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Introduction of a conformational switching element on a pyrrolidine ring. Synthesis and evaluation of (R*,R*)-(+/-)-methyl 3-acetyl-4-[3- (cyclopentyloxy)-4-methoxyphenyl]-3-methyl-1-pyrrolidinecarboxylate, a potent and selective inhibitor of cAMP-specific phosphodiesterase.

作者信息

Stafford J A, Veal J M, Feldman P L, Valvano N L, Baer P G, Brackeen M F, Brawley E S, Connolly K M, Domanico P L, Han B

机构信息

Glaxo Wellcome Research, Research Triangle Park, North Carolina 27709, USA.

出版信息

J Med Chem. 1995 Dec 22;38(26):4972-5. doi: 10.1021/jm00026a003.

DOI:10.1021/jm00026a003
PMID:8544172
Abstract
摘要

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Design, synthesis, and structure-activity relationship, molecular modeling, and NMR studies of a series of phenyl alkyl ketones as highly potent and selective phosphodiesterase-4 inhibitors.一系列苯基烷基酮作为高效且选择性磷酸二酯酶-4抑制剂的设计、合成、构效关系、分子建模及核磁共振研究
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