3-Acetyl coumarins (1) when allowed react with isatin (2) gave corresponding 3-(3′-hydroxy-2′-oxo indolo) acetyl coumarins (3), which on dehydration afforded the corresponding α,β-unsaturated ketones (4). Cyclocondensation of (4) with substituted o-phenylene diamines resulted in novel 3-coumarinyl spiro[indolo-1,5-benzodiazepines] (5). Structures of all the compounds have been established on the basis of their IR, NMR and mass spectral data and have been screened for their antimicrobial activity and antianxiety activity in mice.
An efficient microwave-assisted protocol for the synthesis of fluorinated coumarino sulfonamides 3 was achieved. First the fluoro arylamines were reacted with methyl 2-chlorosulfonyl acetate to afford compounds 2 followed by Knoevenagel condensation with substituted salicylaldehydes to give fluorinated coumarino sulfonamides 3. Comparison of conventional and microwave irradiation showed the later procedure required shorter reaction times, generally gave higher yields and was applicable to a larger set of substrates.
Benzimidazolo benzothiophene derivatives were prepared by liquid phase combinatorial synthesis using soluble polymer support PEG 5000 and 4-fluoro-3-nitrobenzoic acid as starting materials with substituted primary amines. All these synthesized compounds were established by the spectral data and tested for antimicrobial activity against gram positive bacteria, i.e. S. aureus, B. subtilis and gram negative bacteria, E.coli and P.aeruginosa and anti fungal activity against C. albicans. Ampicillin and ciprofloxacin were used as standard for antibacterial activity and cotrimoxazole for anti fungal activity. Compared with standards compounds (1a-h) showed significant activity against bacterial species and 1g showed significant activity against fungal species.
Corresponding Sulfones. -Compound (Id) shows good inhibition against S. aureus and E. coli while (IIa) only displays good activity against E. coli. -(PATIL*, B. S.; KRISHNAMURTHY, G.; NAIK, H. S. B.; LATTHE, P. R.; GHATE, M.; Eur.
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