Synthesis, antimicrobial and ergosterol biosynthesis inhibition activity of clubbed 1,1′-biphenyl-pyrazole derivatives

Abstract

Microbial infections remain a grave threat to global health security due to an increase in antibiotic resistance. The ongoing coronavirus pandemic has increased the risk of microbial and fungal infections....

Synthesis of pyrazolo-azepinone derivatives via Morita–Baylis–Hillman chemistry as potent antimicrobial agents

“…Pyrazole containing heterocyclic compounds are considered to be of great significance because they represent an interesting template for medicinal chemistry. 1 The impact of pyrazole containing compounds is evident from the fact that this pharmacophore is represented by several commercially available drugs such as sildenafil, zometapin, celebrex and rimonabant that are among the best selling drugs, although a few have been retrieved from the market owing to side effects. 2 Fig.…”

Synthesis, Antifungal Ergosterol Inhibition, Antibiofilm Activities, and Molecular Docking on β-Tubulin and Sterol 14-Alpha Demethylase along with DFT-Based Quantum Mechanical Calculation of Pyrazole Containing Fused Pyridine–Pyrimidine Derivatives

“…The pyridine and pyrimidine scaffolds clubbed with the pyrazole showed potential antimicrobial activities. The pyrazole ring-containing compounds showed antifungal activity via ergosterol biosynthesis inhibition and biofilm inhibition. The structural modification of the ciprofloxacin to 7-phenylpyrido­[2,3- d ]­pyrimidine-2,4­(1 H ,3 H )-dione core highlighted in Figure indicates that the pyrido­[2,3- d ]­pyrimidine-2,4­(1 H ,3 H )-dione pharmacophore matches with the quinolin-4­(1 H )-one core of the ciprofloxacin and the phenyl ring at 7-position of the target scaffold matches with the piperazine ring.…”