Literature DB >> 24074842

Studies on substituted benzo[h]quinazolines, benzo[g]indazoles, pyrazoles, 2,6-diarylpyridines as anti-tubercular agents.

Hardesh K Maurya1, Ruby Verma, Saba Alam, Shweta Pandey, Vinay Pathak, Sandeep Sharma, Kishore K Srivastava, Arvind S Negi, Atul Gupta.   

Abstract

Various substituted 5,6-dihydro-8-methoxybenzo[h]quinazolin-2-amine, 1-(3-(4-alkoxyphenyl)-7-methoxy-3,3a,4,5-tetrahydro-2H benzo[g]indazol-2-yl)ethanone, pyrazole and 2,6-diarylpyridine derivatives have been synthesized in good yields by an efficient methodology. The synthesized compounds (4-23) were evaluated for their in vitro anti-tubercular activity against Mycobacterium tuberculosis H37Rv strain. Compounds 6a, 6c, 8a, 19a and 19e exhibited significant anti-tubercular activity at MIC values 50, 100, 50, 25 and 100μM concentration. In vitro cytotoxicity data using THP-1 cells indicated that most active compound 19a is safe as its MIC value is much lower than the cytotoxic value.
Copyright © 2013 Elsevier Ltd. All rights reserved.

Entities:  

Keywords:  AFRWBGJRWRHQOV-UHFFFAOYSA-N; AJTJGWQHYALTSC-UHFFFAOYSA-N; AKKATVMDHBEASX-UHFFFAOYSA-N; AYZGFAJCOVMXLA-UHFFFAOYSA-N; Antitubercular; CFOCPVQZZLPMIO-UHFFFAOYSA-N; CMWJZWOGUWCFQV-UHFFFAOYSA-N; CTEHHBOBZOCAIT-UHFFFAOYSA-N; CTODEFQZHRGULH-UHFFFAOYSA-N; DBXRLXVTWNUHCR-UHFFFAOYSA-N; DSCMLTAZYFVUPH-UHFFFAOYSA-N; DSLIJABHAVBSDV-UHFFFAOYSA-N; DWRUNZAIXLCFIP-UHFFFAOYSA-N; DXBULVYHTICWKT-UHFFFAOYSA-N; DXPKJYJXQICXLT-UHFFFAOYSA-N; Diarylpyridine; FIGVJXMTQDHJMQ-UHFFFAOYSA-N; GYXWNSDLDXGMGU-UHFFFAOYSA-N; HJBWBXRSRQEPRF-UHFFFAOYSA-N; ICSNLGPSRYBMBD-UHFFFAOYSA-N; IEVUNGKXTAPNJR-UHFFFAOYSA-N; ITENFASQOQYRFM-UHFFFAOYSA-N; Indazole; JADFRCNEVYMOAL-UHFFFAOYSA-N; KGHNKNWLMDRAQN-UHFFFAOYSA-N; KXDAEFPNCMNJSK-UHFFFAOYSA-N; LFUDVFOVNMIIIB-UHFFFAOYSA-N; LONGYNYRAPHNDS-UHFFFAOYSA-N; LOQHWUSEIHJYSE-UHFFFAOYSA-N; MHOUKRXEYUPHQG-UHFFFAOYSA-N; MKOXPFXGJVHBRH-UHFFFAOYSA-N; MMVNARZZQWUGQI-UHFFFAOYSA-N; MZCGMLMIRVVUSZ-UHFFFAOYSA-N; MZWNQLWLROXGST-UHFFFAOYSA-N; NFJFJJLADCFCHO-UHFFFAOYSA-N; NKPNESPVSMHQPA-ZRDIBKRKSA-N; NQRYJNQNLNOLGT-UHFFFAOYSA-N; NXWRCPFWNLSYMG-UHFFFAOYSA-N; PAEYRUAPLGXYIJ-UHFFFAOYSA-N; PLGIFHJDPLCSPL-UHFFFAOYSA-N; POMGSLQHWNDZAP-UHFFFAOYSA-N; Pyrazole; QLIZWGWIQMJGMB-UHFFFAOYSA-N; QXQPWPCSFNZDEU-JLHYYAGUSA-N; Quinazoline; RLGJGDBTBWUXKU-UHFFFAOYSA-N; RMGFLMXDCGQKPS-UHFFFAOYSA-N; STGYTXNBWMZKBA-UHFFFAOYSA-N; UBABLIWJMXJJNH-UHFFFAOYSA-N; UPFBAUZYKBLCEO-ZRDIBKRKSA-N; VGLWVBWXBZWXJE-WUKNDPDISA-N; VMNKGGRIISDZAU-UHFFFAOYSA-N; VOISDZHTKJQPAM-UHFFFAOYSA-N; WDWWEAMPRRKLGH-UHFFFAOYSA-N; WGCBFZZUJQDDSF-UHFFFAOYSA-N; WJNQRYCMQPMUDS-PKNBQFBNSA-N; WNRWEBKEQARBKV-UHFFFAOYSA-N; WQMAANNAZKNUDL-UHFFFAOYSA-N; XBPOBCXHALHJFP-UHFFFAOYSA-N; XPAKBGQUORPCMO-PKNBQFBNSA-N; XRWQAJSVMIKRKF-UHFFFAOYSA-N; YNAVUWVOSKDBBP-UHFFFAOYSA-N; YWQRMQADBLJRKZ-UHFFFAOYSA-N; ZVGCJBIDARLIMB-UHFFFAOYSA-N; ZWKKHRLWUFOSPA-UHFFFAOYSA-N; ZXANSLBVWCBHPP-UHFFFAOYSA-N

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Year:  2013        PMID: 24074842     DOI: 10.1016/j.bmcl.2013.08.101

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  4 in total

Review 1.  Synthesis and Pharmacological Activities of Pyrazole Derivatives: A Review.

Authors:  Khalid Karrouchi; Smaail Radi; Youssef Ramli; Jamal Taoufik; Yahia N Mabkhot; Faiz A Al-Aizari; M'hammed Ansar
Journal:  Molecules       Date:  2018-01-12       Impact factor: 4.411

2.  Design and Synthesis of New 6-Nitro and 6-Amino-3,3a,4,5-Tetrahydro-2H-Benzo[g]indazole Derivatives: Antiproliferative and Antibacterial Activity.

Authors:  Viviana Cuartas; María Del Pilar Crespo; Eva-María Priego; Leentje Persoons; Dirk Daelemans; María-José Camarasa; Braulio Insuasty; María-Jesús Pérez-Pérez
Journal:  Molecules       Date:  2019-11-21       Impact factor: 4.411

Review 3.  Current status of pyrazole and its biological activities.

Authors:  Mohd Javed Naim; Ozair Alam; Farah Nawaz; Md Jahangir Alam; Perwaiz Alam
Journal:  J Pharm Bioallied Sci       Date:  2016 Jan-Mar

4.  NSC 18725, a Pyrazole Derivative Inhibits Growth of Intracellular Mycobacterium tuberculosis by Induction of Autophagy.

Authors:  Garima Arora; Assirbad Behura; Tannu Priya Gosain; Ravi P Shaliwal; Saqib Kidwai; Padam Singh; Shamseer Kulangara Kandi; Rohan Dhiman; Diwan S Rawat; Ramandeep Singh
Journal:  Front Microbiol       Date:  2020-01-28       Impact factor: 5.640

  4 in total

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