Design, synthesis, and biological evaluations of (E)‐2‐(1‐[2‐mercapto‐4‐methyl‐1‐phenyl‐1H‐imidazol‐5‐yl]ethylidene)hydrazinecarbothioamide derivatives as antimicrobial agents

Abstract

In recent year, the development of new drugs as antibacterial agents is an important resolution to overcome drug‐resistant pathogens. Imidazole derivatives were synthesized using the microwave irradiation method and were characterized using spectral analysis techniques such as proton nuclear magnetic resonance, mass, and Fourier transform infrared spectroscopy. All the analogous were assessed for their in vitro antimicrobial activity and in silico; minimum inhibition concentration values of some conjugates were evaluated against extended spectrum beta‐lactamases, vancomycin‐resistant enterococci, and Methicillin‐resistant Staphylococcus aureus strains from clinical samples. All the analogous were used as ligands in molecular docking and adsorption, distribution, metabolism, and excretion against saDHPS. Furthermore, compounds were also examined for their in vitro antituberculosis and antimalarial activity.

Biannual Account of Anti‐malarial Agents reported in 2021 and 2022: A Comprehensive Coverage

“…[109] Patel and co-workers reported the imidazole derivative (96) against P. falciparum with IC 50 of 0.15 μg/mL with reference to quinine (IC 50 of 0.268 μg/mL). [110] Further, it has been also investigated for its potential against S. aureus, E. coli and M. tuberculosis along with the additional in silico molecular docking and ADMET studies.…”

“…Sousa and co‐workers reported pyrido[1,2‐ a ]benzimidazole ( 95 ) acting on the trophozoites of P. falciparum with IC 50 of 60.8 nM ( Pf 3D7) and 58.8 nM ( Pf W2) along with its exhaustive in vitro and in vivo profile claiming it as the suitable drug candidate for malaria [109] . Patel and co‐workers reported the imidazole derivative ( 96 ) against P. falciparum with IC 50 of 0.15 μg/mL with reference to quinine (IC 50 of 0.268 μg/mL) [110] . Further, it has been also investigated for its potential against S. aureus , E. coli and M. tuberculosis along with the additional in silico molecular docking and ADMET studies.…”

“…Compounds (103-105) reported strong binding interactions with wild and mutant type PfDHFR-TS in docking analysis and in vitro study shown as the most potent antimalarial property with low toxicity and high selectivity. [118] Next, they also synthesized tetrahydrobenzo [4,5]thieno[2,3- In their experiments, Murwih et al used the Claisen-Schmidt condensation to synthesised the thiophene derivatives (108)(109)(110). Through a ring-closing process involving the previously synthesized chalcones, twelve pyrazolines and eight pyrimidines have been synthesized.…”