title: Discovery of novel antitubercular 3a,4-dihydro-3H-indeno[1,2-c]pyrazole-2-carboxamide/carbothioamide analogues.
abstract: In the present investigation, a series of 3a,4-dihydro-3H-indeno[1,2-c]pyrazole-2-carboxamide/carbothioamide analogues were synthesized and were evaluated for antitubercular activity by two fold serial dilution technique. All the newly synthesized compounds showed low to high inhibitory activities against Mycobacterium tuberculosis H(37)Rv and INH resistant M. tuberculosis. The compound 3-(4-fluorophenyl)-6,7-dimethoxy-3a,4-dihydro-3H-indeno[1,2-c]pyrazole-2-carbothioamide (4o) was found to be the most promising compound active against M. tuberculosis H(37)Rv and isoniazid resistant M. tuberculosis with minimum inhibitory concentration 3.12 μM and 6.25 μM, respectively.
authors.affiliation: New Drug Discovery Research, Department of Medicinal Chemistry, Alwar Pharmacy College, Alwar, Rajasthan 301 030, India. jawedpharma@gmail.com
authors.forename: Mohamed Jawed
authors.initials: MJ
authors.lastname: Ahsan
authors.forename: Jeyabalan Govinda
authors.initials: JG
authors.lastname: Samy
authors.forename: Savita
authors.initials: S
authors.lastname: Soni
authors.forename: Naresh
authors.initials: N
authors.lastname: Jain
authors.forename: Lalit
authors.initials: L
authors.lastname: Kumar
authors.forename: Lalit K
authors.initials: LK
authors.lastname: Sharma
authors.forename: Hemant
authors.initials: H
authors.lastname: Yadav
authors.forename: Lokesh
authors.initials: L
authors.lastname: Saini
authors.forename: Rajput Gopal
authors.initials: RG
authors.lastname: Kalyansing
authors.forename: Narendra S
authors.initials: NS
authors.lastname: Devenda
authors.forename: Ravindra
authors.initials: R
authors.lastname: Prasad
authors.forename: Chandra Bhushan
authors.initials: CB
authors.lastname: Jain
mesh_terms: D000818:Animals; D000995:Antitubercular Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D002522:Chlorocebus aethiops; D055808:Drug Discovery; D007192:Indenes / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D009169:Mycobacterium tuberculosis / Q000187:drug effects*; D011720:Pyrazoles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D013237:Stereoisomerism; D013329:Structure-Activity Relationship; D013854:Thioamides / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D014709:Vero Cells
chemical_list: C568620:3-(4-fluorophenyl)-6,7-dimethoxy-3a,4-dihydro-3H-indeno(1,2-c)pyrazole-2-carbothioamide; D000995:Antitubercular Agents; D007192:Indenes; D011720:Pyrazoles; D013854:Thioamides