Identification of a novel class of quinoline–oxadiazole hybrids as anti-tuberculosis agents
| Autor: | Aarti Anantram, M.K. Ray, Madhav Seervi, Archana Raju, Sadhana Sathaye, Mariam S. Degani, Puneet P. Jain, M.G.R. Rajan |
|---|---|
| Rok vydání: | 2016 |
| Předmět: |
Cell Survival
Clinical Biochemistry Antitubercular Agents Pharmaceutical Science Oxadiazole Nanotechnology Microbial Sensitivity Tests 010402 general chemistry 01 natural sciences Biochemistry Mycobacterium tuberculosis Structure-Activity Relationship Minimum inhibitory concentration chemistry.chemical_compound Drug Discovery Animals Humans Tuberculosis Cytotoxicity Molecular Biology Oxadiazoles biology 010405 organic chemistry Organic Chemistry Quinoline Biological activity Hep G2 Cells Druglikeness biology.organism_classification Combinatorial chemistry Rats 0104 chemical sciences chemistry Microsomes Liver Quinolines Molecular Medicine Bedaquiline |
| Zdroj: | Bioorganic & Medicinal Chemistry Letters. 26:645-649 |
| ISSN: | 0960-894X |
| DOI: | 10.1016/j.bmcl.2015.11.057 |
| Popis: | A series of novel quinoline-oxadiazole hybrid compounds was designed based on stepwise rational modification of the lead molecules reported previously, in order to enhance bioactivity and improve druglikeness. The hybrid compounds synthesized were screened for biological activity against Mycobacterium tuberculosis H37Rv and for cytotoxicity in HepG2 cell line. Several of the hits exhibited good to excellent anti-tuberculosis activity and selectivity, especially compounds 12m, 12o and 12p, showed minimum inhibitory concentration values0.5μM and selectivity index500. The results of this study open up a promising avenue that may lead to the discovery of a new class of anti-tuberculosis agents. |
| Databáze: | OpenAIRE |
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