. Amodiaquine as a Prodrug: Importance of Metabolite(s) in the Antimalarial Effect of Amodiaquine in Humans. Life Sci. 1985, 36, 53-62.
-
(1985)
Life Sci.
, vol.36
, pp. 53-62
-
-
Churchill, F.C.1
Patchen, L.C.2
Campbell, C.C.3
Schwartz, I.K.4
Nguyen-Dinh, P.5
Dickinson, C.M.6
-
23
-
-
0024544340
-
A Comparison of the In vitro Activities of Amodiaquine and Desethylamodiaquine Against Isolates of Plasmodium falciparum
-
(b) Childs, G. E.; Boudreau, E. F.; Milhous, W. K.; Wimonwattratee, T.; Pooyindee, N.; Pang, L.; Davidson, D. E. A Comparison of the In vitro Activities of Amodiaquine and Desethylamodiaquine Against Isolates of Plasmodium falciparum. Am. J. Trop. Med. Hyg. 1989, 40, 7-11.
-
(1989)
Am. J. Trop. Med. Hyg.
, vol.40
, pp. 7-11
-
-
Childs, G.E.1
Boudreau, E.F.2
Milhous, W.K.3
Wimonwattratee, T.4
Pooyindee, N.5
Pang, L.6
Davidson, D.E.7
-
24
-
-
0036154008
-
Amodiaquine Clearance And its Metabolism To N-Desethylamodiaquine Is Mediated By CYP2C8: A New High Affinity and Turnover Enzyme-Specific Probe Substrate
-
(c) Li, X. Q.; Bjorkman, A.; Andersson, T. B.; et al. Amodiaquine Clearance And its Metabolism To N-Desethylamodiaquine Is Mediated By CYP2C8: A New High Affinity and Turnover Enzyme-Specific Probe Substrate. J Pharmacol. Exp. Ther. 2002, 300, 399-407.
-
(2002)
J Pharmacol. Exp. Ther.
, vol.300
, pp. 399-407
-
-
Li, X.Q.1
Bjorkman, A.2
Andersson, T.B.3
-
25
-
-
85039625222
-
-
note
-
(d) A proposed solution to the problem of cross-resistance through metabolism to N-desalkyl metabolites has been offered by conversion of the N-diethylamino function of amodiaquine to either N-pyrollidino or N-tert butylamino. (see ref 28a for details). Since it has already been established that amopyroquine has excellent oral bioavailability, cyclic amine analogues such as 8a and 10a may offer metabolic advantages over isoquine if N-deethylation to desethyl isoquine is a principle route of metabolism.
-
-
-
-
26
-
-
0019188940
-
Ferriprotoporphyrin IX Fulfills the Criteria for Identification as the CQ receptor of Malaria Parasites
-
For studies on hematin 4-aminoquinoline interactions, see: (a) Chou, A. C.; Chevli, R.; Fitch, C. D. Ferriprotoporphyrin IX Fulfills the Criteria for Identification as the CQ receptor of Malaria Parasites. Biochemistry 1980, 19, 1543-1549.
-
(1980)
Biochemistry
, vol.19
, pp. 1543-1549
-
-
Chou, A.C.1
Chevli, R.2
Fitch, C.D.3
-
27
-
-
0034601111
-
Characterisation of Chloroquine-Hematin Mu-Oxo Dimer Binding by Isothermal Titration Calorimetry Biochim
-
(b) Vippagunata, S. R.; Dorn, A.; Ridley, R. G.; Vennerstrom, J. L. Characterisation of Chloroquine-Hematin Mu-Oxo Dimer Binding by Isothermal Titration Calorimetry Biochim. Biophys. Acta 2000, 1475, 133-140.
-
(2000)
Biophys. Acta
, vol.1475
, pp. 133-140
-
-
Vippagunata, S.R.1
Dorn, A.2
Ridley, R.G.3
Vennerstrom, J.L.4
-
28
-
-
0020214978
-
Interactions between Chloroquine Ferriprotoporphyrine I.X. Nuclear Magnetic-Resonance Study
-
(c) Moreau, D.; Perly, B.; Biguet, J. Interactions between Chloroquine and Ferriprotoporphyrine IX. Nuclear Magnetic-Resonance Study. Biochimie 1982, 64, 1015-1025.
