Synthesis, antibacterial and anticancer activity, and docking study of aminoguanidines containing an alkynyl moiety.

ABSTRACT: Two series of aminoguanidines containing an alkynyl moiety were designed, synthesised, and screened for antibacterial and anticancer activities. Generally, the series 3a-3j with a 1,2-diphenylethyne exhibited better antibacterial activity than the other series (6a-6k) holding 1,4-diphenylbuta-1,3-diyne moiety antibacterial activity. Most compounds in series 3a-3j showed potent growth inhibition against the tested bacterial strains, with minimum inhibitory concentration (MIC) values in the range 0.25-8 µg/mL. Compound 3g demonstrated rapid and persistent bactericidal activity at 2 × MIC. The resistance study revealed that resistance of the tested bacteria towards 3g is not easily developed. Molecular docking studies revealed that compounds 3g and

SUBMITTER: Deng X 

PROVIDER: S-EPMC6968633 | biostudies-literature | 2020 Dec

REPOSITORIES: biostudies-literature