Synthesis and antibacterial activity of dithiolopyrrolone derivatives / 国际药学研究杂志
Journal of International Pharmaceutical Research
;
(6): 840-847, 2019.
Article
in Chinese
| WPRIM
| ID: wpr-845232
ABSTRACT
Objective:
To design and synthesize novel dithiolopyrrolone derivatives with antibacterial activity.Methods:
Fourteen N-aryldithiolopyrrolone derivatives with 6-amino-4H-[1,2]dithiolo[4,3-b]pyrrol-5-one skeleton were synthesized via amidation and nucleophilic substitution reactions. The in vitro antimicrobial activity against Staphy- lococcus aureus was assayed for all of the synthesized fourteen derivatives by the paper disk diffusion method. For select- ed compounds,the minimum inhibition concentration on S. aureus was determined and the inhibitory activity on the Esch- erichia coli RNA polymerase(RNAP)was further evaluated. In addition,a predictive investigation for the action mecha- nism of the most potent compound 2i was performed by the molecular docking study on RNAP. Results and Conclu- sion The structures of the synthesized compounds were confirmed by 1H NMR,13C NMR and ESI-MS. The compound 2i showed a potent antibacterial activity and the molecular docking study revealed the interaction of 2i with the switch re- gion of the bacterial RNA polymerase. Compound 2i might serve as a new lead compound for further optimization into po- tential antibacterial agents.
Full text:
Available
Index:
WPRIM (Western Pacific)
Language:
Chinese
Journal:
Journal of International Pharmaceutical Research
Year:
2019
Type:
Article
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