-
(1982)
Biochimie
, vol.64
, pp. 1015-1025
-
-
Moreau, D.1
Perly, B.2
Biguet, J.3
-
29
-
-
0034719487
-
Structure-Function Relationships in Aminoquinolines: Effect of Amino and Chloro Groups on Quinoline-Hematin Complex Formation, Inhibition of β-Hematin Formation and Antiplasmoidal Activity
-
(d) Egan, T.; Hunter, R.; Kaschula, C. H.; Marques, H. M.; Misplon, A.; Walden, J. Structure-Function Relationships in Aminoquinolines: Effect of Amino and Chloro Groups on Quinoline-Hematin Complex Formation, Inhibition of β-Hematin Formation and Antiplasmoidal Activity. J. Med. Chem. 2000, 43, 283-291.
-
(2000)
J. Med. Chem.
, vol.43
, pp. 283-291
-
-
Egan, T.1
Hunter, R.2
Kaschula, C.H.3
Marques, H.M.4
Misplon, A.5
Walden, J.6
-
30
-
-
0035871063
-
Mechanism of Malarial Haem Detoxification inhibition by Chloroquine
-
(e) Pandey, A. V.; Bisht, H.; Babbarwal, V. K.; Srivastav, J.; Pandey, K. C.; Chauhan, V. S. Mechanism of Malarial Haem Detoxification inhibition by Chloroquine. Biochem. J. 2001, 355, 333-338.
-
(2001)
Biochem. J.
, vol.355
, pp. 333-338
-
-
Pandey, A.V.1
Bisht, H.2
Babbarwal, V.K.3
Srivastav, J.4
Pandey, K.C.5
Chauhan, V.S.6
-
31
-
-
0030870923
-
Thermodynamic Factors Controlling the Interaction of Quinoline Antimalarial Drugs with Ferriprotoporphyrin IX.J
-
(f) Egan, T. J.; Mavuso, W. W.; Ross, D. C.; Marques, H. M. Thermodynamic Factors Controlling the Interaction of Quinoline Antimalarial Drugs with Ferriprotoporphyrin IX. J. Inorg. Biochem. 1997, 68, 137-145.
-
(1997)
Inorg. Biochem.
, vol.68
, pp. 137-145
-
-
Egan, T.J.1
Mavuso, W.W.2
Ross, D.C.3
Marques, H.M.4
-
32
-
-
1542745991
-
Common Mechanism for Blockade of Heme Polymerisation by Antimalarial Quinolines
-
(f) Sullivan, D. J.; Matile, H.; Ridley, R. G.; Goldberg, D. E. A. Common Mechanism for Blockade of Heme Polymerisation by Antimalarial Quinolines. J. Biol. Chem. 1998, 272, 31103-31107.
-
(1998)
J. Biol. Chem.
, vol.272
, pp. 31103-31107
-
-
Sullivan, D.J.1
Matile, H.2
Ridley, R.G.3
Goldberg, D.E.A.4
-
33
-
-
0033523894
-
-
(g) Vippagunata, S. R.; Dorn, A.; Matile, H.; Bhattacharjee, A. K.; Karle, J. M.; Ellis, W. Y.; Ridley, R. G.; Vennerstrom, J. L. J. Med. Chem. 1999, 42, 4630-4639.
-
(1999)
J. Med. Chem.
, vol.42
, pp. 4630-4639
-
-
Vippagunata, S.R.1
Dorn, A.2
Matile, H.3
Bhattacharjee, A.K.4
Karle, J.M.5
Ellis, W.Y.6
Ridley, R.G.7
Vennerstrom, J.L.8
-
34
-
-
0031818645
-
Access to Hematin: The basis of Chloroquine resistance
-
(i) Bray, P. G.; Mungthin, M.; Ridley, R. Ward, S. A. Access to Hematin: the basis of Chloroquine resistance. Mol. Pharmacol. 1998, 54, 170-179.
-
(1998)
Mol. Pharmacol.
, vol.54
, pp. 170-179
-
-
Bray, P.G.1
Mungthin, M.2
Ridley, R.3
Ward, S.A.4
-
35
-
-
0014952885
-
Plasmodium falciparum in Owl Monkeys. Drug Resistance and CQ Binding Capacity
-
(j) Fitch, C. D. Plasmodium falciparum in Owl Monkeys. Drug Resistance and CQ Binding Capacity. Science, 1970, 169, 289-290.
