Identification of new antileishmanial leads from hits obtained by high-throughput screening

Antimicrobial Agents and Chemotherapy

Volumn 56, Issue 3, 2012, Pages 1182-1189

  Zhu, Xiaohua ^a   Pandharkar, Trupti ^a   Werbovetz, Karl ^a  

^a OHIO STATE UNIVERSITY   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

(2 HYDROXYPROPYL)BETA CYCLODEXTRIN; ANTILEISHMANIAL AGENT; BENZOTHIAZOLE DERIVATIVE; BETA CYCLODEXTRIN; BETA LACTAMASE; CYANINE DYE; MILTEFOSINE; PODOPHYLLOTOXIN DERIVATIVE; THIAZOLE ORANGE; UNCLASSIFIED DRUG;

AMASTIGOTE; ANIMAL CELL; ANIMAL MODEL; ARTICLE; BODY WEIGHT; COMMERCIAL PHENOMENA; CONCENTRATION (PARAMETERS); CONTROLLED STUDY; CYTOTOXICITY; DATA BASE; DRUG EFFICACY; DRUG IDENTIFICATION; DRUG SCREENING; IN VITRO STUDY; LEISHMANIA; LEISHMANIA DONOVANI; LEISHMANIA MAJOR; MOUSE; NONHUMAN; PARASITEMIA; PRIORITY JOURNAL; PROMASTIGOTE; VERO CELL; VISCERAL LEISHMANIASIS;

ANIMALS; BENZOTHIAZOLES; CARBOCYANINES; CELL SURVIVAL; CERCOPITHECUS AETHIOPS; DATABASES, FACTUAL; FEMALE; HIGH-THROUGHPUT SCREENING ASSAYS; INHIBITORY CONCENTRATION 50; LEISHMANIA; LEISHMANIA DONOVANI; LIVER; MACROPHAGES; MICE; MICE, INBRED BALB C; TRYPANOCIDAL AGENTS; VERO CELLS;

EID: 84863116413     PISSN: 00664804     EISSN: 10986596     Source Type: Journal    
DOI: 10.1128/AAC.05412-11     Document Type: Article

References (45)

