Molecular hybridization conceded exceptionally potent quinolinyl-oxadiazole hybrids through phenyl linked thiosemicarbazide antileishmanial scaffolds: In silico validation and SAR studies
The high potential of quinoline containing natural products and their derivatives in medicinal chemistry led us to discover a novel series of compounds 6–23 based on the concept of molecular hybridization. Most of the synthesized analogues exhibited potent leishmanicidal potential. The most potent c...
| Published in: | Bioorganic Chemistry |
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| Main Author: | |
| Format: | Article |
| Language: | English |
| Published: |
Academic Press Inc.
2017
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| Online Access: | https://www.scopus.com/inward/record.uri?eid=2-s2.0-85013078177&doi=10.1016%2fj.bioorg.2017.02.005&partnerID=40&md5=e5c710c4b1205f0ad97509871f6d5cee |
| Summary: | The high potential of quinoline containing natural products and their derivatives in medicinal chemistry led us to discover a novel series of compounds 6–23 based on the concept of molecular hybridization. Most of the synthesized analogues exhibited potent leishmanicidal potential. The most potent compound (23, IC50 = 0.10 ± 0.001 μM) among the series was found ∼70 times more lethal than the standard drug. The current series 6–23 conceded in the development of fourteen (14) extraordinarily active compounds against leishmaniasis. In silico analysis were also performed to probe the mode of action while all the compounds structure were established by NMR and Mass spectral analysis. © 2017 Elsevier Inc. |
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| ISSN: | 452068 |
| DOI: | 10.1016/j.bioorg.2017.02.005 |