-
(1970)
Science
, vol.169
, pp. 289-290
-
-
Fitch, C.D.1
-
36
-
-
0030066679
-
The Behaviour of Qinghaosu (Artemisinin) In The Presence of Heme Iron (II) and (III)
-
For the role of hematin/heme in activation of peroxides, see: (a) Haynes, R. K.; Vonwiller, S. C. The Behaviour of Qinghaosu (Artemisinin) In The Presence of Heme Iron (II) and (III) Tetrahedron Lett. 1996, 37 253-256.
-
(1996)
Tetrahedron Lett.
, vol.37
, pp. 253-256
-
-
Haynes, R.K.1
Vonwiller, S.C.2
-
37
-
-
0035207181
-
Why Artemisinin and Certain Synthetic Peroxides are Potent Antimalarials. Implications for the Mode of Action
-
(b) Jefford, C. W. Why Artemisinin and Certain Synthetic Peroxides are Potent Antimalarials. Implications for the Mode of Action. Curr. Med. Chem. 2001, 8, 1803-1826.
-
(2001)
Curr. Med. Chem.
, vol.8
, pp. 1803-1826
-
-
Jefford, C.W.1
-
38
-
-
0034864129
-
New Class of Small Nonpeptidyl Compounds Blocks Plasmodium falciparum Development In vitro by Inhibiting Plasmepsins
-
(a) Jiang S. P.; Prigge S. T.; Wei, L., et al. New Class of Small Nonpeptidyl Compounds Blocks Plasmodium falciparum Development In vitro by Inhibiting Plasmepsins. Antimicrob. Agents 2001, 45, 2577-2584.
-
(2001)
Antimicrob. Agents
, vol.45
, pp. 2577-2584
-
-
Jiang, S.P.1
Prigge, S.T.2
Wei, L.3
-
39
-
-
0031691453
-
Antimalarial Synergy of Cysteine and Aspartic Protease Inhibitors
-
(b) Semenov, A.; Olson, J. E.; Rosenthal, P. J. Antimalarial Synergy of Cysteine and Aspartic Protease Inhibitors. Antimicrob. Agents 1998, 42, 2254-2258.
-
(1998)
Antimicrob. Agents
, vol.42
, pp. 2254-2258
-
-
Semenov, A.1
Olson, J.E.2
Rosenthal, P.J.3
-
40
-
-
0033057631
-
Antimalarial Effects in Mice of Orally Administered Peptidyl Cysteine Protease Inhibitors
-
(c) Olson, J. E.; Garson, K. Lee, G. K.; Semenov, A.; Rosenthal, P. J. Antimalarial Effects in Mice of Orally Administered Peptidyl Cysteine Protease Inhibitors. Biol. Med. Chem. 1999, 7, 633-638.
-
(1999)
Biol. Med. Chem.
, vol.7
, pp. 633-638
-
-
Olson, J.E.1
Garson, K.2
Lee, G.K.3
Semenov, A.4
Rosenthal, P.J.5
-
41
-
-
0034831503
-
Transport proteins of Plasmodium falciparum: Defining the limits of metabolism
-
Krishna, S.; Webb, R.;, Woodrow, C. Transport proteins of Plasmodium falciparum: defining the limits of metabolism. Intern. J. Parasitol. 2001, 31, 1331-1342.
-
(2001)
Intern. J. Parasitol.
, vol.31
, pp. 1331-1342
-
-
Krishna, S.1
Webb, R.2
Woodrow, C.3
-
42
-
-
0033646097
-
Atovaquone Resistance in Malaria Parasites
-
Vaidya, A. B.; Mather, M. W. Atovaquone Resistance in Malaria Parasites. Drug Resist. Update 2000, 3, 283-287.
-
(2000)
Drug Resist. Update
, vol.3
, pp. 283-287
-
-
Vaidya, A.B.1
Mather, M.W.2
-
43
-
-
0033614986
-
New 4-Aminoquinoline Mannich Base Antimalarials 1. Effect of an Alkyl Substituent in the 5′-Position of the 4′-Hydroxylanilino Side Chain
-
(a)Raynes, K. J.; Stocks, P. A.; O'Neill, P. M.; Park, B. K.; Ward, S. A. New 4-Aminoquinoline Mannich Base Antimalarials 1. Effect of an Alkyl Substituent in the 5′-Position of the 4′-Hydroxylanilino Side Chain. J. Med. Chem. 1999, 42, 2747-2751.
