Back to Search
Start Over
Synthesis and antitubercular evaluation of novel dibenzo[b,d]thiophene tethered imidazo[1,2-a]pyridine-3-carboxamides.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2016 Jul 01; Vol. 26 (13), pp. 3135-3140. Date of Electronic Publication: 2016 Apr 30. - Publication Year :
- 2016
-
Abstract
- A series of novel dibenzo[b,d]thiophene tethered imidazo[1,2-a]pyridine carboxamides 7a-s were designed and synthesized. The required building block, 2-dibenzo[b,d]thiophenyl imidazo[1,2-a]pyridine carboxylic acid (5) was synthesized from commercial dibenzo[b,d]thiophene in good yields following five-step reaction sequence. The desired carboxamides 7a-s was prepared through coupling of acid 5 with various benzyl amines. All the new analogues 7a-s was characterized by their NMR and mass spectral analysis. Among nineteen new compounds 7a-s screened for in vitro antimycobacterial activity against Mycobacterium tuberculosis H37Rv, three compounds 7k (MIC: 0.78μg/mL); 7e and 7n (MIC: 1.56μg/mL) were identified as potent analogues with low cytotoxicity. The results reported here will help global efforts for identification of potential lead antimycobacterial agents.<br /> (Copyright © 2016 Elsevier Ltd. All rights reserved.)
- Subjects :
- Antitubercular Agents chemical synthesis
Antitubercular Agents chemistry
Cell Proliferation drug effects
Dose-Response Relationship, Drug
HEK293 Cells
Humans
Imidazoles chemical synthesis
Imidazoles chemistry
Microbial Sensitivity Tests
Molecular Structure
Pyridines chemical synthesis
Pyridines chemistry
Structure-Activity Relationship
Thiophenes chemical synthesis
Thiophenes chemistry
Antitubercular Agents pharmacology
Imidazoles pharmacology
Mycobacterium tuberculosis drug effects
Pyridines pharmacology
Thiophenes pharmacology
Subjects
Details
- Language :
- English
- ISSN :
- 1464-3405
- Volume :
- 26
- Issue :
- 13
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 27184765
- Full Text :
- https://doi.org/10.1016/j.bmcl.2016.04.088