Design, Synthesis, Docking Study of Pyrazolohydrazinopyrimidin-4-one Derivatives and Their Application as Antimicrobials.

New series of pyrazoles 4a-c and pyrazolopyrimidines 5a-f had been constructed. The newly synthesized compounds were assessed for their antimicrobial activity towards E. coli and P. aeruginosa (gram -ve bacteria), B. subtilis and S. aureus (gram +ve bacteria) and A. flavus and C. albicans (representative of fungi). The pyrazolylpyrimidine-2,4-dione derivative 5b is the most active candidate against B. subtilis (MIC=60 µg/mL) and P. aeruginosa (MIC=45 µg/mL). Regarding antifungal potential, compound 5f was the most effective against A. flavus (MIC=33 µg/mL). Similarly, compound 5c displayed strong antifungal activity towards C. Albicans (MIC=36 µg/mL) in reference to amphotericin B (MIC=60 µg/mL). Finally, the novel compounds had been docked inside dihydropteroate synthase (DHPS) to suggest the binding mode of these compounds.

Synthesis of Chalcones Derivatives and Their Biological Activities: A Review.

Chalcone derivatives are considered valuable species because they possess a ketoethylenic moiety, CO-CH=CH-. Due to the presence of a reactive α,ß-unsaturated carbonyl group, chalcones and their derivatives possess a wide spectrum of antiproliferative, antifungal, antibacterial, antiviral, antileishmanial, and antimalarial pharmacological properties. Recent developments in heterocyclic chemistry have led to the synthesis of chalcone derivatives, which had been biologically investigated toward certain disease targets. The major aspect of this review is to present the most recent synthesis of chalcones bearing N, O, and/or S heterocycles, revealing their biological potential during the past decade (2010-2021). Based on a review of the literature, many chalcone-heterocycle hybrids appear to exhibit promise as future drug candidates owing to their similar or superior activities compared to those of the standards. Thus, this review may prove to be beneficial for the development and design of new potent therapeutic drugs based on previously developed strategies.