Search of antitubercular activities in tetrahydroacridines: synthesis and biological evaluation.
A series of 9-substituted tetrahydroacridines were synthesized by nucleophilic substitution of chloro group with different nucleophiles in 9-chlorotetrahydroacridine (2). The latter could be obtained by POCl(3) mediated cyclization of the intermediate enamine, which in turn, was prepared by acid catalyzed condensation of anthranilic acid and cyclohexanone. Most of the compounds on antitubercular evaluation against M. tuberculosis H37 Rv and H37 Ra strains exhibited potent activities with MIC 6.125-0.78 microg/mL comparable to the standard drugs.
Tripathi
R P
RP
Medicinal and Process Chemistry Division, Central Drug Research Institute, Lucknow 226001, India. rpt_56@yahoo.com
Verma
S S
SS
Pandey
Jyoti
J
Agarwal
K C
KC
Chaturvedi
Vinita
V
Manju
Y K
YK
Srivastva
A K
AK
Gaikwad
A
A
Sinha
S
S
D000166:Acridines / Q000138:chemical synthesis* / Q000494:pharmacology*; D000995:Antitubercular Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D008826:Microbial Sensitivity Tests; D009169:Mycobacterium tuberculosis / Q000187:drug effects*; D013329:Structure-Activity Relationship
D000166:Acridines; D000995:Antitubercular Agents