Structural modifications of quinolone-3-carboxylic acids with anti-HIV activity

Bioorg Med Chem. 2011 Aug 15;19(16):5039-45. doi: 10.1016/j.bmc.2011.06.020.

Qiu-Qin He ¹, Shuang-Xi Gu, Jia Liu, Hai-Qiu Wu, Xuan Zhang, Liu-Meng Yang, Yong-Tang Zheng, Fen-Er Chen

Affiliations

Affiliation

1 Department of Chemistry, Fudan University, Shanghai 200433, PR China.

PMID: 21763149 DOI: 10.1016/j.bmc.2011.06.020

Abstract

A series of new quinolone-3-carboxylic acids featuring a hydroxyl group at C-5 position were synthesized and evaluated for their in vitro activity against HIV in C8166 Cell Culture. All the compounds showed anti-HIV-1 activity with low micromolar to submicromolar EC(50) values. The most active compound 2k exhibited activity against wild-type HIV-1 with an EC(50) value of 0.13 μΜ. Preliminary structure-activity relationship of the newly synthesized Quinolone analogues was also investigated. Further docking study revealed that the anti-HIV activity of these compounds might involve a two-metal chelating mechanism.

Name
Email *

	Sorry, but the email address you supplied was invalid.