Synthesis and Antibacterial Activity of 3-(2-(5- Amino-1h-Pyrazol-4-Yl) Thiazol-4-Yl)-2h-Chromen2-One and Its Derivatives

Abstract

A simple and convenient method for the preparation of 3-(2-(5-amino-1H-pyrazole-4-yl)thiazol-4-yl)-2H-chromene-2-one and 3-(2-(5-amino-3-methyl-1H-pyrazole-4-yl)thiazol-4-yl)-2H-chromene-2-ones (3a-f and 5a-f) have been prepared in good yields. The compounds have been synthesized from 2-(4-(2-oxo-2H-chromene-3-yl)thiazol-2yl)acetonitrile (1a-f), with DMF-DMA, DMA-DMA and hydrazine hydrochloride in ethanol resulted in the formation of title compounds. In this regard the whole compounds were tested for promising antibacterial activity, characterized by analytical and spectral data.

Coumarin‐containing hybrids and their antibacterial activities

“…The thiazole‐tethered coumarin–pyrazole hybrids 14 (inhibition zone: 10–20 mm at 100 µg/ml) showed potential activity against S. aureus , B. subtilis , E. coli , and Salmonella paratyphoid ( S. paratyphi b ), and the activity of hybrids 14a,b (inhibition zone: 20 mm at 100 µg/ml) was equal to that of ciprofloxacin (inhibition zone: 20 mm at 100 µg/ml) against Gram‐positive S. aureus and B. subtilis . [ 53 ] The majority of hybrids 15 (MIC: > 250 µg/ml) were devoid of activity against E. coli , S. aureus , E. faecalis , Vibrio cholera ( V. cholera ), and Streptococcus pyogenes ( S. pyogenes ), whereas hybrids 15a,b (MIC: 15.67–31.25 µg/ml) were superior to kanamycin (MIC: 31.25 and 62.50 µg/ml) against S. aureus and S. pyogenes . [ 54 ] Moreover, these two hybrids also displayed excellent antimicrobial activity and synergistic effects when used together with kanamycin and amphotericin B.…”