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2
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1542332577
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note
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See ref3 for a selected list of our publications in this area since 1993.
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3
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0037464497
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Further studies on 2,4-diamino-5-(2′,5′-disubstituted benzyl)pyrimidines as potent and selective inhibitors of dihydrofolate reductases from three major opportunistic pathogens of AIDS
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Rosowsky, A.; Forsch, R. A.; Queener, S. F. Further studies on 2,4-diamino-5-(2′,5′-disubstituted benzyl)pyrimidines as potent and selective inhibitors of dihydrofolate reductases from three major opportunistic pathogens of AIDS. J. Med. Chem. 2003, 46, 1726-1736.
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Inhibition of Pneumocystis carinii, Toxoplasma gondii, and Mycobacterium avium dihydrofolate reductases by 2,4-diamino-[2-methoxy-5-(ω -carboxyalkyloxy)benzyl]pyrimidines: Marked improvement in potency relative to trimethoprim and species selectivity relative to piritrexim
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Rosowsky, A.; Forsch, R. A.; Queener, S. F. Inhibition of Pneumocystis carinii, Toxoplasma gondii, and Mycobacterium avium dihydrofolate reductases by 2,4-diamino-[2-methoxy-5-(ω-carboxyalkyloxy)benzyl]pyrimidines: Marked improvement in potency relative to trimethoprim and species selectivity relative to piritrexim. J. Med. Chem. 2002, 45, 233-241.
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Kuyper, L. F.; Roth, B.; Baccanari, D. P.; Ferone, R.; Beddell, C. R.; Champness, J. N.; Stammers, D. K.; Dann, J. G.; Norrington, F. E.; Baker, D. J. ; Goodford, P. J. Receptor-based design of dihydrofolate reductase inhibitors: comparison of crystallographically determined enzyme binding with enzyme affinity in a series of carboxy-substituted trimethoprim analogues. J. Med. Chem. 1985, 28, 303-311.
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1542362389
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note
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Structural studies are planned on the ternary complexes of 15 and 28 with PcDHFR and NADPH in order to determine the 3D orientation of the COOH group in relation to the benzyl moiety (V. Cody, personal communication).
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10
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1542272475
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note
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Work on the structure of Tg DHFR ternary complexes with several of the compounds in this paper is currently in progress in the laboratory of Dr. Amy Anderson at Dartmouth College and will be reported in due course.
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11
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0033802522
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Antimycobacterial activities of 2,4-diamino-5-deazapteridine derivatives and effects on mycobacterial dihydrofolate reductase
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Suling, W. J.; Seitz, L. E.; Pathak, V.; Westbrook, L.; Barrow, E. W.; Zywno-van Ginkel, S.; Reynolds, R. C.; Piper, J. R.; Barrow, W. R. Antimycobacterial activities of 2,4-diamino-5-deazapteridine derivatives and effects on mycobacterial dihydrofolate reductase. Antimicrob. Agents Chemother. 2000, 44, 2784-2793.
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Reynolds, R.C.7
Piper, J.R.8
Barrow, W.R.9
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0034864126
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Isolation of rat dihydrofolate reductase gene and characterization of recombinant enzyme
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Wang, Y.; Bruenn, J. A.; Queener, S. F.; Cody, V. Isolation of rat dihydrofolate reductase gene and characterization of recombinant enzyme. Antimicrob. Agents Chemother. 2001, 45, 2517-2523.
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0035171461
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Activity of moxifloxacin by itself and in combination with ethambutol, rifabutin, and azithromycin in vitro and in vivo against Mycobacterium avium
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Bermudez, L. E.; Inderlied, C. B.; Kolonoski, P.; Petrofsky, M.; Aralar, P.; Wu, M.; Young, L. S. Activity of moxifloxacin by itself and in combination with ethambutol, rifabutin, and azithromycin in vitro and in vivo against Mycobacterium avium. Antimicrob. Agents Chemother. 2001, 45, 217-222.
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Aralar, P.5
Wu, M.6
Young, L.S.7
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14
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1542332580
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note
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We are indebted to Dr. Chris Lambros of the AIDS Opportunistic Infections Program of the NIAID, Bethesda, MD, for kindly arranging to have these assays performed.
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15
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0028243447
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In vitro susceptibility of clinical isolates of Mycobacterium avium and M. intracellulare to folate antagonists
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Raszka, W. V., Jr.; Skillman, L. P.; McEvoy, P. L. In vitro susceptibility of clinical isolates of Mycobacterium avium and M. intracellulare to folate antagonists. Diagn. Microbiol. Infect. Dis. 1994, 18, 201-204.
