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抗高血脂 2 - 取代噻吩并[3,2 - d]嘧啶 - 4(3H)-酮的合成及定量构效关系

Synthesis and quantitative structure-activity relationships of antihyperlipaemic 2-substituted thieno[3,2-d]pyrimidin-4(3H)-ones.

作者信息

Shishoo C J, Jain K S, Rathod I S, Thakkar B J, Brahmbhatt S B, Gandhi T P, Bangaru R, Goyal R K

机构信息

L. M. College of Pharmacy, Ahmedabad, India.

出版信息

Arzneimittelforschung. 1996 Mar;46(3):273-6.

PMID:8901148
Abstract

The synthesis, antihyperlipaemic evaluation and quantitative structure-activity relationships (QSAR) of two series of thieno[3,2-d]pyrimidin-4-one derivatives are reported. While most of the compounds in these series were found to exhibit antihyperlipaemic activity, the QSAR study of these two series indicated a positive influence of only the electronic nature of the 2-substitutents on the biological activity. The lipophilic and the steric parameters did not appear to be significant.

摘要

报道了两个系列噻吩并[3,2 - d]嘧啶 - 4 - 酮衍生物的合成、抗高血脂活性评价及定量构效关系(QSAR)。虽然发现这些系列中的大多数化合物具有抗高血脂活性,但对这两个系列的QSAR研究表明,只有2 - 取代基的电子性质对生物活性有积极影响。亲脂性和空间参数似乎并不显著。

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