Title : ( Design, synthesis, and structure–activity relationship study of 5-amido-1-(2,4-dinitrophenyl)-1H-4- pyrazolecarbonitrils as DD-carboxypeptidase/ penicillin-binding protein inhibitors with Gram-positive antibacterial activity )
Authors: Hamid Sadeghian , Ali Sadeghian , Mehdi Pordel , Mohammad Rahimizadeh , , , Mehdi Bakavoli ,
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Abstract
In this study, we report the design, synthesis, and structure–activity relationships of a series of 5-amido-1-(2,4-dinitrophenyl)-1H-4-pyrazolecarbonitriles as DD-carboxypeptidase/penicillin-binding protein (PBP) inhibitors with Grampositive antibacterial activity. Our results show that the compounds with larger, more polarizable, and electron-rich substituted benzamide moieties such as paradimethyaminobenzamide (3j) and para-methoxybenzamide (3i) exhibit better antibacterial activity against methicillin-susceptible Staphylococcus aureus and methicillin-resistant Staphylococcus aureus with minimum inhibition concentration (MIC) values of 3.8 and 15.3 lM for both of them. These results are in accordance with estimated inhibition constants (Ki) that are obtained from docking with PBP2 and PBP4 of Staphylococcus aureus.
Keywords
, Staphylococcus aureus Docking MIC Multiple alignment b, Lactamase
@article{paperid:1016425,
author = {Hamid Sadeghian and Ali Sadeghian and Pordel, Mehdi and Rahimizadeh, Mohammad and , and , and Bakavoli, Mehdi},
title = {Design, synthesis, and structure–activity relationship study of 5-amido-1-(2,4-dinitrophenyl)-1H-4- pyrazolecarbonitrils as DD-carboxypeptidase/ penicillin-binding protein inhibitors with Gram-positive antibacterial activity},
journal = {Medicinal Chemistry Research},
year = {2010},
volume = {19},
number = {2},
month = {February},
issn = {1054-2523},
pages = {103--119},
numpages = {16},
keywords = {Staphylococcus aureus Docking MIC Multiple alignment
b-Lactamase},
}
%0 Journal Article
%T Design, synthesis, and structure–activity relationship study of 5-amido-1-(2,4-dinitrophenyl)-1H-4- pyrazolecarbonitrils as DD-carboxypeptidase/ penicillin-binding protein inhibitors with Gram-positive antibacterial activity
%A Hamid Sadeghian
%A Ali Sadeghian
%A Pordel, Mehdi
%A Rahimizadeh, Mohammad
%A ,
%A ,
%A Bakavoli, Mehdi
%J Medicinal Chemistry Research
%@ 1054-2523
%D 2010
