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NITD-688, a pan-serotype inhibitor of the dengue virus NS4B protein, shows favorable pharmacokinetics and efficacy in preclinical animal models.
Moquin SA, Simon O, Karuna R, Lakshminarayana SB, Yokokawa F, Wang F, Saravanan C, Zhang J, Day CW, Chan K, Wang QY, Lu S, Dong H, Wan KF, Lim SP, Liu W, Seh CC, Chen YL, Xu H, Barkan DT, Kounde CS, Sim WLS, Wang G, Yeo HQ, Zou B, Chan WL, Ding M, Song JG, Li M, Osborne C, Blasco F, Sarko C, Beer D, Bonamy GMC, Sasseville VG, Shi PY, Diagana TT, Yeung BKS, Gu F. Moquin SA, et al. Among authors: diagana tt. Sci Transl Med. 2021 Feb 3;13(579):eabb2181. doi: 10.1126/scitranslmed.abb2181. Sci Transl Med. 2021. PMID: 33536278
Preclinical evaluation of the antifolate QN254, 5-chloro- N'6'-(2,5-dimethoxy-benzyl)-quinazoline-2,4,6-triamine, as an antimalarial drug candidate.
Nzila A, Rottmann M, Chitnumsub P, Kiara SM, Kamchonwongpaisan S, Maneeruttanarungroj C, Taweechai S, Yeung BK, Goh A, Lakshminarayana SB, Zou B, Wong J, Ma NL, Weaver M, Keller TH, Dartois V, Wittlin S, Brun R, Yuthavong Y, Diagana TT. Nzila A, et al. Among authors: diagana tt. Antimicrob Agents Chemother. 2010 Jun;54(6):2603-10. doi: 10.1128/AAC.01526-09. Epub 2010 Mar 29. Antimicrob Agents Chemother. 2010. PMID: 20350951 Free PMC article.
Spirotetrahydro beta-carbolines (spiroindolones): a new class of potent and orally efficacious compounds for the treatment of malaria.
Yeung BK, Zou B, Rottmann M, Lakshminarayana SB, Ang SH, Leong SY, Tan J, Wong J, Keller-Maerki S, Fischli C, Goh A, Schmitt EK, Krastel P, Francotte E, Kuhen K, Plouffe D, Henson K, Wagner T, Winzeler EA, Petersen F, Brun R, Dartois V, Diagana TT, Keller TH. Yeung BK, et al. Among authors: diagana tt. J Med Chem. 2010 Jul 22;53(14):5155-64. doi: 10.1021/jm100410f. J Med Chem. 2010. PMID: 20568778 Free PMC article.
Spiroindolones, a potent compound class for the treatment of malaria.
Rottmann M, McNamara C, Yeung BK, Lee MC, Zou B, Russell B, Seitz P, Plouffe DM, Dharia NV, Tan J, Cohen SB, Spencer KR, González-Páez GE, Lakshminarayana SB, Goh A, Suwanarusk R, Jegla T, Schmitt EK, Beck HP, Brun R, Nosten F, Renia L, Dartois V, Keller TH, Fidock DA, Winzeler EA, Diagana TT. Rottmann M, et al. Among authors: diagana tt. Science. 2010 Sep 3;329(5996):1175-80. doi: 10.1126/science.1193225. Science. 2010. PMID: 20813948 Free PMC article.
Indolcarboxamide is a preclinical candidate for treating multidrug-resistant tuberculosis.
Rao SP, Lakshminarayana SB, Kondreddi RR, Herve M, Camacho LR, Bifani P, Kalapala SK, Jiricek J, Ma NL, Tan BH, Ng SH, Nanjundappa M, Ravindran S, Seah PG, Thayalan P, Lim SH, Lee BH, Goh A, Barnes WS, Chen Z, Gagaring K, Chatterjee AK, Pethe K, Kuhen K, Walker J, Feng G, Babu S, Zhang L, Blasco F, Beer D, Weaver M, Dartois V, Glynne R, Dick T, Smith PW, Diagana TT, Manjunatha UH. Rao SP, et al. Among authors: diagana tt. Sci Transl Med. 2013 Dec 4;5(214):214ra168. doi: 10.1126/scitranslmed.3007355. Sci Transl Med. 2013. PMID: 24307692
Lead optimization of imidazopyrazines: a new class of antimalarial with activity on Plasmodium liver stages.
Zou B, Nagle A, Chatterjee AK, Leong SY, Tan LJ, Sim WL, Mishra P, Guntapalli P, Tully DC, Lakshminarayana SB, Lim CS, Tan YC, Abas SN, Bodenreider C, Kuhen KL, Gagaring K, Borboa R, Chang J, Li C, Hollenbeck T, Tuntland T, Zeeman AM, Kocken CH, McNamara C, Kato N, Winzeler EA, Yeung BK, Diagana TT, Smith PW, Roland J. Zou B, et al. Among authors: diagana tt. ACS Med Chem Lett. 2014 Jul 6;5(8):947-50. doi: 10.1021/ml500244m. eCollection 2014 Aug 14. ACS Med Chem Lett. 2014. PMID: 25147620 Free PMC article.
Direct inhibitors of InhA are active against Mycobacterium tuberculosis.
Manjunatha UH, S Rao SP, Kondreddi RR, Noble CG, Camacho LR, Tan BH, Ng SH, Ng PS, Ma NL, Lakshminarayana SB, Herve M, Barnes SW, Yu W, Kuhen K, Blasco F, Beer D, Walker JR, Tonge PJ, Glynne R, Smith PW, Diagana TT. Manjunatha UH, et al. Among authors: diagana tt. Sci Transl Med. 2015 Jan 7;7(269):269ra3. doi: 10.1126/scitranslmed.3010597. Sci Transl Med. 2015. PMID: 25568071 Free PMC article.
66 results