Multi-step synthesis of indole-N-ethyltriazole hybrids amalgamated with N-arylated ethanamides: structure-activity relationship and mechanistic explorations through tyrosinase inhibition, kinetics and computational ascriptions
In the study presented here, novel bioactive series of indole-N-ethyltriazole hybrids was synthesized and structures of these hybrid molecules (9a-h) were corroborated by IR, 1H-NMR, 13C-NMR, EI-MS and CHN analysis data. The in vitro studies of these multi-functional molecules demonstrated their pot...
| Published in: | Journal of Molecular Structure |
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| Main Author: | |
| Format: | Article |
| Language: | English |
| Published: |
Elsevier B.V.
2022
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| Online Access: | https://www.scopus.com/inward/record.uri?eid=2-s2.0-85127463628&doi=10.1016%2fj.molstruc.2022.132953&partnerID=40&md5=a567d0d1dd7289e4bc0c51a9dcf8ddab |
| Summary: | In the study presented here, novel bioactive series of indole-N-ethyltriazole hybrids was synthesized and structures of these hybrid molecules (9a-h) were corroborated by IR, 1H-NMR, 13C-NMR, EI-MS and CHN analysis data. The in vitro studies of these multi-functional molecules demonstrated their potent tyrosinase inhibition relative to the standard used and all the synthesized compounds showed mild hemolysis. The kinetics mechanism was exposed by lineweaver-burk plots which revealed that, 9c, inhibited tyrosinase non-competitively by forming an enzyme-inhibitor complex. So, it was summated that these hybrid molecules might lead to further research gateways for obtaining better and safe therapeutic agents for skin pigmentation and related ailments. © 2022 |
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| ISSN: | 222860 |
| DOI: | 10.1016/j.molstruc.2022.132953 |