Literature DB >> 27686965

Benzimidazole-core as an antimycobacterial agent.

Rangappa S Keri1, Chethana Kolambae Rajappa2, Siddappa A Patil2, Bhari Mallanna Nagaraja2.   

Abstract

Mycobacterium tuberculosis (Mtb) is considered as one of the precarious bacterial infections around the world. Through a projected 8.7 million new tuberculosis (TB) cases and 1.4 million mortalities per annum, this deadly infection resulted insubstantial amount of human deaths than any other single organism bacterial infections. TB is one of India's most threatening human health problems and it accounts for approximately 33% of the global health issues. Subsequently, for TB there is an imperative need for the improvement of existing drug candidates with newer targets and specified mechanism of action. Within the wide spectra of heterocycles, benzimidazole and its substituted analogues were evidenced promising biological efficacies enabling them to perform as new drug or prodrug candidates. Exceptional structural features of this class of heterocycle and versatile biological applications made it a privileged structural backbone in new drug design and discovery. Majorly, 2,5- and 2,6-disubstituted benzimidazole derivatives shown to induce significant antiTB potential. To seek more insights on this unique feature of benzimidazole candidates, there is an urgency to assemble the recent advances in this promising area. This review presents an overview of the recent advancements and focuses on the structural features responsible for unique antiTB applications and compiled published reports on benzimidazole derivatives emphasizing on different approaches employed for their syntheses in order to help medicinal and clinical chemists in designing next generation, yet effective and safer antiTB candidates.
Copyright © 2016 Institute of Pharmacology, Polish Academy of Sciences. Published by Elsevier Urban & Partner Sp. z o.o. All rights reserved.

Entities:  

Keywords:  2,5-/2,6-Disubstituted benzimidazole; AntiTB agents; Medicinal chemistry; Multistep synthesis; Mycobacterium tuberculosis; Tubercle bacillus

Mesh:

Substances:

Year:  2016        PMID: 27686965     DOI: 10.1016/j.pharep.2016.08.002

Source DB:  PubMed          Journal:  Pharmacol Rep        ISSN: 1734-1140            Impact factor:   3.024


  4 in total

1.  Discovery of newer pyrazole derivatives with potential anti-tubercular activity via 3D-QSAR based pharmacophore modelling, virtual screening, molecular docking and molecular dynamics simulation studies.

Authors:  Palmi Modi; Shivani Patel; Mahesh Chhabria
Journal:  Mol Divers       Date:  2022-08-15       Impact factor: 3.364

2.  Novel Antimycobacterial Compounds Suppress NAD Biogenesis by Targeting a Unique Pocket of NaMN Adenylyltransferase.

Authors:  Andrei L Osterman; Irina Rodionova; Xiaoqing Li; Eduard Sergienko; Chen-Ting Ma; Antonino Catanzaro; Mark E Pettigrove; Robert W Reed; Rashmi Gupta; Kyle H Rohde; Konstantin V Korotkov; Leonardo Sorci
Journal:  ACS Chem Biol       Date:  2019-04-17       Impact factor: 5.100

3.  3D QSAR-based design and liquid phase combinatorial synthesis of 1,2-disubstituted benzimidazole-5-carboxylic acid and 3-substituted-5H-benzimidazo[1,2-d][1,4]benzodiazepin-6(7H)-one derivatives as anti-mycobacterial agents.

Authors:  Nikum D Sitwala; Vivek K Vyas; Piyush Gedia; Kinjal Patel; Rania Bouzeyen; Saqib Kidwai; Ramandeep Singh; Manjunath D Ghate
Journal:  Medchemcomm       Date:  2019-03-22       Impact factor: 3.597

4.  Synthesis, density functional theory study and in vitro antimicrobial evaluation of new benzimidazole Mannich bases.

Authors:  Maria Marinescu; Ludmila Otilia Cinteză; George Iuliu Marton; Mariana-Carmen Chifiriuc; Marcela Popa; Ioana Stănculescu; Christina-Marie Zălaru; Cristina-Elena Stavarache
Journal:  BMC Chem       Date:  2020-07-25
  4 in total

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