New thiazolyl-coumarin hybrids: Design, synthesis, characterization, X-ray crystal structure, antibacterial and antiviral evaluation

An Overview of Coumarin as a Versatile and Readily Accessible Scaffold with Broad-Ranging Biological Activities

“…For these reasons, a constant effort in the development of new drugs for the treatment of this disease is of greatest importance. In 2019 Osman and co-workers combined two bioactive moieties into a single molecule in order to obtain new bioactive compounds with antibacterial and antiviral effects [125]. In particular, based on a previous study of the same research team, in which coumarin scaffolds and thiazole moiety were combined leading to compounds endowed with both antibacterial and antiviral activities, the potentiality of this combination was further explored [126], [127].…”

Coumarin‐containing hybrids and their antibacterial activities

“…The coumarin–thiazole hybrids 24 (MIC: 73–434 µM) and their derivatives 25 (MIC: 49–316 µM) were sensitive to Gram‐positive bacteria ( Streptococcus pneumoniae [ S. pneumoniae ] and S. aureus ) and Gram‐negative bacteria ( E. coli , Enterobacter aerogenes [ E. aerogenes ], and Salmonella typhi [ S. typhi ]), and the SAR revealed that phenyl ring at R 2 position was more favorable than alkyl groups for hybrids 24 , whereas alkyl groups were more preferable for hybrids 25 . [ 70 ] Three hybrids, 24a,b (MIC: 73–79 µM) and 25a (MIC: 49–98 µM), were comparable to or better than the references kanamycin (MIC: 129 µM), streptomycin (MIC: 54–107 µM), and vancomycin (MIC: 22–173 µM) against all tested pathogens, indicating that these three hybrids could be useful starting points in drug development to combat various types of bacterial infections.…”

Crystal structure of ethyl 2,2-difluoro-2-(7-methoxy-2-oxo-2H-chromen-3-yl)acetate, C14H12F2O5

“…The great interest about these compounds is due to their biological activities against different pathologies, which motivate the development of several drugs that are mainly antithrombotics, such as warfarin and acenocoumarol. Based on this findings, these compounds are also used for preliminary studies of antibacterials [4], antivirals [5], antifungals [6]. Molecules containing fluorine atom(s) regularly exhibit beneficial effects in pharmaceuticals.…”