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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: szklennik p. 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.
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: szklennik p. 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
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. Among authors: szklennik p. 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
1-Pentyl-3-phenylacetylindoles, a new class of cannabimimetic indoles.
Huffman JW, Szklennik PV, Almond A, Bushell K, Selley DE, He H, Cassidy MP, Wiley JL, Martin BR. Huffman JW, et al. Among authors: szklennik pv. Bioorg Med Chem Lett. 2005 Sep 15;15(18):4110-3. doi: 10.1016/j.bmcl.2005.06.008. Bioorg Med Chem Lett. 2005. PMID: 16005223