Design, synthesis and biological evaluation of pyrrolo-pyridine derivatives as HIV-1 integrase inhibitors / 国际药学研究杂志
Journal of International Pharmaceutical Research
;
(6): 940-946, 2016.
Article
in Chinese
| WPRIM
| ID: wpr-845484
ABSTRACT
Objective To design and synthesze novel pyrrolopyridine as integrase inhibitors. Method The launched anti-HIV drug raltegravir was selected as template compounds. According to the concept of bioisosterism and molecular docking, a series of pyrrolopyridine compounds (6a-6t) were designed, synthesized and their anti-integrase 3’-processing activity were analyzed. Results The designed compounds were successfully synthesized and the structures of these compounds were confirmed by 1H NMR, 13C NMR and ESI-HRMS. The anti-IN 3’-P activity of these compounds were also measured. The binding mode and docking energy of representative compounds were analyzed. Conclusion The structure-activity relationships of these compounds were also analyzed by the results of docking. These results lay the foundation for the further optimization of these compounds.
Full text:
Available
Index:
WPRIM (Western Pacific)
Language:
Chinese
Journal:
Journal of International Pharmaceutical Research
Year:
2016
Type:
Article
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