No abstract

A modest, efficient, and mild synthetic procedure has been developed for the synthesis of novel series of 1,3,4‐oxadiazole containing azaspirocycles derivatives. The reaction of 1,3,4‐oxadiazole derivative with diverse azaspiro compounds under room temperature condition with helps of sodium iodide catalyst and polar aprotic solvent. Numerous compensations of this strategy embrace less time required, yield increment, consumption of all reactants, and mild condition. All synthesized compounds evaluated for in vitro antidiabetic and antibacterial screening. Among them some compounds show significant biological response.

A novel route has been established for the synthesis of novel pyrido [3,4-d]pyridazin-1(2H)-one derivative. Synthesis of intermediate 4-methyl-7-(piperazin-1-yl)pyrido [3,4-d]pyridazin-1(2H)-one carried out in the presence of Pd(PPh 3 ) 2 Cl 2 catalyst. Ten novel derivatives were synthesized, isolated, and characterized by various spectroscopic techniques. All synthesized molecules were screened for in silico parameters and evaluated for α-glucosidase and α-amylase inhibitory assay. Furthermore, all synthesized molecules were screened for anticancer activity against human lung cell line (A549), human melanoma cell line (A375) and breast cancer (MCF-7) cell lines and their cytotoxic effects were compared. Among the compounds, 8i showed higher inhibition than standard acarbose in the antidiabetic assay. In addition, 8 g exhibited more potency than positive control doxorubicin on lung, breast, and melanoma cancer cell lines. A molecular docking study was carried out on 1RPK and 4HJO as Epidermal growth factor receptor (EGFR) proteins.Ashish J. Radia and Jaydeep N. Lalpara contributed equally to this work.