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A facile stereoselective synthesis of dispiro-indeno pyrrolidine/pyrrolothiazole–thiochroman hybrids and evaluation of their antimycobacterial, anticancer and AchE inhibitory activities

Authors :
Subbu Perumal
Sundaravel Vivek Kumar
Shanmugam Muthusubramanian
Mohamed Ashraf Ali
Hasnah Osman
Chelliah Bharkavi
Source :
Bioorganic & Medicinal Chemistry. 24:5873-5883
Publication Year :
2016
Publisher :
Elsevier BV, 2016.

Abstract

A facile stereoselective synthesis of novel dispiro indeno pyrrolidine/pyrrolothiazole–thiochroman hybrids has been achieved by 1,3-dipolar cycloaddition of azomethine ylides, generated in situ from ninhydrin and sarcosine/thiaproline, on a series of 3-benzylidenethiochroman-4-ones. The synthesised compounds were screened for their antimycobacterial, anticancer and AchE inhibition activities. Compound 4l (IC50 1.07 μM) has been found to exhibit the most potent antimycobacterial activity compared to cycloserine (12 times), pyrimethamine (37 times) and ethambutol (IC50

Details

ISSN :
09680896
Volume :
24
Database :
OpenAIRE
Journal :
Bioorganic & Medicinal Chemistry
Accession number :
edsair.doi.dedup.....b2586640a1917d068fd7d805ebdf7af0