Literature DB >> 24077526

Development of 3-phenyl-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine derivatives as novel Mycobacterium tuberculosis pantothenate synthetase inhibitors.

Ganesh Samala1, Parthiban Brindha Devi, Radhika Nallangi, Perumal Yogeeswari, Dharmarajan Sriram.   

Abstract

Forty 3-phenyl-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine derivatives were synthesized from piperidin-4-one by five step synthesis and evaluated for Mycobacterium tuberculosis (MTB) pantothenate synthetase (PS) inhibition study, in vitro activities against MTB, cytotoxicity against RAW 264.7 cell line. Among the compounds, 1-benzoyl-N-(4-nitrophenyl)-3-phenyl-6,7-dihydro-1H-pyrazolo[4,3-c]pyridine-5(4H)-carboxamide (6ac) was found to be the most active compound with IC₅₀ of 21.8 ± 0.8 μM against MTB PS, inhibited MTB with MIC of 26.7 μM and it was non-cytotoxic at 50 μM.
Copyright © 2013 Elsevier Masson SAS. All rights reserved.

Entities:  

Keywords:  Cytotoxicity; Pantothenate synthetase; Tuberculosis

Mesh：

Substances：

Year:  2013        PMID： 24077526     DOI： 10.1016/j.ejmech.2013.08.036

Source DB:  PubMed          Journal:  Eur J Med Chem        ISSN： 0223-5234            Impact factor:   6.514


  8 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, synthesis and anti-mycobacterial evaluation of imidazo[1,2-a]pyridine analogues.

Authors:  Yogesh Mahadu Khetmalis; Surendar Chitti; Anjani Umarani Wunnava; Banoth Karan Kumar; Muthyala Murali Krishna Kumar; Sankaranarayanan Murugesan; Kondapalli Venkata Gowri Chandra Sekhar
Journal:  RSC Med Chem       Date:  2022-01-03

3.  Salicylanilide diethyl phosphates as potential inhibitors of some mycobacterial enzymes.

Authors:  Martin Krátký; Eva Novotná; Shalini Saxena; Perumal Yogeeswari; Dharmarajan Sriram; Markéta Švarcová; Jarmila Vinšová
Journal:  ScientificWorldJournal       Date:  2014-11-04

4.  Synthesis and evaluation of antimicrobial, antitubercular and anticancer activities of 2-(1-benzoyl-1H-benzo[d]imidazol-2-ylthio)-N-substituted acetamides.

Authors:  Snehlata Yadav; Siong Meng Lim; Kalavathy Ramasamy; Mani Vasudevan; Syed Adnan Ali Shah; Abhishek Mathur; Balasubramanian Narasimhan
Journal:  Chem Cent J       Date:  2018-05-26       Impact factor: 4.215

Review 5.  Vitamin in the Crosshairs: Targeting Pantothenate and Coenzyme A Biosynthesis for New Antituberculosis Agents.

Authors:  Hailey S Butman; Timothy J Kotzé; Cynthia S Dowd; Erick Strauss
Journal:  Front Cell Infect Microbiol       Date:  2020-12-15       Impact factor: 5.293

Review 6.  Inhibitors of pantothenate synthetase of Mycobacterium tuberculosis - a medicinal chemist perspective.

Authors:  Amaroju Suresh; Singireddi Srinivasarao; Yogesh Mahadu Khetmalis; Shashidhar Nizalapur; Murugesan Sankaranarayanan; Kondapalli Venkata Gowri Chandra Sekhar
Journal:  RSC Adv       Date:  2020-10-07       Impact factor: 4.036

7.  Confirmation of a Protein-Protein Interaction in the Pantothenate Biosynthetic Pathway by Using Sortase-Mediated Labelling.

Authors:  Philip M Morrison; Matthew R Balmforth; Samuel W Ness; Daniel J Williamson; Michael D Rugen; W Bruce Turnbull; Michael E Webb
Journal:  Chembiochem       Date:  2016-03-01       Impact factor: 3.164

8.  Alanine mutation of the catalytic sites of Pantothenate Synthetase causes distinct conformational changes in the ATP binding region.

Authors:  Bharati Pandey; Sonam Grover; Sukriti Goyal; Anchala Kumari; Aditi Singh; Salma Jamal; Jagdeep Kaur; Abhinav Grover
Journal:  Sci Rep       Date:  2018-01-17       Impact factor: 4.379
  8 in total

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