Indole-fused spirochromenes as potential anti-tubercular agents: design, synthesis and in vitro evaluation
| Autor: | Sridhar Balasubramanian, Vikas Kumar Aamate, Siva Krishna Vagolu, Pamula Chiranjeevi, Dharmarajan Sriram, M. Sarasija, Ashok Dogamanti |
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| Rok vydání: | 2020 |
| Předmět: |
medicine.drug_class
Antitubercular Agents 010402 general chemistry Antimycobacterial 01 natural sciences Catalysis Inorganic Chemistry Mycobacterium tuberculosis Drug Discovery medicine Physical and Theoretical Chemistry Anti tubercular Cytotoxicity Molecular Biology Indole test Strain (chemistry) biology 010405 organic chemistry Chemistry Organic Chemistry General Medicine biology.organism_classification Combinatorial chemistry In vitro 0104 chemical sciences Design synthesis Information Systems |
| Zdroj: | Molecular Diversity. 25:2137-2148 |
| ISSN: | 1573-501X 1381-1991 |
| Popis: | As part of an ongoing effort to develop new anti-tubercular agents, a series of novel indole-fused spirochromene hybrids (7a–l) were efficiently synthesized in excellent yields by the popular ‘Fisher–Indole synthesis’ approach. The structure elucidation of the target compounds was carried out by different spectral techniques including 1H-NMR, 13C-NMR, ESI Mass, and FTIR analysis. Additionally, the proposed structure of 7i was proved by single-crystal X-ray analysis. These compounds (7a–l) were screened for in vitro anti-tubercular activity against Mycobacterium tuberculosis H37Rv (ATCC 27294) strain. The results showed that most of the targets exhibited promising antimycobacterial activity with MICs of 1.56–6.25 μg/mL and weak cytotoxicity (19.93–32.16% at 50 μg/mL). Among them, compound 7l was found to be the most active compound (MIC of 1.56 μg/mL) with a good safety profile (32.16% at 50 μg/mL). |
| Databáze: | OpenAIRE |
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