Zobrazeno 1 - 10
of 62
pro vyhledávání: '"Karnail S. Atwal"'
Autor:
Dezhi Xing, John Lloyd, Karnail S. Atwal, Mei Mann Hsueh, Yolanda Caringal, Ruth R. Wexler, Alexander Kover, Paul Levesque, Ji Jiang, Timothy W. Harper, Mary Lee Conder, Heather Finlay, Michael A. Blanar
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 23:1743-1747
Previously disclosed C6 amido and benzimidazole dihydropyrazolopyrimidines were potent and selective blockers of IKur current. Syntheses and SAR for C6 triazolo and imidazo dihydropyrazolopyrimidines series are described. Trifluoromethylcyclohexyl N(
Autor:
Zheming Ruan, S. M. Seiler, Herbert E. Klei, Jing Zhang, Jeffrey A. Robl, Stephen P. O'connor, Mengxiao Shi, Liang Schweizer, John E. Macor, R. Michael Lawrence, Karnail S. Atwal, William A. Schumacher, Eddie C.-K. Liu, Sharon N. Bisaha, Doree F. Sitkoff, Ying Wang, Chi Li, Thomas E. Steinbacher, Yan Shi, Philip D. Stein, Kevin Kish
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:7516-7521
The design, synthesis and SAR of a novel class of valerolactam-based arylsulfonamides as potent and selective FXa inhibitors is reported. The arylsulfonamide-valerolactam scaffold was derived based on the proposed bioisosterism to the arylcyanoguanid
Autor:
Danshi Li, Karnail S. Atwal, Mary Lee Conder, Lin Yan, John Lloyd, Tonya Jenkins-West, Bhandaru Rao S, Huabin Sun, Tram Hyunh, Hong Shi, Alexander Kover, Paul Levesque, Wayne Vacarro, Heather Finlay, Christine Huang
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:1436-1439
Design and synthesis of pyrazolodihydropyrimidines as KV1.5 blockers led to the discovery of 7d as a potent and selective antagonist. This compound showed atrial selective prolongation of effective refractory period in rabbits and was selected for cl
Autor:
Joseph Yanchunas, Eddie C.-K. Liu, Christine Huang, S. M. Seiler, Yan Shi, Ying Wang, Karnail S. Atwal, Thomas E. Steinbacher, Doree F. Sitkoff, Andrew T. Pudzianowski, William A. Schumacher, Karen S. Hartl, Sharon N. Bisaha, Chi Li, Stephen P. O'connor, Kevin Kish, Mengxiao Shi, Philip D. Stein, Herbert E. Klei, Jing Zhang
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 19:6882-6889
We report the design and synthesis of a novel class of N,N'-disubstituted aroylguanidine-based lactam derivatives as potent and orally active FXa inhibitors. The structure-activity relationships (SAR) investigation led to the discovery of the nicotin
Autor:
Karnail S. Atwal, Michael Nyman, Paul Levesque, Mary Lee Conder, John Lloyd, Heather Finlay, Tonya West
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:2714-2718
The design and synthesis of a series of highly functionalized pyrano-[2,3b]-pyridines is described. These compounds were assayed for their ability to block the IKur channel encoded by the gene hKV1.5 in patch-clamped L-929 cells. Six of the compounds
Autor:
David P. Rotella, Robert Zahler, David J. Augeri, Timur Gungor, Aiying Wang, William S. Slusarchyk, Scott A. Bolton, James C. Sutton, Jeffrey A. Robl, Zulan Pi, Karnail S. Atwal, Ligaya M. Simpkins, Yajun Liu, Chet Kwon, Lawrence G. Hamann, Rex A. Parker, Guohua Zhao, Mark S. Kirby, Zhong Sun, David R. Magnin, Jovita Marcinkeviciene, James G. Robertson
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:6476-6480
The synthesis and structure–activity relationships of novel dipeptidyl peptidase IV inhibitors replacing the classical cyanopyrrolidine P1 group with other small nitrogen heterocycles are described. A unique potency enhancement was achieved with β
Autor:
Wei Han, Patrick Y.S. Lam, Philip D. Stein, John E. Macor, Jing Zhang, Robert Zahler, Eddie C.-K. Liu, Karnail S. Atwal, Yan Shi, Ying Wang, Saleem Ahmad, Lawrence J. Kennedy, Stephen P. O'connor, S. M. Seiler, Jeffrey A. Robl, Zilun Hu, Doree F. Sitkoff
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:5952-5958
The design and synthesis of a novel class of amino(methyl) pyrrolidine-based sulfonamides as potent and selective FXa inhibitors is reported. The amino(methyl) pyrrolidine scaffolds were designed based on the proposed bioisosterism to the piperazine
Autor:
Thomas M. Monticello, Paul G. Sleph, Karnail S. Atwal, Gary J. Grover, Feng-Li Wang, David W. Green, Hossain Monshizadegan
Publikováno v:
American Journal of Physiology-Heart and Circulatory Physiology. 287:H1747-H1755
Mitochondrial F1F0-ATPase normally synthesizes ATP in the heart, but under ischemic conditions this enzyme paradoxically causes ATP hydrolysis. Nonselective inhibitors of this enzyme (aurovertin, oligomycin) inhibit ATP synthesis in normal tissue but
Autor:
Gary J. Grover, Francis N. Ferrara, Karnail S. Atwal, Paulina Wang, Paul G. Sleph, Sarah C. Traeger, David W. Green, Hossain Monshizadegan, W. Lynn Rogers
Publikováno v:
Journal of Medicinal Chemistry. 47:1081-1084
In this paper we show that 4-aryl-CH2-imidazole-substituted benzopyran compounds with 3S,4R-stereochemistry are cardioprotective by inhibiting the F1F0 mitochondrial ATP hydrolase. Compounds (e.g., 13) with 3R,4S-stereochemistry act as mitochondrial
Autor:
Saleem Ahmad, Charles R. Dorso, Gamini Chandrasena, Karnail S. Atwal, Wen Liu, Donald W. Combs, Bang-Chi Chen, Khehyong Ngu, David S. Weinstein, Mark S. Kirby, Shung C. Wu
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 14:177-180
Inhibition of the sodium hydrogen exchanger isoform-1 (NHE-1) has been shown to limit damage to the myocardium under ischemic conditions in animals. While most known NHE-1 inhibitors are acylguanidines, this report describes the design and synthesis