Literature DB >> 21824772

Synthesis and biological evaluation of some novel N-aryl-1,4-dihydropyridines as potential antitubercular agents.

Amit R Trivedi1, Dipti K Dodiya, Bipin H Dholariya, Vipul B Kataria, Vimal R Bhuva, Viresh H Shah.   

Abstract

1,4-Dihydropyridines are the emerging class of antitubercular agent. Recently, studies have revealed that 1,4-dihydropyridine-3,5-dicarbamoyl derivatives with lipophilic groups have demonstrated excellent antitubercular activity. We have synthesized new N-aryl-1,4-dihydropyridines bearing carbethoxy and acetyl group at C-3 and C-5 of the DHP ring. In addition, 1H-pyrazole ring is substituted at C-4 position. The lowest minimum inhibitory concentration value, 0.02 μg/mL, was found for diethyl 1-(2-chlorophenyl)-1,4-dihydro-2,6-dimethyl-4-(1,3-diphenyl-1H-pyrazol-4-yl)pyridine-3,5-dicarboxylate 4e making it more potent than first line antitubercular drug isoniazid. In addition, this compound exhibited relatively low cytotoxicity.
Copyright © 2011 Elsevier Ltd. All rights reserved.

Entities:  

Mesh:

Substances:

Year:  2011        PMID: 21824772     DOI: 10.1016/j.bmcl.2011.07.068

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


  3 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.  Acridinedione as selective flouride ion chemosensor: a detailed spectroscopic and quantum mechanical investigation.

Authors:  Nafees Iqbal; Syed Abid Ali; Iqra Munir; Saima Khan; Khurshid Ayub; Mariya Al-Rashida; Muhammad Islam; Zahid Shafiq; Ralf Ludwig; Abdul Hameed
Journal:  RSC Adv       Date:  2018-01-09       Impact factor: 4.036

3.  Antimicrobial activity of novel c2-substituted 1,4-dihydropyridine analogues.

Authors:  Petra Olejníková; L'ubomír Svorc; Denisa Olšovská; Anna Panáková; Zuzana Vihonská; Katarína Kovaryová; Stefan Marchalín
Journal:  Sci Pharm       Date:  2014-01-12
  3 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.