Design & synthesis of hybrid pharmacophore of β-lactam, 1,8-naphthyridine, and secondary amines; Discover their in vitro antimicrobial, anticancer properties & DFT and ADMET prediction studies.

Autor: Pandya, Keyur M., Battula, Satyanarayana, Kumar, K. A. Aravinda, Patel, Rajesh J., Patel, Navin B.
Zdroj: Medicinal Chemistry Research; Jun2023, Vol. 32 Issue 6, p1098-1108, 11p
Abstrakt: An efficient synthetic strategy was developed for the synthesis of hybrid pharmacophores; encompass the merging of β-lactams, 1,8-naphthyridine and secondary amines/pyridines. With a simple unified synthetic protocol, we prepared a series of substituted 3-chloro-1-((3-(2-(trifluoromethyl)phenyl)-1,8-naphthyridin-2-yl)amino)azetidin-2-one compounds (8a–8j) and evaluated for their antimicrobial, and anticancer activities (against MDA-MB-231 cell line). Notably, compounds 8d, 8g, and 8j were identified as potent anticancer molecules and comparable to Cisplatin. Compounds 8d and 8g were found to have promising antitubercular efficacy even greater than the standards Streptomycin and Ciprofloxacin. Compounds 8a, 8d, 8g, 8i, and 8j also displayed potency against both Gram-positive and Gram-negative bacteria and comparable to Ampicillin & Ciprofloxacin. Further, the biological activities were supported and studied by DFT studies and ADMET predictions. [ABSTRACT FROM AUTHOR]
Databáze: Complementary Index
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