Bioorganic chemistry · 2020
Synthesis and biological evaluation of substituted phenyl azetidine-2-one sulphonyl derivatives as potential antimicrobial and antiviral agents.
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Mandal Milan Kumar, Ghosh Swagatika, Bhat Hans Raj, Naesens Lieve, Singh Udaya Pratap
Аннотация
In the present study, we intend to synthesize a series of novel substituted phenyl azetidine-2-one sulphonyl derivatives. The entire set of derivatives 5 (a-t) were screened for in-vitro antibacterial, and antifungal activity, and among them eleven compounds were further screened for the antiviral activity to predict their efficacy against pathogenic viruses. Interestingly, compound 5d, 5e, 5f, 5h, 5i, and 5j showed similar or better antibacterial activity as compared to ampicillin (standard). Moreover, compounds 5h, 5i, 5j, and 5q showed good inhibitory activity against fungal strains whereas other derivatives had mild or diminished activity in comparison with standard drug clotrimazole. The antimicrobial study indicated that compounds having electron-withdrawing groups showed the highest activity. Interestingly, these tested compounds showed weak antiviral activity against Vaccinia virus, Human Coronavirus (229E), Reovirus-1, Herpes simplex virus, Sindbis virus, Coxsackievirus B4, Yellow Fever virus, and Influenza B virus in HEL cell, Vero cell, and MDCK cell cultures. The findings of the present study might open new avenues to target human disease-causing deadly microbes and viruses.
Предметные рубрики MeSH
AnimalsAnti-Bacterial AgentsAntifungal AgentsAntiviral AgentsAspergillus fumigatusAspergillus nigerAzetidinesCandida albicansCell Line, TumorChlorocebus aethiopsDogsEscherichia coliHumansMadin Darby Canine Kidney CellsMicrobial Sensitivity TestsMolecular StructurePseudomonas aeruginosaStaphylococcus aureusStructure-Activity RelationshipSulfonamidesVero CellsViruses