Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 29, Issue 18, Pages 2604-2608Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2019.07.055
Keywords
Melanogenesis; alpha-MSH; Arbutin; N-Arylindazole-3-carboxamides; N-Benzoylindazoles
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Funding
- National Research Foundation of Korea (NRF) - Korea government (MSIT) [NRF-2019R1F1A1057601]
- Medical Research Center Program [2017R1A5A2015541]
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We have designed and synthesized twenty-six N-arylindazole-3-carboxamide (3a-p) and N-benzoylindazole (6a-j) derivatives to discover with excellent inhibition activities of alpha-MSH-stimulated melanogenesis. In the bio evaluation studies of these compounds, we discovered eighteen compounds, out of twenty-six exhibited more potent inhibition than the positive control arbutin. From the SAR studies, we identified 3k and 6g as lead compounds which displayed almost 5 and 9 times more potent inhibition of alpha-MSH-stimulated melanogenesis respectively than the reference arbutin. It is also evident the presence of electron withdrawing group at para position (R-3) for the compounds (3a-p) and presence of +M group at ortho position (R-5) for the compounds (6a-j) were crucial for their excellent inhibition activities of alpha-MSH-stimulated melanogenesis.
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