New lactam-containing benzenesulfonamides: design, synthesis, and in silico and in vitro studies
RUSSIAN CHEMICAL BULLETIN(2021)
摘要
A virtual set of new lactam-containing derivatives of arylsulfonylglycines 1a–d and 2a–d was designed and analyzed using structure–activity computer models (web-services PASS Online, AntiBac-Pred, and GUSAR Acutetoxicity). The antimicrobial activity against Staphylococcus aureus along with low toxicity was predicted for these derivatives. Compounds 1a–d and 2a–d were synthesized by the reactions of N -trimethylsilyl lactams with 4-substituted [(phenyl)sulfonyl]aminoacetyl chlorides. The structures of new compounds were confirmed by IR spectroscopy, NMR spectroscopy, and elemental analysis data. According to the results of studies in vitro , compounds 1a–d and 2a–d efficiently suppress the growth of S. aureus. Lactam-containing benzenesulfonamides bearing the bromine atom or methyl or nitro group at position 4 manifested the most pronounced activity.
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关键词
N-trialkylsilyl lactams, acyl chlorides, sulfonamides, Staphylococcus aureus, antimicrobial activity, structure–, activity relationship
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