Literature DB >> 21807509

Discovery of novel antitubercular 3a,4-dihydro-3H-indeno[1,2-c]pyrazole-2-carboxamide/carbothioamide analogues.

Mohamed Jawed Ahsan1, Jeyabalan Govinda Samy, Savita Soni, Naresh Jain, Lalit Kumar, Lalit K Sharma, Hemant Yadav, Lokesh Saini, Rajput Gopal Kalyansing, Narendra S Devenda, Ravindra Prasad, Chandra Bhushan Jain.   

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.
Copyright © 2011 Elsevier Ltd. All rights reserved.

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Year:  2011        PMID： 21807509     DOI： 10.1016/j.bmcl.2011.07.035

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


  6 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.  Synthesis, Type II diabetes inhibitory activity, antimicrobial evaluation and docking studies of indeno[1,2-c]pyrazol-4(1H)-ones.

Authors:  Satbir Mor; Suchita Sindhu
Journal:  Med Chem Res       Date:  2019-10-26       Impact factor: 1.965

3.  Synthesis, Characterization and Biological Evaluation of New 3,5-Disubstituted-Pyrazoline Derivatives as Potential Anti-Mycobacterium tuberculosis H37Ra Compounds.

Authors:  Kok Tong Wong; Hasnah Osman; Thaigarajan Parumasivam; Unang Supratman; Mohammad Tasyriq Che Omar; Mohamad Nurul Azmi
Journal:  Molecules       Date:  2021-04-05       Impact factor: 4.411

4.  Synthesis, characterisation, and in vitro anticancer activity of curcumin analogues bearing pyrazole/pyrimidine ring targeting EGFR tyrosine kinase.

Authors:  Mohamed Jawed Ahsan; Habibullah Khalilullah; Sabina Yasmin; Surender Singh Jadav; Jeyabalan Govindasamy
Journal:  Biomed Res Int       Date:  2013-09-09       Impact factor: 3.411

Review 5.  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

6.  Utility of 5-(furan-2-yl)-3-(p-tolyl)-4,5-dihydro-1H-pyrazole-1-carbothioamide in the synthesis of heterocyclic compounds with antimicrobial activity.

Authors:  Abdou O Abdelhamid; Ibrahim E El Sayed; Yasser H Zaki; Ahmed M Hussein; Mangoud M Mangoud; Mona A Hosny
Journal:  BMC Chem       Date:  2019-04-01
  6 in total

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