Synthesis and pharmacological evaluation of 1,3-diaryl substituted pyrazole based (thio)urea derivatives as potent antimicrobial agents against multi-drug resistant <i>Staphylococcus aureus</i> and <i>Mycobacterium tuberculosis</i>
Ojaswitha Ommi, Mohammad Naiyaz Ahmad, Siva Nageswara Rao Gajula, Parita Wanjari, Shashikanta Sau, Puja Kumari Agnivesh, Santosh K. Sahoo, Nitin Pal Kalia, Rajesh Sonti, Srinivas Nanduri, Arunava Dasgupta, Sidharth Chopra, Venkata Madhavi Yaddanapudi
Abstract
, which include various strains of MRSA and VRSA, and elicited bacteriostatic properties. In an enzymatic assay, 7a effectively inhibited DNA gyrase supercoiling activity at a concentration of 8 times MIC. Further, molecular modeling studies suggested that compound 7a binds at the active site of DNA gyrase with good affinity.
Topics & Concepts
Mycobacterium tuberculosisStaphylococcus aureusAntimicrobialThio-CytotoxicityChemistryMicrobiologyDrugMethicillin-resistant Staphylococcus aureusTuberculosisPyrazoleCombinatorial chemistryPharmacologyIn vitroMedicineStereochemistryBiologyBacteriaBiochemistryGeneticsPathologySynthesis and biological activitySynthesis and Biological EvaluationClick Chemistry and Applications