Synthesis of Quinolin-2-one Alkaloid Derivatives and Their Inhibitory Activities against HIV-1 Reverse TranscriptaseReportar como inadecuado




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1

National Research Center of Engineering Technology For Utilization of Functional Ingredients From Botanicals, College of Horticulture and Landscape Architecture, Hunan Agricultural University, Changsha 410128, Hunan, China

2

School of Pharmaceutical Sciences, Sun Yat-Sen University, Guangzhou 510006, Guangdong,China

3

Hunan Engineering Research Center of Botanical Extract, Changsha410128, Hunan, China





*

Authors to whom correspondence should be addressed.



Abstract Based on an established common pharmacophore of HIV-1 non-nucleoside reverse transcriptase inhibitors NNTTIs, a series of quinolin-2-one derivatives were synthesized and assayed for their in vitro activities against HIV-1 reverse transcriptase RT for the first time. Some of the tested compounds were active against HIV-1 RT. Compounds 4a2 and 4d2 showed inhibitory activities with IC50 values of 0.21 and 0.15 mM, respectively, with a mode of interaction with RT residues of the allosteric pocket similar to that of efavirenz.

Keywords: quinolin-2-one; alkaloid; synthesis; HIV-1 RT; activity quinolin-2-one; alkaloid; synthesis; HIV-1 RT; activity





Autor: Pi Cheng 1,3,* , Qiong Gu 2, Wei Liu 1, Jian-Feng Zou 1, Yang-Yong Ou 3, Zhong-Yong Luo 3 and Jian-Guo Zeng 1,3,*

Fuente: http://mdpi.com/



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