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Discovery of 4-((2S,4S)-4-Ethoxy-1-((5-methoxy-7-methyl-1H-indol-4-yl)methyl)piperidin-2-yl)benzoic Acid (LNP023), a Factor B Inhibitor Specifically Designed To Be Applicable to Treating a Diverse Array of Complement Mediated Diseases.
Mainolfi N, Ehara T, Karki RG, Anderson K, Mac Sweeney A, Liao SM, Argikar UA, Jendza K, Zhang C, Powers J, Klosowski DW, Crowley M, Kawanami T, Ding J, April M, Forster C, Serrano-Wu M, Capparelli M, Ramqaj R, Solovay C, Cumin F, Smith TM, Ferrara L, Lee W, Long D, Prentiss M, De Erkenez A, Yang L, Liu F, Sellner H, Sirockin F, Valeur E, Erbel P, Ostermeier D, Ramage P, Gerhartz B, Schubart A, Flohr S, Gradoux N, Feifel R, Vogg B, Wiesmann C, Maibaum J, Eder J, Sedrani R, Harrison RA, Mogi M, Jaffee BD, Adams CM. Mainolfi N, et al. Among authors: serrano wu m. J Med Chem. 2020 Jun 11;63(11):5697-5722. doi: 10.1021/acs.jmedchem.9b01870. Epub 2020 Feb 19. J Med Chem. 2020. PMID: 32073845
Discovery of diamide compounds as diacylglycerol acyltransferase 1 (DGAT1) inhibitors.
Nakajima K, April M, Brewer JT, Daniels T, Forster CJ, Gilmore TA, Jain M, Kanter A, Kwak Y, Li J, McQuire L, Serrano-Wu MH, Streeper R, Szklennik P, Thompson J, Wang B. Nakajima K, et al. Among authors: serrano wu mh. Bioorg Med Chem Lett. 2016 Feb 15;26(4):1245-8. doi: 10.1016/j.bmcl.2016.01.025. Epub 2016 Jan 11. Bioorg Med Chem Lett. 2016. PMID: 26804232
Discovery of an Orally Bioavailable Benzimidazole Diacylglycerol Acyltransferase 1 (DGAT1) Inhibitor That Suppresses Body Weight Gain in Diet-Induced Obese Dogs and Postprandial Triglycerides in Humans.
Nakajima K, Chatelain R, Clairmont KB, Commerford R, Coppola GM, Daniels T, Forster CJ, Gilmore TA, Gong Y, Jain M, Kanter A, Kwak Y, Li J, Meyers CD, Neubert AD, Szklennik P, Tedesco V, Thompson J, Truong D, Yang Q, Hubbard BK, Serrano-Wu MH. Nakajima K, et al. Among authors: serrano wu mh. J Med Chem. 2017 Jun 8;60(11):4657-4664. doi: 10.1021/acs.jmedchem.7b00173. Epub 2017 May 24. J Med Chem. 2017. PMID: 28498655 Clinical Trial.
Intestinally Targeted Diacylglycerol Acyltransferase 1 (DGAT1) Inhibitors Robustly Suppress Postprandial Triglycerides.
Serrano-Wu MH, Coppola GM, Gong Y, Neubert AD, Chatelain R, Clairmont KB, Commerford R, Cosker T, Daniels T, Hou Y, Jain M, Juedes M, Li L, Mullarkey T, Rocheford E, Sung MJ, Tyler A, Yang Q, Yoon T, Hubbard BK. Serrano-Wu MH, et al. ACS Med Chem Lett. 2012 Apr 4;3(5):411-5. doi: 10.1021/ml3000512. eCollection 2012 May 10. ACS Med Chem Lett. 2012. PMID: 24900485 Free PMC article.
A new structural alert for benzimidazoles: 2,6-dimethylphenyl substituents increase mutagenic potential and time-dependent CYP3A4 inhibition risk.
Kwak Y, Coppola G, Forster CJ, Gilmore TA, Gong Y, Kanter A, Neubert A, Stroup B, Szklennik P, Glowienke S, Stadelmann P, Bell L, Bickford S, Gangl E, Gunduz M, Jain M, Zhan J, Serrano-Wu MH. Kwak Y, et al. Bioorg Med Chem Lett. 2011 Mar 1;21(5):1422-4. doi: 10.1016/j.bmcl.2011.01.023. Epub 2011 Jan 11. Bioorg Med Chem Lett. 2011. PMID: 21295471
Discovery of heterocyclic replacements for the coumarin core of anti-tubercular FadD32 inhibitors.
Fang C, Lee KK, Nietupski R, Bates RH, Fernandez-Menendez R, Lopez-Roman EM, Guijarro-Lopez L, Yin Y, Peng Z, Gomez JE, Fisher S, Barros-Aguirre D, Hubbard BK, Serrano-Wu MH, Hung DT. Fang C, et al. Among authors: serrano wu mh. Bioorg Med Chem Lett. 2018 Dec 1;28(22):3529-3533. doi: 10.1016/j.bmcl.2018.09.037. Epub 2018 Sep 29. Bioorg Med Chem Lett. 2018. PMID: 30316633 Free PMC article.
HCV NS5A replication complex inhibitors. Part 4. Optimization for genotype 1a replicon inhibitory activity.
St Laurent DR, Serrano-Wu MH, Belema M, Ding M, Fang H, Gao M, Goodrich JT, Krause RG, Lemm JA, Liu M, Lopez OD, Nguyen VN, Nower PT, O'Boyle DR 2nd, Pearce BC, Romine JL, Valera L, Sun JH, Wang YK, Yang F, Yang X, Meanwell NA, Snyder LB. St Laurent DR, et al. J Med Chem. 2014 Mar 13;57(5):1976-94. doi: 10.1021/jm301796k. Epub 2013 Apr 10. J Med Chem. 2014. PMID: 23573957
30 results