In the present report, a novel series of 1-indanone alpha(1)-adrenoceptor antagonists were designed and synthesized based on 3D-pharmacophore model. Their in vitro alpha(1)-adrenoceptor antagonistic assay showed that three compounds (2a, 2m, and 2o) had similar or improved alpha(1)-adrenoceptor antagonistic activities relative to the positive control prazosin. Based on these results, a three-dimensional quantitative structure-activity relationship study was performed using a Self-Organizing Molecular Field Analysis method to provide insight for the future development of alpha(1)-adrenoceptor antagonists.
Rational design, synthesis, biologic evaluation, and structure-activity relationship studies of novel 1-indanone alpha(1)-adrenoceptor antagonists. Publishing Authors By Initials
Rational design, synthesis, biologic evaluation, and structure-activity relationship studies of novel 1-indanone alpha(1)-adrenoceptor antagonists. Journal Published:
PUBLICATION TYPE: Research Support, Non-U.S. Gov
Journal: Chemical biology & drug design
VOLUME: 70
Page Numbers: 461-4
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ISSN: 1747-0277
DAY: 10
MONTH: 10
YEAR: 2007
Rational design, synthesis, biologic evaluation, and structure-activity relationship studies of novel 1-indanone alpha(1)-adrenoceptor antagonists. Information
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LANGUAGE: eng
NlmUniqueID: 101262549
Rational design, synthesis, biologic evaluation, and structure-activity relationship studies of novel 1-indanone alpha(1)-adrenoceptor antagonists. Keywords Mesh Terms:
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Grant and Affiliation Information for Rational design, synthesis, biologic evaluation, and structure-activity relationship studies of novel 1-indanone alpha(1)-adrenoceptor antagonists.
AFFILIATION: Department of Medicinal Chemistry, China Pharmaceutical University, Nanjing, China.
Country: England
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MEDLINETA: Chem Biol Drug Des
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