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SAR and molecular mechanism study of novel acylhydrazone compounds targeting HIV-1 CA |
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| Authors: | Yinxue Jin Zhiwu Tan Meizi He Baohe Tian Shixing Tang Indira Hewlett Ming Yang |
| Institution: | 1. State Key Laboratory of Natural and Biomimetic Drugs, Peking University, PO Box 261, Beijing 100191, China;2. Center for Biologics Evaluation and Research, Food and Drug Administration, Bethesda, MD 20892, USA |
| Abstract: | We synthesized a series of acylhydrazone compounds bearing naturally occurring amino acids’ side chains as HIV assembly inhibitors. Biological evaluation indicated that the compounds had anti-SIV and capsid assembly inhibitory activities. The structure–activity relationship (SAR) study showed that compounds bearing proper aromatic side chains had potential antiviral activities. The molecular modeling experiments revealed the molecular mechanism that they could bind to CA in the same manner as CAP-1 and occupy two more grooves. |
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