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Synthesis and Antimicrobial Activity of the Hybrid Molecules between Sulfonamides and Active Antimicrobial Pleuromutilin Derivative
Author(s) -
Chen Liangzhu,
Yang Dexue,
Pan Zhikun,
Lai Lihong,
Liu Jianhua,
Fang Binghu,
Shi Shuning
Publication year - 2015
Publication title -
chemical biology and drug design
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.59
H-Index - 77
eISSN - 1747-0285
pISSN - 1747-0277
DOI - 10.1111/cbdd.12486
Subject(s) - antimicrobial , microbiology and biotechnology , broth microdilution , staphylococcus aureus , minimum inhibitory concentration , chemistry , bacteria , biology , genetics
A series of novel hybrid molecules between sulfonamides and active antimicrobial 14‐o‐(3‐carboxy‐phenylsulfide)‐mutilin were synthesized, and their in vitro antibacterial activities were evaluated by the broth microdilution. Results indicated that these compounds displayed potent antimicrobial activities in vitro against various drug‐susceptible and drug‐resistant Gram‐positive bacteria such as Staphylococci and streptococci , including methicillin‐resistant Staphylococcus aureus , and mycoplasma. In particular, sulfapyridine analog ( 6c ) exhibited more potent inhibitory activity against Gram‐positive bacteria and mycoplasma, including Staphylococcus aureus (MIC = 0.016–0.063 μ g/mL), methicillin‐resistant Staphylococcus aureus (MIC = 0.016 μ g/mL), Streptococcus pneumoniae (MIC = 0.032–0.063 μ g/mL), Mycoplasma gallisepticum (MIC = 0.004 μ g/mL), with respect to other synthesized compounds and reference drugs sulfonamide (MIC = 8–128 μ g/mL) and valnemulin (MIC = 0.004–0.5 μ g/mL). Furthermore, comparison between MIC values of pleuromutilin‐sulfonamide hybrids 6a–f with pleuromutilin parent compound 3 revealed that these modifications at 14 position side chain of the pleuromutilin with benzene sulfonamide could greatly improve the antibacterial activity especially against Gram‐positives.