-
(1999)
J. Med. Chem.
, vol.42
, pp. 2747-2751
-
-
Raynes, K.J.1
Stocks, P.A.2
O'Neill, P.M.3
Park, B.K.4
Ward, S.A.5
-
44
-
-
0031916653
-
The Relationship Between Antimalarial Activity, Accumulation and Inhibition of Haem Polymerisation in Plasmodium falciparum in Vitro
-
(b) Hawley, S. R.; Bray, P. G.; Mungthin, M.; Atkinson, J. D.; O'Neill, P. M.; Ward, S. A. The Relationship Between Antimalarial Activity, Accumulation and Inhibition of Haem Polymerisation in Plasmodium falciparum in Vitro. Antimicrob. Agents Chemother. 1998, 42, 682-686.
-
(1998)
Antimicrob. Agents Chemother.
, vol.42
, pp. 682-686
-
-
Hawley, S.R.1
Bray, P.G.2
Mungthin, M.3
Atkinson, J.D.4
O'Neill, P.M.5
Ward, S.A.6
-
45
-
-
0032580374
-
Synthesis of the 8-Aminoquinoline Antimalarial 5-Fluoroprimaquine
-
O'Neill, P. M.; Storr, R. C.; Park, B. K. Synthesis of the 8-Aminoquinoline Antimalarial 5-Fluoroprimaquine. Tetrahedron 1998, 4615-4622.
-
(1998)
Tetrahedron
, pp. 4615-4622
-
-
O'Neill, P.M.1
Storr, R.C.2
Park, B.K.3
-
46
-
-
0031660992
-
Effect of disposition of Mannich Antimalarial Agents on Their Pharmacology and Toxicology, Antimicrob
-
Ruscoe, J. E.; Tingle, M. D.; O'Neill, P. M.; Ward, S. A.; Park, B. K. Effect of disposition of Mannich Antimalarial Agents on Their Pharmacology and Toxicology, Antimicrob. Agents Chemother. 1998, 42, 2410-2416.
-
(1998)
Agents Chemother.
, vol.42
, pp. 2410-2416
-
-
Ruscoe, J.E.1
Tingle, M.D.2
O'Neill, P.M.3
Ward, S.A.4
Park, B.K.5
-
47
-
-
0032410803
-
Metabolism-dependent Neutrophil Toxicity of Amodiaquine: A Comparison with Pyronaridine and related Antimalarial Drugs
-
Naisbitt, D. N.; Maggs, J. L.; Pirmohamed, MP.; O'Neill, P. M.; Park, B. K, Metabolism-dependent Neutrophil Toxicity of Amodiaquine: A Comparison with Pyronaridine and related Antimalarial Drugs. Chem. Res. Toxicol. 1998, 11 (12), 1586-1595.
-
(1998)
Chem. Res. Toxicol.
, vol.11
, Issue.12
, pp. 1586-1595
-
-
Naisbitt, D.N.1
Maggs, J.L.2
Pirmohamed, M.P.3
O'Neill, P.M.4
Park, B.K.5
-
48
-
-
0030894527
-
Disposition of Amodiaquine and Related Antimalarials in Human Leucocytes: Implications for Drug Design
-
Naisbitt, D. J.; Ruscoe, J. E.; Williams, D.; O'Neill, P. M.; Pirmohamed, M.; Park, B. K.; Disposition of Amodiaquine and Related Antimalarials in Human Leucocytes: Implications for Drug Design. J. Pharmacol. Exp. Ther. 1997, 280, 884-893.
-
(1997)
J. Pharmacol. Exp. Ther.
, vol.280
, pp. 884-893
-
-
Naisbitt, D.J.1
Ruscoe, J.E.2
Williams, D.3
O'Neill, P.M.4
Pirmohamed, M.5
Park, B.K.6
-
49
-
-
0029988111
-
The Effect of Fluorine Substitution on the Antimalarial Activity of Tebuquine
-
O'Neill, P., M.; Hawley, S. R.; Storr, R. C.; Ward, S. A.; Park, B. K. The Effect of Fluorine Substitution on the Antimalarial Activity of Tebuquine. Biol. Med. Chem. Lett. 1996, 6, 391-392.
