Results in Chemistry (Jan 2022)
Novel (quinolin-8-yl-oxy)-pyrazole/thiophene derivatives: Synthesis, characterization and their pharmacological evaluation
Abstract
Two novel series of pyrazole and thiophene-linked quinoline analogues via amide bond were conveniently synthesized and characterized by IR, NMR, and HRMS analysis. The synthesized compounds were evaluated for their antimicrobial, anti-inflammatory, and anti-leukemic activity. The antimicrobial evaluation of the target compounds clearly showed that compound 11c has better activity compared to other compounds against tested pathogens. The anti-inflammatory assay of the selected compounds showed that 12c with IC50 value 118.73 µg/ml exhibited significant activity than standard drug Aspirin (IC50, 107.75 µg/ml). The compound 12a out of the twelve newly prepared quinoline heterocycles displayed superior antileukemic activity and was comparable with the standard drug against human monocytic leukemia cell lines (THP-1). Representing the two different quinolinyl-pyrazole/thiophene analogues, compounds 11d, 11e, and 12a displayed the remarkable cytotoxicity against THP-1 cell lines with IC50 values 112.46, 105.42, and 98.88 µg/ml respectively.
