Zobrazeno 1 - 10
of 24
pro vyhledávání: '"Achyutharao Sidduri"'
Publikováno v:
ACS Medicinal Chemistry Letters. 14:176-182
Publikováno v:
Synthesis. 46:430-444
Discovery, optimization, and early development of drug candidates are very challenging and require a versatile synthetic chemistry toolbox. Organozinc chemistry is a powerful methodology for carbon–carbon bond formation which tolerates several func
Autor:
Nadine Tare, Gerry Kaplan, Aruna Railkar, Anjula Pamidimukkala, Karl Frank, Gary Cavallo, Duk Soon Choi, Louise Gerber, Louis M. Renzetti, Jianping Lou, Jefferson Wright Tilley, Achyutharao Sidduri
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 23:1036-1040
From a series of N-acyl 4-(3-pyridonyl)phenylalanine derivatives of 4, the trifluoromethyl derivative 28 was identified as a potent, dual acting alpha4 integrin antagonist with activity in primate models of allergic asthma. Investigation of a series
Autor:
Duk Soon Choi, Louise Gerber, Jianping Lou, Louis M. Renzetti, Karl Frank, Achyutharao Sidduri, Aruna Railkar, Anjula Pamidimukkala, Gary Cavallo, Jefferson Wright Tilley, Nadine Tare
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 23:1026-1031
N-Acyl 4-(5-pyrimidine-2,4-dionyl)phenylalanine derivatives of type 4 were designed to replace the 2,6-dichlorobenzoylamine portion of compound 1 in order to identify novel compounds with improved potency against α4-integrins. Several derivatives we
Autor:
Yonglin Ren, Ryan Craig Schoenfeld, Adrian J. Fretland, Maria E. Fuentes, Kung-Ching Chang, Yimin Qian, Rachid Hamid, Yun Chen, Achyutharao Sidduri, Matthew Michael Hamilton, Christopher S. Stevenson, Gabriel Stephen Deems, Lin Zhang, Terry Truitt, Dramane Ibrahim Laine, Arjun Narayanan, Ruoqi Peng, David C. Budd, Matthew C. Lucas, Rama K. Kondru, Ruben Alvarez Sanchez
Publikováno v:
Journal of Medicinal Chemistry. 55:7920-7939
Lysophosphatidic acid is a class of bioactive phospholipid that mediates most of its biological effects through LPA receptors, of which six isoforms have been identified. The recent results from LPA1 knockout mice suggested that blocking LPA1 signali
Publikováno v:
Synthetic Communications. 40:3691-3698
The synthesis of various aryl methyl sulfides has been achieved by treatment of nitroarenes with a combination of (methylthio)trimethylsilane and cesium carbonate in dimethylsulfoxide. This reaction gives access to aryl methyl sulfide derivatives in
Autor:
Ramakanth Sarabu, Jianping Lou, Achyutharao Sidduri, David J Moore, Jagdish Kumar Racha, Joseph Grimsby, Wendy Lea Corbett, Cheryl Spence, Robert Francis Kester, Linda Marcus, Mark T. Dvorozniak, Joseph F. Grippo
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:5673-5676
The phenylacetamide 1 represents the archtypical glucokinase activator (GKA) in which only the R -isomer is active. In order to probe whether the chiral center could be replaced, we prepared a series of olefins 2 and show in the present work that the
Autor:
Tina Molinaro, Robert Alan Goodnow, Louis M. Renzetti, Alexandra Hicks, Satish Choudhry, Xin Wei, Gesine J. Hermann, Qi Qiao, Anjula Pamidimukkala, A. Robert Catala, Maureen Hargaden, Jian Ping Lou, Nadine Tare, John O’Neil, Ueli Gubler, Karen Pozzani, David J Moore, Jennifer Santiago, Ruben Marcano, Paul Gillespie, Rachid Hamid, Noal Cohen, Hyesun Oh, Lisa C. F. Chao, Laura Singer, Jefferson Wright Tilley, Romyr Dominique, Grazyna Kurylko, Ying L. Li, Radhika Venkat, Achyutharao Sidduri, Matthew Blake Wright, Ann F. Hoffman, Shahid Tannu, Gary Cavallo, Nader Fotouhi, Thomas Egan, Martin Lamb, Jessica D. Ventre, Agnieszka Kowalczyk, D Lavelle, Helena Mancebo
Publikováno v:
Journal of Medicinal Chemistry. 53:3502-3516
The inhibition of LTB(4) binding to and activation of G-protein-coupled receptors BLT1 and BLT2 is the premise of a treatment for several inflammatory diseases. In a lead optimization effort starting with the leukotriene B(4) (LTB(4)) receptor antago
Autor:
Jin-Jun Liu, Christophe Michoud, Feng Chi, Yang Wen, Qing Xiang, Nam T. Le, Shaoqing Chen, Nicole Jackson, Jian Ping Lou, Li Chen, Chunlin Zhao, Achyutharao Sidduri, Louis Portland, Lyubomir T. Vassilev, Fred Konzelmann, Yingsi Chen, Christian Tovar
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:2134-2138
A novel series of quinolinyl-methylene-thiazolinones has been identified as potent and selective cyclin-dependent kinase 1 (CDK1) inhibitors. Their synthesis and structure activity relationships (SAR) are described. Representative compounds from this
Publikováno v:
Current Topics in Medicinal Chemistry. 4:1509-1523
Starting with a cyclic peptide of moderate potency as a VLA-4 antagonist, highly potent and conformationally defined cyclic peptides were developed incorporating a constrained tyrosine and an achiral Asp-Pro spacer. N-Acyl phenylalanine derivatives w