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Molecules 2016, 21(9), 1198; doi:10.3390/molecules21091198

Synthesis and Anti-HIV-1 Activity Evaluation for Novel 3a,6a-Dihydro-1H-pyrrolo[3,4-c]pyrazole-4,6-dione Derivatives

1
College of Life Sciences, China Jiliang University, Hangzhou 310018, Zhejiang, China
2
CAS Key Laboratory of Receptor Research, Shanghai Institute of Materia Medica, Shanghai Institutes for Biological Sciences, Chinese Academy of Sciences, Shanghai 201203, China
3
Key Laboratory of Animal Models and Human Disease Mechanisms of Chinese Academy of Sciences and Yunnan Province, Kunming Institute of Zoology, Chinese Academy of Sciences, Kunming 650223, Yunnan, China
*
Authors to whom correspondence should be addressed.
Academic Editor: Diego Muñoz-Torrero
Received: 9 August 2016 / Revised: 30 August 2016 / Accepted: 30 August 2016 / Published: 8 September 2016
(This article belongs to the Section Medicinal Chemistry)
View Full-Text   |   Download PDF [849 KB, uploaded 12 September 2016]   |  

Abstract

The search for new molecular constructs that resemble the critical two-metal binding pharmacophore and the halo-substituted phenyl functionality required for HIV-1 integrase (IN) inhibition represents a vibrant area of research within drug discovery. As reported herein, we have modified our recently disclosed 1-[2-(4-fluorophenyl)ethyl]-pyrrole-2,5-dione scaffolds to design 35 novel compounds with improved biological activities against HIV-1. These new compounds show single-digit micromolar antiviral potencies against HIV-1 and low toxicity. Among of them, compound 9g and 15i had potent anti-HIV-1 activities (EC50 < 5 μM) and excellent therapeutic index (TI, CC50/EC50 > 100). These two compounds have potential as lead compounds for further optimization into clinical anti-HIV-1 agents. View Full-Text
Keywords: anti-HIV-1; integrase; synthesis; SAR; AIDS anti-HIV-1; integrase; synthesis; SAR; AIDS
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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Liu, G.-N.; Luo, R.-H.; Zhou, Y.; Zhang, X.-J.; Li, J.; Yang, L.-M.; Zheng, Y.-T.; Liu, H. Synthesis and Anti-HIV-1 Activity Evaluation for Novel 3a,6a-Dihydro-1H-pyrrolo[3,4-c]pyrazole-4,6-dione Derivatives. Molecules 2016, 21, 1198.

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