-
(1996)
Biol. Med. Chem. Lett.
, vol.6
, pp. 391-392
-
-
O'Neill, P.M.1
Hawley, S.R.2
Storr, R.C.3
Ward, S.A.4
Park, B.K.5
-
50
-
-
0030582428
-
The Role of Drug Accumulation in 4-Aminoquinoline Antimalarial Potency -the Influence of Structural Substitution and Physicochemical Properties
-
(a) Hawley, S. R.; Bray, P. G.; O'Neill, P. M.; Park, B. K.; Ward, S. A. The Role of Drug Accumulation in 4-Aminoquinoline Antimalarial Potency -the Influence of Structural Substitution and Physicochemical Properties, Biochem. Pharmacol. 1996, 52, 723-733.
-
(1996)
Biochem. Pharmacol.
, vol.52
, pp. 723-733
-
-
Hawley, S.R.1
Bray, P.G.2
O'Neill, P.M.3
Park, B.K.4
Ward, S.A.5
-
51
-
-
0037020024
-
-
(b) For a study demonstrating that pfcrt mutations have little effect on amodiaquine activity in contrast to chloroquine, see: Sidhu, A. B.; Verdier-Pinard, D.; Fidock, D. A. Science 2002, 298 (5591), 74-75.
-
(2002)
Science
, vol.298
, Issue.5591
, pp. 74-75
-
-
Sidhu, A.B.1
Verdier-Pinard, D.2
Fidock, D.A.3
-
52
-
-
0029817144
-
Manipulation of the N-Alkyl Substituent in Amodiaquine to Overcome the Verapamil Sensitive Chloroquine Resistance Mechanism
-
(a) Hawley, S. R.; Bray, P. G. O'Neill, P. M.; Naisbitt, D. J.; Park, B. K.; Ward, S. A.; Manipulation of the N-Alkyl Substituent in Amodiaquine to Overcome the Verapamil Sensitive Chloroquine Resistance Mechanism. Antimicrob. Agents Chemother. 1996, 40, 2345-2349.
-
(1996)
Antimicrob. Agents Chemother.
, vol.40
, pp. 2345-2349
-
-
Hawley, S.R.1
Bray, P.G.2
O'Neill, P.M.3
Naisbitt, D.J.4
Park, B.K.5
Ward, S.A.6
-
53
-
-
0028802468
-
The Bioactivation of Amodiaquine by Human Polymorphonuclear Leukocytes In-Vitro - Chemical Mechanisms and the Effects of Fluorine Substitution
-
(b) Tingle, M. D.; Jewell, H.; Maggs, J. L; O'Neill, P. M.; Park, B. K. The Bioactivation of Amodiaquine by Human Polymorphonuclear Leukocytes In-Vitro - Chemical Mechanisms and the Effects of Fluorine Substitution. Biochem. Pharmacol. 1995, 50, 1113-1119.
-
(1995)
Biochem. Pharmacol.
, vol.50
, pp. 1113-1119
-
-
Tingle, M.D.1
Jewell, H.2
Maggs, J.L.3
O'Neill, P.M.4
Park, B.K.5
-
54
-
-
0028920789
-
The Effect of Chemical Substitution on the Metabolic-Activation, Metabolic Detoxication, and Pharmacological Activity of Amediaquine in the Mouse
-
(c) Ruscoe, J. E.; Jewell, H.; Maggs, J. L.; O'Neill, P. M.; Storr, R. C.; Ward, S. A.; Park, B. K. The Effect of Chemical Substitution on the Metabolic-Activation, Metabolic Detoxication, and Pharmacological Activity of Amediaquine in the Mouse. J. Pharm. Exp. Ther. 1995, 273, 393-404.
-
(1995)
J. Pharm. Exp. Ther.
, vol.273
, pp. 393-404
-
-
Ruscoe, J.E.1
Jewell, H.2
Maggs, J.L.3
O'Neill, P.M.4
Storr, R.C.5
Ward, S.A.6
Park, B.K.7
-
55
-
-
0030451452
-
Physiochemical Properties Correlated with Drug Resistance and the Reversal of Drug Resistance in Plasmodium falciparum
-
(d) Bray, P. G.; Hawley, S. R.; Mungthin, M.; Ward, S. A. Physiochemical Properties Correlated with Drug Resistance and the Reversal of Drug Resistance in Plasmodium falciparum. Mol. Pharmacol. 1996, 50, 1559-1566.