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Response to treatment of infection due to Mycobacterium avium complex with trimethoprim-sulfamethoxazole
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Effectiveness of various antimicrobial agents against Mycobacterium avium complex in the beige mouse model
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Ji, B.; Lounis, N.; Truffot-Pernot, C.; Grosset, J. Effectiveness of various antimicrobial agents against Mycobacterium avium complex in the beige mouse model. Antimicrob. Agents Chemother. 1994, 38, 2521-2529.
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18
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0032876004
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Mefloquine is active in vitro and in vivo against Mycobacterium avium complex
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Bermudez, L. L.; Kolonoski, P.; Wu, M.; Aralar, P. A.; Inderlied, C. B.; Young, L. S. Mefloquine is active in vitro and in vivo against Mycobacterium avium complex. Antimicrob. Agents Chemother. 1999, 43, 1870-1874.
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Young, L.S.6
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19
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0031982891
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Emergence of Mycobacterium avium populations resistant to macrolides during experimental chemotherapy
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Bermudez, L. E.; Petrofsky, M.; Kolonoski, P.; Young, L. S. Emergence of Mycobacterium avium populations resistant to macrolides during experimental chemotherapy. Antimicrob. Agents Chemother. 1998, 42, 180-183.
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0028072216
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Clarithromycin, dapsone, and a combination of both used to treat of prevent disseminated Mycobacterium avium infection in beige mice
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Bermudez, L. E.; Inderlied, C. B.; Kolonoski, P.; Petrofsky, M.; Young, L. S. Clarithromycin, dapsone, and a combination of both used to treat of prevent disseminated Mycobacterium avium infection in beige mice. Antimicrob. Agents Chemother. 1994, 38, 2717-2721.
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Young, L.S.5
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21
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0028921162
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Intracellular activities of roxithromycin used alone and in association with other drugs against Mycobacterium avium complex in human macrophages
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Rastogi, N.; Labrousse, V.; Bryskier, A. Intracellular activities of roxithromycin used alone and in association with other drugs against Mycobacterium avium complex in human macrophages. Antimicrob. Agents Chemother. 1995, 39, 976-978.
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0030052421
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Identification of a class of sulfonamides highly active against dihydropteroate synthase from Toxoplasma gondii, Pneumocystis carinii, and Mycobacterium avium
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Chio, L. C.; Bolyard, L. A.; Nasr, M.; Queener, S. F. Identification of a class of sulfonamides highly active against dihydropteroate synthase from Toxoplasma gondii, Pneumocystis carinii, and Mycobacterium avium. Antimicrob. Agents Chemother. 1996, 40, 727-733.
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24
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0034063524
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Identification of Cryptosporidium parvum dihydrofolate reductase inhibitors by complementation in Saccharomyces cerivisiae
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Brophy, V. H.; Vasquez, J.; Nelson, R. G.; Forney, J. R.; Rosowsky, A.; Sibley, C. H. Identification of Cryptosporidium parvum dihydrofolate reductase inhibitors by complementation in Saccharomyces cerivisiae. Antimicrob. Agents Chemother. 2000, 44, 1019-1028.
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Nelson, R.G.3
Forney, J.R.4
Rosowsky, A.5
Sibley, C.H.6
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25
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0035165406
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Efficacies of lipophilic inhibitors of dihydrofolate reductase against parasitic protozoa
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Lau, H.; Ferlan, J. T.; Brophy, V. H.; Rosowsky, A.; Sibley, C. H. Efficacies of lipophilic inhibitors of dihydrofolate reductase against parasitic protozoa. Antimicrob. Agents Chemother. 2001, 45, 187-195.
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Pyrimethamine and WR99210 exert opposing selection on dihydrofolate reductase from Plasmodium vivax
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For a recent critical review of the serious problem of controlling pyrimethamine-resistant malaria in areas of the world where it is endemic, such as sub-Saharan Africa, see the following. Sibley, C. H.; Hyde, J. E.; Sims, P. F. G.; Plowe, C. V.; Kublin, J. G.; Mberu, E. K.; Cowman, A. F.; Winstanley, P. A.; Watkins, W. M.; Nzila, A. M. Trends Parasitol. 2001, 17, 582-588.
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Synthesis of diaryl ethers using an easy-to-prepare, air-stable, soluble copper(I) catalyst
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