1. Berman J, et al. 1998. Efficacy and safety of liposomal amphotericin B (AmBisome) for visceral leishmaniasis in endemic developing countries. Bull. World Health Organ. 76:25-32. (Pubitemid 28254976)
2. Delfín D, Bhattacharjee A, Yakovich A, Werbovetz K. 2006. Activity of and initial mechanistic studies on a novel antileishmanial agent identified through in silico pharmacophore development and database searching. J. Med. Chem. 49:4196-4207. (Pubitemid 44036663)
3. Delfín D, Morgan R, Zhu X, Werbovetz K. 2009. Redox-active dinitrophenylthioethers against Leishmania: synthesis, structure-activity relationships and mechanism of action studies. Bioorg. Med. Chem. 17:820-829.
4. de Morais-Teixeira E, Damasceno Q, Galuppo M, Romanha A, Rabello A. 2011. The in vitro leishmanicidal activity of hexadecylphosphocholine (miltefosine) against four medically relevant Leishmania species of Brazil. Mem. Inst. Oswaldo Cruz 106:475-478.
5. De Muylder G, et al. 2011. A screen against Leishmania intracellular amastigotes: comparison to a promastigote screen and identification of a host cell-specific hit. PLoS Negl. Trop. Dis. 5:e1253.
6. 3 (edelfosine) and amphotericin B. Acta Trop. 81:151-157.
7. Gamo F, et al. 2010. Thousands of chemical starting points for antimalarial lead identification. Nature 465:305-310.
8. Guiguemde W, et al. 2010. Chemical genetics of Plasmodium falciparum. Nature 465:311-315.
9. Hailu A, et al. 2010. Geographical variation in the response of visceral leishmaniasis to paromomycin in East Africa: a multicentre, open-label, randomized trial. PLoS Negl. Trop. Dis. 4:e709.
10. Khatami A, Firooz A, Gorouhi F, Dowlati Y. 2007. Treatment of acute Old World cutaneous leishmaniasis: a systematic review of the randomized controlled trials. J. Am. Acad. Dermatol. 57:335.e1-e29.
11. Mackey A, et al. 2006. Discovery of trypanocidal compounds by whole cell HTS of Trypanosoma brucei. Chem. Biol. Drug Des. 67:355-363.
12. Matlashewski G, et al. 2011. Visceral leishmaniasis: elimination with existing interventions. Lancet Infect. Dis. 11:322-325.
13. Mishra A, Behera R, Behera P, Mishra B, Behera G. 2000. Cyanines during the 1990s: a review. Chem. Rev. 100:1973-2011.
14. Mueller M, et al. 2007. Unresponsiveness to AmBisome in some Sudanese patients with kala-azar. Trans. R. Soc. Trop. Med. Hyg. 101:19-24. (Pubitemid 44660703)
15. Murray H, Berman J, Davies C, Saravia N. 2005. Advances in leishmaniasis. Lancet 366:1561-1577. (Pubitemid 41540115)
16. Musa A, et al. 2010. Paromomycin for the treatment of visceral leishmaniasis in Sudan: a randomized, open-label, dose-finding study. PLoS Negl. Trop. Dis. 4:e855.
17. Neal R, Allen S, McCoy N, Olliaro P, Croft S. 1995. The sensitivity of Leishmania species to aminosidine. J. Antimicrob. Chemother. 35:577-584.
18. Oliveira A, et al. 2009. Severe adverse reactions to meglumine antimoniate in the treatment of visceral leishmaniasis: a report of 13 cases in the southwestern region of Brazil. Trop. Doct. 39:180-182.
19. Palumbo E. 2009. Current treatment for cutaneous leishmaniasis: a review. Am. J. Ther. 16:178-182.
20. Pucadyil T, Tewary P, Madhubala R, Chattopadhyay A. 2004. Cholesterol is required for Leishmania donovani infection: implications in leishmaniasis. Mol. Biochem. Parasitol. 133:145-152. (Pubitemid 38032863)
21. Pudhom K, et al. 2009. Synthesis and biological properties of a rhodacyanine derivative, SSJ-127, having high efficacy against malaria protozoa. Heterocycles 77:207-210.
22. Pudhom K, et al. 2006. Synthesis of three classes of rhodacyanine dyes and evaluation of their in vitro and in vivo antimalarial activity. Bioorg. Med. Chem. 14:8550-8563. (Pubitemid 44755266)
23. Rijal S, et al. 2003. Sodium stibogluconate cardiotoxicity and safety of generics. Trans. R. Soc. Trop. Med. Hyg. 97:597-598. (Pubitemid 40590103)
24. Romero G, Boelaert M. 2010. Control of visceral leishmaniasis in Latin America - a systematic review. PLoS Negl. Trop. Dis. 4:e584.
25. Salem M, Werbovetz K. 2005. Antiprotozoal compounds from Psorothamnus polydenius. J. Nat. Prod. 68:108-111. (Pubitemid 40175942)
26. Seaman J, et al. 1995. Liposomal amphotericin B (AmBisome) in the treatment of complicated kala-azar under field conditions. Clin. Infect. Dis. 21:188-193.
27. Sharlow E, et al. 2009. Identification of potent chemotypes targeting Leishmania major using a high-throughput, low-stringency, computationally enhanced, small molecule screen. PLoS Negl. Trop. Dis. 3:e540.
28. Siqueira-Neto J, et al. 2010. Antileishmanial high-throughput drug screening reveals drug candidates with new scaffolds. PLoS Negl. Trop. Dis. 4:e675.
29. Soto J, et al. 2004. Miltefosine for New World cutaneous leishmaniasis. Clin. Infect. Dis. 38:1266-1272. (Pubitemid 38608569)
30. Sundar S, Chakravarty J, Agarwal D, Rai M, Murray H. 2010. Single-dose liposomal amphotericin B for visceral leishmaniasis in India. N. Engl. J. Med. 362:504-512.
31. Sundar S, et al. 2000. Failure of pentavalent antimony in visceral leishmaniasis in India: report from the center of the Indian epidemic. Clin. Infect. Dis. 31:1104-1107. (Pubitemid 32299375)
32. Sundar S, et al. 2008. New treatment approach in Indian visceral leishmaniasis: single-dose liposomal amphotericin B followed by short-course oral miltefosine. Clin. Infect. Dis. 47:1000-1006.
33. Sundar S, et al. 2011. Comparison of short-course multidrug treatment with standard therapy for visceral leishmaniasis in India: an open-label, non-inferiority, randomised controlled trial. Lancet 377:477-486.
34. Takasu K, et al. 2002. Rhodacyanine dyes as antimalarials. 1. Preliminary evaluation of their activity and toxicity. J. Med. Chem. 45:995-998. (Pubitemid 34173909)
35. Takasu K, Pudhom K, Kaiser M, Brun R, Ihara M. 2006. Synthesis and antimalarial efficacy of aza-fused rhodacyanines in vitro and in the P. berghei mouse model. J. Med. Chem. 49:4795-4798. (Pubitemid 44162709)
36. Takasu K, et al. 2004. Antileishmanial activities of rhodacyanine dyes. Heterocycles 64:215-221.
37. Tilton F, La Du J, Vue M, Alzarban N, Tanguay R. 2006. Dithiocarbamates have a common toxic effect on zebrafish body axis formation. Toxicol. Appl. Pharmacol. 216:55-68. (Pubitemid 44402632)
38. Tuon F, et al. 2008. Treatment of New World cutaneous leishmaniasis - a systematic review with a meta-analysis. Int. J. Dermatol. 47:109-124.
39. van Boxtel A, et al. 2010. Dithiocarbamates induce craniofacial abnormalities and downregulate sox9a during zebrafish development. Toxicol. Sci. 117:209-217.
40. van der Meide W, et al. 2009. Evaluation of treatment with pentamidine for cutaneous leishmaniasis in Suriname. Int. J. Dermatol. 48:52-58.
41. Vélez I, et al. 2010. Efficacy of miltefosine for the treatment of American cutaneous leishmaniasis. Am. J. Trop. Med. Hyg. 83:351-356.
42. Wang M, et al. 2010. Novel arylimidamides for the treatment of visceral leishmaniasis. Antimicrob. Agents Chemother. 54:2507-2516.
43. Wasan E, et al. 2010. A novel tropically stable oral amphotericin B formulation (iCo-010) exhibits efficacy against visceral leishmaniasis in a murine model. PLoS Negl. Trop. Dis. 4:e913.
44. Wasan K, et al. 2009. Highly effective oral amphotericin B formulation against murine visceral leishmaniasis. J. Infect. Dis. 200:357-360.
45. Yang M, et al. 2010. Fluorinated rhodacyanine (SJL-01) possessing high efficacy for visceral leishmaniasis (VL). J. Med. Chem. 53:368-373.