-
(1996)
Mol. Pharmacol.
, vol.50
, pp. 1559-1566
-
-
Bray, P.G.1
Hawley, S.R.2
Mungthin, M.3
Ward, S.A.4
-
56
-
-
0035899179
-
Synthesis and in Vitro and in Vivo Antimalarial Activity of New 4-Anilinoquinolines
-
(e) Delarue, S.; Girault, S.; Maes, L.; Debreu-Fontaine, M.-A.; Mehdi, L.; Grellier, P.; Sergheraert, C. Synthesis and in Vitro and in Vivo Antimalarial Activity of New 4-Anilinoquinolines. J. Med. Chem. 2001, 44, 2827-2833.
-
(2001)
J. Med. Chem.
, vol.44
, pp. 2827-2833
-
-
Delarue, S.1
Girault, S.2
Maes, L.3
Debreu-Fontaine, M.-A.4
Mehdi, L.5
Grellier, P.6
Sergheraert, C.7
-
57
-
-
31544439163
-
Potential Antimalarials. VIII. Mono- and di-Mannich Bases of 2-(7′-trifluoromethylquinolin-4′-ylamino)phenol via 2-Nitrophenols
-
(a) Barlin, G. B.; Yan, H. Potential Antimalarials. VIII. Mono- and di-Mannich Bases of 2-(7′-trifluoromethylquinolin-4′-ylamino)phenol via 2-Nitrophenols. Aust. J. Chem. 1989, 42, 2191-2199.
-
(1989)
Aust. J. Chem.
, vol.42
, pp. 2191-2199
-
-
Barlin, G.B.1
Yan, H.2
-
58
-
-
0000343954
-
Potential antimalarials. XV. Di-Mannich bases of 2-[7-chloroquinolin-4′ylamino]phenol and 2-[7′-bromo(and trifluoromethyl)-1′,5′-naphthyridin-4′-ylamino]phenol
-
(b) Barlin, G. B.; Nguyen, T. M. T.; Kotecka, B.; Rieckmann, K. H. Potential antimalarials. XV. Di-Mannich bases of 2-[7-chloroquinolin-4′ ylamino]phenol and 2-[7′-bromo(and trifluoromethyl)-1′,5′ -naphthyridin-4′-ylamino]phenol. Aust. J. Chem. 1992, 45, 1651-1662.
-
(1992)
Aust. J. Chem.
, vol.45
, pp. 1651-1662
-
-
Barlin, G.B.1
Nguyen, T.M.T.2
Kotecka, B.3
Rieckmann, K.H.4
-
59
-
-
0026672298
-
The In vitro and In vivo Antimalarial Activity of Some Mannich bases Derived from 4-(7′-trifluorome-thyl-1′,5′ -naphthyridin-4′-ylamino)phenol, 2-(7′-trifluoro methyl-quinolin-4′-ylamino)phenol, and 4′-chloro-5-(7″ -trifluoro-methylquinolin-4″ylamino)biphenyl-2-ols
-
(c) Barlin, G. B.; Jiravinyu, C.; Butcher, G. A.; Kotecka, B.; Rieckmann, K. The In vitro and In vivo Antimalarial Activity of Some Mannich bases Derived from 4-(7′-trifluorome-thyl-1′,5′ -naphthyridin-4′-ylamino)phenol, 2-(7′-trifluoro methyl-quinolin-4′-ylamino)phenol, and 4′-chloro-5-(7″ -trifluoro-methylquinolin-4″ylamino)biphenyl-2-ols. Ann. Trop. Med. Parasitol. 1992, 86, 323-331.
-
(1992)
Ann. Trop. Med. Parasitol.
, vol.86
, pp. 323-331
-
-
Barlin, G.B.1
Jiravinyu, C.2
Butcher, G.A.3
Kotecka, B.4
Rieckmann, K.5
-
60
-
-
9444258557
-
4-Aminoquinoline Analogues of CQ with Shortened Side Chains Retain Activity Against CQ resistant Plasmodium falciparum
-
Ridley, R. G.; Hofheinz, H.; Matile, H.; Jaquet, C.; Dorn, A.; Masciadri, R.; Jolidon, S.; Richter, W. F.; Guenzi, A.; Girometta, M. A.; Urwyler, H.; Huber, W.; Thiathong, S. Peters, W. 4-Aminoquinoline Analogues of CQ with Shortened Side Chains Retain Activity Against CQ resistant Plasmodium falciparum. Antimicrob. Chemother. 1996, 40, 1846-1854.
