Synthesis of Some Biologically Active Pyrazole, Thiazolidinone, and Azetidinone Derivatives.

Abstract

Derivatives. -A variety of novel benzopyranylpyrazoles are synthesized from chalcones (I) and converted into thiazolidinone (IX) and azetidinone derivatives (XI). All the compounds obtained are screened for their in vitro antibacterial activity. -(PAWAR, R. B.; MULWAD, V. V.; Chem. Heterocycl. Compd. (N. Y.) 40 (2004) 2, 219-226; Dep. Chem., Inst. Sci., Bombay 400 032, India; Eng.) -M. Schroeter 50-102

3-Substituted-4-hydroxycoumarin as a new scaffold with potent CDK inhibition and promising anticancer effect: Synthesis, molecular modeling and QSAR studies

“…The intermediate chalcone compounds 4a-d were prepared by conventional Claisen-Schmidt condensation reaction of 1 with the previously mentioned aryl aldehydes in the presence of piperidine drops in ethanol [41][42][43] (Scheme 2). The coumarin-pyrazoline hybrids 5-7 were synthesized through 1,4-addition of hydrazine hydrate or phenyl hydrazine to the α,ß unsaturated carbonyl moiety of the chalcones 4a-d, followed by dehydration and rearrangement (Scheme 2).…”

“…The chalcone compounds 4a, 4b, 4c and 4d were prepared according to the reported methods [41][42][43].…”

“…The reaction mixture was cooled and the formed precipitate was filtered off, washed with ethanol and recrystallized from methyl alcohol to give the target compounds 5a [41], 5b, 5c and 5d. …”

Monocyclic β-Lactams: New Structures for New Biological Activities

“…Azetidinone 20 is an exemplificative molecule which contains a hydroxycoumarine moiety. That family of new -lactams was screened in vitro for antibacterial activity against various bacterial strains and resulted moderately active [33]. Compound 21 represents a new congener of -lactam incorporating the 2-aminobenzothiazole and azetidinone moieties in a single molecular framework, it is highly active against S. aureus and E. coli [34].…”

Antibacterial and β‐Lactamase Inhibitory Activity of Monocyclic β‐Lactams

“…For example, Pawar et al . reported compound 126 and its R 1 ‐demethoxy analogue in a primarily synthetic work (Table ) . These compounds, incorporating a promiscuous coumarin scaffold on R 1 , were assayed against a modest set of bacterial strains (Table ).…”