Design and synthesis of pyridone inhibitors of non-nucleoside reverse transcriptase期刊界 All Journals 搜尽天下杂志传播学术成果专业期刊搜索期刊信息化学术搜索

Design and synthesis of pyridone inhibitors of non-nucleoside reverse transcriptase

Authors:	Gomez Robert Jolly Samson Williams Theresa Tucker Thomas Tynebor Robert Vacca Joe McGaughey Georgia Lai Ming-Tain Felock Peter Munshi Vandna DeStefano Daniel Touch Sinoeun Miller Mike Yan Youwei Sanchez Rosa Liang Yuexia Paton Brenda Wan Bang-Lin Anthony Neville

Affiliation:	^aDepartment of West Point Discovery Chemistry, Merck Research Labs., 770 Sumneytown Pike, PO Box 4, West Point, PA 19486-0004, United States;^bDepartment of Chemistry Modeling and Informatics, Merck Research Labs., 770 Sumneytown Pike, PO Box 4, West Point, PA 19486-0004, United States;^cDepartment of In Vitro Pharmacology, Merck Research Labs., 770 Sumneytown Pike, PO Box 4, West Point, PA 19486-0004, United States;^dDepartment of ID Antiviral HIV Discovery, Merck Research Labs., 770 Sumneytown Pike, PO Box 4, West Point, PA 19486-0004, United States;^eDepartment of Structural Chemistry, Merck Research Labs., 770 Sumneytown Pike, PO Box 4, West Point, PA 19486-0004, United States;^fDepartment of DMPK Preclinical WP, Merck Research Labs., 770 Sumneytown Pike, PO Box 4, West Point, PA 19486-0004, United States;^gDepartment of Boston Discovery Chemistry, Merck Research Labs., 33 Avenue Louis Pasteur, Boston, MA 02115-5727, United States

Abstract:	Next generation NNRTIs are sought which possess both broad spectrum antiviral activity against key mutant strains and a high genetic barrier to the selection of new mutant viral strains. Pyridones were evaluated as an acyclic conformational constraint to replace the aryl ether core of MK-4965 (1) and the more rigid indazole constraint of MK-6186 (2). The resulting pyridone compounds are potent inhibitors of HIV RT and have antiviral activity in cell culture that is superior to other next generation NNRTI’s.

Keywords:
本文献已被 ScienceDirect PubMed 等数据库收录！

设为首页 | 免责声明 | 关于勤云 | 加入收藏