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Design and synthesis of 2-N-substituted indazolone derivatives as non-carboxylic acid glycogen synthase activators

Autor: Paul Gillespie, Yimin Qian, Tsutomu Sato, Kuo-Sen Huang, Xiaolei Zhang, Weiya Yun, Andrée R. Olivier, Karin Conde-Knape, Stuart Hayden, Qing Xiang, David Robert Bolin

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 23:2936-2940

Glycogen synthase (GS) catalyzes the transfer of glucose residues from UDP-glucose to a glycogen polymer chain, a critical step for glucose storage. Patients with type 2 diabetes normally exhibit low glycogen levels and decreased muscle glucose uptak

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::42f0b4762534c5230f05d9b76ca11a0f
https://doi.org/10.1016/j.bmcl.2013.03.049

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N-substituted sultam carboxylic acids as novel glycogen synthase activators

Autor: Kuo-Sen Huang, Joseph A. Sergi, Stuart Hayden, Yonglin Ren, Weiya Yun, Qing Xiang, Mei Liu, Andrée R. Olivier, Yimin Qian, Karin Conde-Knape, Lin Yi, Xiaolei Zhang, David Robert Bolin, Paul Gillespie

Publikováno v: MedChemComm. 4:833-838

Decreased glycogen synthesis and turnover is a common defect in type 2 diabetic patients. Activating glycogen synthase, the enzyme that catalyses the transfer of glucose from UDP-glucose to a glycogen polymer chain, could be a potential therapeutic t

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::b67c30062c4f82fb0eca49ee3fd28dd4
https://doi.org/10.1039/c3md00053b

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7-Phenyl-pyrido[2,3-d]pyrimidine-2,4-diamines: Novel and highly selective protein tyrosine phosphatase 1B inhibitors

Autor: Kshitij Chhabilbhai Thakkar, Bruce L. Banner, Shiming Li, Nicholas Marcopulos, Joseph A. Sergi, Jolly Bose, Weiya Yun, Catherine Zwingelstein, Adrian Wai-Hing Cheung, Kyungjin Kim, Steven Joseph Berthel, Bingbing Wang, Lucja Orzechowski, Andrée R. Olivier

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 22:7518-7522

High throughput screening of the Roche compound collection led to the identification of diaminopyrroloquinazoline series as a novel class of PTP1B inhibitors. Structural modification of diaminopyrroloquinazoline series resulted in pyrido[2,3-d]pyrimi

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c232213a45381b928aa7b22c684842bc
https://doi.org/10.1016/j.bmcl.2012.10.035

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Discovery and optimization of 2-phenyloxazole derivatives as diacylglycerol acyltransferase-1 inhibitors

Autor: Rebecca Taub, Weiya Yun, Toni Whittard, David Robert Bolin, Yimin Qian, Shiming Li, Paul Gillespie, Sonja Kazmer, Yingsi Chen, Mushtaq Ahmad, Stanley Wertheimer, Karin Conde-Knape

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 21:7205-7209

In a discovery effort to find safe and effective DGAT-1 inhibitors, we have identified 2-phenyloxazole 4-carboxamide 1 as a conformationally constrained analog of a hydrazide hit, which was previously identified from high-throughput screening. Furthe

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::22686f43ba28ecf4b6fd5f817ee02e70
https://doi.org/10.1016/j.bmcl.2011.09.039

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N-Acyl-l-phenylalanine derivatives as potent VLA-4 antagonists that mimic a cyclic peptide conformation

Autor: Li Chen, Weiya Yun, Richard V. Trilles, Karen Rowan, David C. Fry, Jefferson Wright Tilley, Charles H. Cook, Virginia Schwinge, Robert M. Campbell

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 12:137-140

A series of N-benzylpyroglutamyl-L-phenylalanine derivatives bearing carbamoyl substituents in the 3- or 4-positions was prepared and assayed for inhibition of the interaction between VCAM and VLA-4. Potent inhibition was observed in a number of anal

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1e28b1c8519567294c5c8237e485742d
https://doi.org/10.1016/s0960-894x(01)00711-9

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Solid-phase synthesis of N-substituted amidinophenoxy pyridines as factor Xa inhibitors

Autor: Amy Liang, Lan Trinh, Weiya Yun, Raju Mohan, Morrissey Michael M, Brad O. Buckman

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 8:1877-1882

An arylamidine linker has been employed for the solid-phase synthesis of N-substituted amidinoaryloxypyridine analogs 2 via nucleophilic substitution on a fluoropydyl template. Two novel N-substituted amidinoaryloxypyridine derivatives 2a and 2b were

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6bfeb15a075f3a8985898231f11c76db
https://doi.org/10.1016/s0960-894x(98)00333-3

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Heck reaction on solid support: synthesis of indole analogs

Autor: Weiya Yun, Raju Mohan

Publikováno v: Tetrahedron Letters. 37:7189-7192

The intramolecular Heck reaction of polymer bound arylhalides such as 1 affords indole analogs 11 in high yield. The precursor is readily assembled from acid chlorides and allylic bromides and offers an approach to diverse libraries of indole analogs

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::33c024008d25b59959862353853997a1
https://doi.org/10.1016/0040-4039(96)01635-8

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1,2,9,9a-tetrahydrocyclopropa[c]benz[e]indol-4-one (CBI) analogs of CC-1065 and the duocarmycins: synthesis and evaluation

Autor: Weiya Yun, Dale L. Boger, Nianhe Han

Publikováno v: Bioorganic & Medicinal Chemistry. 3:1429-1453

An extensive study of analogs of the potent antitumor antibiotics CC-1065 and the duocarmycins which incorporate the 1,2,9,9 a -tetrahydrocyclopropa[c]benz [e]indol-4-one (CBI) alkylation subunit are detailed. In contrast to early speculation, deep-s

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ffc994f7d9cf54440f92816dde4337ab
https://doi.org/10.1016/0968-0896(95)00130-9

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