TY - JOUR
T1 - Antimycobacterial activity
T2 - A facile three-component [3+2]-cycloaddition for the regioselective synthesis of highly functionalised dispiropyrrolidines
AU - Wei, Ang Chee
AU - Ali, Mohamed Ashraf
AU - Yoon, Yeong Keng
AU - Ismail, Rusli
AU - Choon, Tan Soo
AU - Kumar, Raju Suresh
AU - Arumugam, Natarajan
AU - Almansour, Abdulrahman I.
AU - Osman, Hasnah
N1 - Funding Information:
The authors wish to express their thanks to Pharmacogenetic and Novel Therapeutic Research, Institute for Research in Molecular Medicine, Universiti of Sains Malysia, Pennag and this work were funded through Research Grant No.RUC (1001/PSK/8620012).
Copyright:
Copyright 2013 Elsevier B.V., All rights reserved.
PY - 2012/8/1
Y1 - 2012/8/1
N2 - A series of twelve dispiropyrrolidines were synthesized using [3+2]-cycloaddition reactions. The synthesized compounds were screened for their antimycobacterial activity against M. tuberculosis H37Rv and INH resistant M. tuberculosis strains using agar dilution method, four of them showed good activity with MIC of less than 1 μM. Compound 4′-[5-(4-fluorophenyl)pyridin-3-yl]-1′-methyldispiro[indan-2, 2′ pyrrolidine-3′,2″-indan]-1,3,1″-trione (4b) was found to be the most active with MIC of 0.1215 and 5.121 μM, respectively.
AB - A series of twelve dispiropyrrolidines were synthesized using [3+2]-cycloaddition reactions. The synthesized compounds were screened for their antimycobacterial activity against M. tuberculosis H37Rv and INH resistant M. tuberculosis strains using agar dilution method, four of them showed good activity with MIC of less than 1 μM. Compound 4′-[5-(4-fluorophenyl)pyridin-3-yl]-1′-methyldispiro[indan-2, 2′ pyrrolidine-3′,2″-indan]-1,3,1″-trione (4b) was found to be the most active with MIC of 0.1215 and 5.121 μM, respectively.
KW - Antimycobacterial activity
KW - Azomethineylide
KW - Dispiropyrrolidines
KW - Indanone
KW - Intermolecular 1,3-dipolar cycloaddition
UR - http://www.scopus.com/inward/record.url?scp=84863980673&partnerID=8YFLogxK
U2 - 10.1016/j.bmcl.2012.06.047
DO - 10.1016/j.bmcl.2012.06.047
M3 - Article
C2 - 22749825
AN - SCOPUS:84863980673
VL - 22
SP - 4930
EP - 4933
JO - Bioorganic and Medicinal Chemistry Letters
JF - Bioorganic and Medicinal Chemistry Letters
SN - 0960-894X
IS - 15
ER -