-
(1996)
Antimicrob. Chemother.
, vol.40
, pp. 1846-1854
-
-
Ridley, R.G.1
Hofheinz, H.2
Matile, H.3
Jaquet, C.4
Dorn, A.5
Masciadri, R.6
Jolidon, S.7
Richter, W.F.8
Guenzi, A.9
Girometta, M.A.10
Urwyler, H.11
Huber, W.12
Thiathong, S.13
Peters, W.14
-
61
-
-
0030483601
-
Aminoquinolines that Circumvent Resistance in Plasmodium falciparum in vitro
-
(a) De, D.; Krogstad, F. M.; Cogswell, F. B.; Krogstad, D. J. Aminoquinolines that Circumvent Resistance in Plasmodium falciparum in vitro. Am. J. Trop. Med. Hyg. 1996, 55, 579-583.
-
(1996)
Am. J. Trop. Med. Hyg.
, vol.55
, pp. 579-583
-
-
De, D.1
Krogstad, F.M.2
Cogswell, F.B.3
Krogstad, D.J.4
-
62
-
-
0032481004
-
Structure-activity Relationships for Antiplasmodial Activity Among 7-Substituted 4-Aminoquinolines
-
(b) De, D.; Krogstad, F. M.; Byers, L. D.; Krogstad, D. J. Structure-activity Relationships for Antiplasmodial Activity Among 7-Substituted 4-Aminoquinolines. J. Med. Chem. 1998, 41, 4918-4926.
-
(1998)
J. Med. Chem.
, vol.41
, pp. 4918-4926
-
-
De, D.1
Krogstad, F.M.2
Byers, L.D.3
Krogstad, D.J.4
-
63
-
-
0037038320
-
Novel Short Chain Chloroquine Analogues Retain Activity Against Chloroquine Resistant K1 Plasmodium falciparum
-
Stocks, P. A.; Raynes, K. A.; Bray, P. G.; Park, B. K.; O'Neill, PM.; Ward, S. A. Novel Short Chain Chloroquine Analogues Retain Activity Against Chloroquine Resistant K1 Plasmodium falciparum. J. Med. Chem, 2002, 45, 4975-4983.
-
(2002)
J. Med. Chem.
, vol.45
, pp. 4975-4983
-
-
Stocks, P.A.1
Raynes, K.A.2
Bray, P.G.3
Park, B.K.4
O'Neill, P.M.5
Ward, S.A.6
-
64
-
-
0017311840
-
Human Malaria Parasites in Continuous Culture
-
Trager, W.; Jenson, J. B. Human Malaria Parasites in Continuous Culture. Science 1976, 193, 673-675.
-
(1976)
Science
, vol.193
, pp. 673-675
-
-
Trager, W.1
Jenson, J.B.2
-
65
-
-
0018606732
-
Quantitative Assessment of Antimalarial activity in vitro by Semi-automated Microdilution Technique
-
Desjardins, R. E.; Canfield, C. J.; Haynes, J. D.; Chulay, J. D. Quantitative Assessment of Antimalarial activity in vitro by Semi-automated Microdilution Technique. Antimicrob. Agents Chemother. 1979, 16, 710-718.
-
(1979)
Antimicrob. Agents Chemother.
, vol.16
, pp. 710-718
-
-
Desjardins, R.E.1
Canfield, C.J.2
Haynes, J.D.3
Chulay, J.D.4
-
67
-
-
85039616598
-
-
AntiMalarial Compounds. WO 02/072554 A1, Sept 19, 2002, PCT/GB02/01410 (Mar 14, 2002)
-
Park, B. K.; O'Neill, P. M.; Ward, S. A.; Stocks, P. A. AntiMalarial Compounds. WO 02/072554 A1, Sept 19, 2002, PCT/GB02/01410 (Mar 14, 2002).
-
-
-
Park, B.K.1
O'Neill, P.M.2
Ward, S.A.3
Stocks, P.A.4
|