1333140-89-8Relevant academic research and scientific papers
Synthesis and biological evaluation of HQCAs with aryl or benzyl substituents on N-1 position as potential HIV-1 integrase inhibitors
He, Qiu-Qin,Zhang, Xuan,Wu, Hai-Qiu,Gu, Shuang-Xi,Ma, Xiao-Dong,Yang, Liu-Meng,Zheng, Yong-Tang,Chen, Fen-Er
, p. 5553 - 5558 (2011/10/19)
A series of new 5-hydroxylquinolone-3-carboxylic acids (HQCAs) with various aryl or benzyl substituents on N-1 position were synthesized and evaluated for their anti-HIV activity in C8166 cell culture. Most of the target compounds displayed activity against wide-type HIV-1 in the low micromolar range in infected C8166 cells. The most active compound 5g exhibited activity against wild-type HIV-1 and HIV-1 mutant virus A17 with an EC50 value of 3.17 and 17.88 μM, respectively. The biological results and the docking study revealed that the substitution pattern on N-1 position of the quinolone core might contribute to physicochemical properties of HQCAs and resulted in great influence on their antiviral potency.
Structural modifications of quinolone-3-carboxylic acids with anti-HIV activity
He, Qiu-Qin,Gu, Shuang-Xi,Liu, Jia,Wu, Hai-Qiu,Zhang, Xuan,Yang, Liu-Meng,Zheng, Yong-Tang,Chen, Fen-Er
, p. 5039 - 5045 (2011/10/03)
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 submi
