Facile one pot microwave induced solvent-free synthesis and antifungal, antitubercular screening of spiro [1,5]-benzothiazepin-2,3'[3'H]indol-2[1'H]-ones.
Microwave activation coupled with dry media technique as a green chemistry procedure has been applied to synthesis of a series of some new title compounds. They have been obtained by the reaction of in situ synthesized 1,3-dihydro-3-[2-(phenyl/4-fluorophenyl)-2-oxoethylidene)-indol-2(1H)-one (4a, b) with substituted aminobenzenethiols (5a-d). The key intermediates 4a, b were also prepared in one step by this improved technique by reacting isatin and substituted acetophenones (2a, b). The results obtained under microwave irradiation when compared with that following conventional method demonstrate the versatility of the process. The title compounds 7a-e have also been screened for their antifungal and antitubercular activity, 7a and 7e showing maximum inhibition of growth of Alternaria alternata and Fusarium oxysporium and 7b, c, e revealing significant antitubercular activity.
Dandia
Anshu
A
Department of Chemistry, University of Rajasthan, Jaipur, India. dranshudandia@eth.net
Sati
Meha
M
Arya
Kapil
K
Sharma
Rekha
R
Loupy
André
A
D000935:Antifungal Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D000995:Antitubercular Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D004353:Drug Evaluation, Preclinical / Q000379:methods; D008826:Microbial Sensitivity Tests / Q000379:methods; D013678:Technology, Pharmaceutical / Q000379:methods*; D013841:Thiazepines / Q000138:chemical synthesis* / Q000494:pharmacology
D000935:Antifungal Agents; D000995:Antitubercular Agents; D013841:Thiazepines