Design, synthesis and evaluation of 6-(4-((substituted-1H-1,2,3-triazol-4-yl)methyl)piperazin-1-yl)phenanthridine analogues as antimycobacterial agents
| Autor: | Perumal Yogeeswari, Dharmarajan Sriram, Kondapalli Venkata Gowri Chandra Sekhar, Hunsur Nagendra Nagesh, Damarla Harika Rao, Kalaga Mahalakshmi Naidu, Jonnalagadda Padma Sridevi |
|---|---|
| Rok vydání: | 2013 |
| Předmět: |
Antimycobacterial Agents
Cell Survival Stereochemistry Clinical Biochemistry Antitubercular Agents Triazole Pharmaceutical Science Microbial Sensitivity Tests Biochemistry Piperazines Cell Line Mice Structure-Activity Relationship chemistry.chemical_compound Drug Discovery Animals Piperazine Molecular Biology Phenanthridine Organic Chemistry Mycobacterium tuberculosis Triazoles Phenanthridines Design synthesis chemistry Drug Design Mycobacterium tuberculosis H37Rv Click chemistry Molecular Medicine Click Chemistry Selectivity |
| Zdroj: | Bioorganic & Medicinal Chemistry Letters. 23:6805-6810 |
| ISSN: | 0960-894X |
| DOI: | 10.1016/j.bmcl.2013.10.016 |
| Popis: | Focus in this Letter is made to design and synthesize a series of nineteen new 6-(4-((substituted-1H-1,2,3-triazol-4-yl)methyl)piperazin-1-yl)phenanthridine analogues employing click chemistry and evaluated for their anti-tubercular activity against Mycobacterium tuberculosis H37Rv. Among the tested compounds, 7f and 7j exhibited good activity (MIC = 3.125 μg/mL), while 8a displayed excellent activity (MIC = 1.56 μg/mL) against the growth of M. tuberculosis H37Rv. In addition, 7f, 7j and 8a compounds were subjected to cytotoxic studies against mouse macrophage (RAW264.7) cell lines and the selectivity index values are >15 indicating suitability of compounds for further drug development. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
|
Full Text from ScienceDirect