SYNTHESIS AND BIOLOGICAL EVALUATION OF NOVEL (2-OXO-3-(ARYLIMINO) INDOLIN-1-YL)-N-ARYL PROPANAMIDES AS ANTI-HUMAN IMMUNODEFICIENCY AGENTS

Biplab Debnath; Ping Wang; Liu-meng Yang; Yong-tang Zheng; Swastika Ganguly

doi:10.22159/ajpcr.2018.v11i12.27288

Authors

Biplab Debnath Department of Pharmaceutical Chemistry, Bharat Technology, Howrah, West Bengal, India.
Ping Wang Key Laboratory of Animal Models and Human Disease Mechanisms of the Chinese Academy of Sciences and Yunnan Province, KIZ-SU Joint Laboratory of Animal Models and Drug Development, Kunming Institute of Zoology, Chinese Academy of Sciences, Kunming, Yunnan 650223, China.
Liu-meng Yang Key Laboratory of Animal Models and Human Disease Mechanisms of the Chinese Academy of Sciences and Yunnan Province, KIZ-SU Joint Laboratory of Animal Models and Drug Development, Kunming Institute of Zoology, Chinese Academy of Sciences, Kunming, Yunnan 650223, China.
Yong-tang Zheng Key Laboratory of Animal Models and Human Disease Mechanisms of the Chinese Academy of Sciences and Yunnan Province, KIZ-SU Joint Laboratory of Animal Models and Drug Development, Kunming Institute of Zoology, Chinese Academy of Sciences, Kunming, Yunnan 650223, China.
Swastika Ganguly Department of Pharmaceutical Sciences and Technology, Birla Institute of Technology, Ranchi, Jharkhand, India.

DOI:

https://doi.org/10.22159/ajpcr.2018.v11i12.27288

Keywords:

Isatin analogs, Synthesis, Human immunodeficiency virus, Biological screening, Absorption, distribution, metabolism and elimination

Abstract

Objective: Acquired immunodeficiency syndrome (AIDS) was first identified in the Western world in 1981. Since then, AIDS has been increasingly wide spreading, its rapid worldwide dissemination brought about by modern mass tourism. Isatin (1 H-indole-2, 3-Dione), an endogenous compound identified in many organisms, shows a wide range of biological activities. In view of the above details, we wish to report the synthesis and evaluation of novel isatin analogs, as promising anti-human immunodeficiency (HIV) agents.

Methods: A series of novel isatin analogs (3a-3p) were synthesized, and their chemical structures were confirmed by nuclear magnetic resonance:1H, 13C, ESI-MS spectral data, and CHNS.

Results: The compounds were evaluated as inhibitors of HIV type-1 in MT-4 cell cultures. Of these sixteen compounds, only 5 compounds showed potent anti-HIV activity.

Conclusion: Evaluation of compound properties in silico showed that they possess significant drug-like characteristics.

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