Anti-human immunodeficiency activity of novel 2-arylpyrrolidine analogs
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- 作者：Ashot H. Martirosyan ; Sahak P. Gasparyan…
- 关键词：Pyrrolidinecarbonitriles ; Aminomethylpyrrolidines ; Anti ; HIV ; 1 ; Cytotoxicity activity
- 刊名：Medicinal Chemistry Research
- 出版年：2017
- 出版时间：January 2017
- 年：2017
- 卷：26
- 期：1
- 页码：101-108
- 全文大小：
- 刊物主题：Pharmacology/Toxicology; Biochemistry, general; Cell Biology;
- 出版者：Springer US
- ISSN：1554-8120
- 卷排序：26
文摘
A series of 26 new compounds were synthesized and screened for their anti-human immunodeficiency virus-1 and cytotoxicity activity. Of these, 14 were found to be inhibitors of human immunodeficiency virus replications in primary human lymphocytes with 50 % effective concentration values <20 µM. Moreover, most of the compounds were cytotoxic to human lymphocytes, CEM, and Vero cells. Our structure activity relationship study identified different patterns. Compounds 2g–j and 4 (whose structure is closer to the loviride structure) were very potent. Comparing the activity of the compounds containing the 2-aryl substituents, we observed that compounds with benzyloxyphenyl groups were more potent. Compounds in which the 1-aryl moiety contained methyl group in 4- or 3,5-positions also showed high activity. In the series of compounds containing the nitrile, amine, and amide groups, we observed a decrease in activity with CN > NH2 > C(O)NH2. The difference of activity between the 5-membered and 4-membered rings compounds was not significant. This initial information could be used to design improved anti-human immunodeficiency virus compounds in this class.