Synthesis, biological evaluation and computational studies of pyrazole derivatives as Mycobacterium tuberculosis CYP121A1 inhibitors

Abstract

evaluated for binding affinity with Mycobacterium tuberculosis (Mtb) CYP121A1 and antimycobacterial activity against Mtb H37Rv. Antimycobacterial susceptibility was measured using the spot-culture growth inhibition assay (SPOTi): the imidazoles displayed minimum...

Synthesis and pharmacological evaluation of 1,3-diaryl substituted pyrazole based (thio)urea derivatives as potent antimicrobial agents against multi-drug resistant Staphylococcus aureus and Mycobacterium tuberculosis

“…Like pyrazoles, triazoles come under the class of azoles and have received much attention as antibacterial and antitubercular agents. 25–31 Triazoles act as bioisosteres of various functional groups and five-membered heterocycles, leading to compounds with optimal activity. 32…”

“…24 Furthermore, 1,3 diaryl pyrazole based imidazole derivatives C have been identified as Mtb CYP121A inhibitors that have also shown promising antimycobacterial activity. 25 The potential of pyrazole derivatives as antimicrobial agents encouraged us to combine it with other pharmacophoric units that may provide an overall improvement in affinity, efficacy and pharmacokinetic parameters.…”

“…Like pyrazoles, triazoles come under the class of azoles and have received much attention as antibacterial and antitubercular agents. [25][26][27][28][29][30][31] Triazoles act as bioisosteres of various functional groups and five-membered heterocycles, leading to compounds with optimal activity. 32 On the other hand, urea and thiourea functionalities are known for their potential to form multiple stable hydrogen bonds with various residues in the active site of enzymes and receptors.…”

Antioxidant activity, Dielectric and Electrical Properties of N-benzyl-N'-(5-methyl-1H-pyrazol-3-yl) propanimidamide.

“…They are also known to be very active as enzyme inhibitors [19], antitumor agents [20], anticonvulsants [21,22], anti-HCV [23] and they also can play a very interesting role as antioxidant activities [24]. The antioxidant activities has been revealed by in vitro tests for DPPH Radical Scavenging Activity, Hydroxyl Radical Scavenging Activity [25], Hydrogen peroxide scavenging activity [26] and Reducing Power Assay [27] either Ferrous ion chelating ability (FIC).…”