Transformation of Santonin to a Naproxen Analogue with Anti-Inflammatory Activity

Autor:	Kapil Mandrah, Somendu Kumar Roy, Ram A. Vishwakarma, Devendra Kumar Patel, Bharat Goel, Shreyans K. Jain, Rohit Singh, Ankita Asati
Rok vydání:	2019
Předmět:	Naproxen medicine.drug_class Anti-Inflammatory Agents Pharmaceutical Science Medicinal chemistry Anti-inflammatory Analytical Chemistry chemistry.chemical_compound Drug Discovery medicine Potency Cyclooxygenase Inhibitors IC50 Santonin Pharmacology Natural product Molecular Structure biology Anti-Inflammatory Agents Non-Steroidal Organic Chemistry Complementary and alternative medicine chemistry Cyclooxygenase 2 Cyclooxygenase 1 biology.protein Molecular Medicine Cyclooxygenase Two-dimensional nuclear magnetic resonance spectroscopy medicine.drug
Zdroj:	Journal of Natural Products. 82:1710-1713
ISSN:	1520-6025 0163-3864
Popis:	Santonin, a natural product, was aromatized with molecular iodine as the catalyst. The new compound was characterized as ( S)-methyl-2-(7-hydroxy-5,8-dimethylnaphthalen-2-yl) propanoate (2) based on 2D NMR spectroscopic data. Structurally, compound 2 was highly similar to the anti-inflammatory drug naproxen. The new naproxen analogue had significant potency against cyclooxygenase 1 and 2 (IC50 = 31.0 and 66.1 μM, respectively).
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c43b54a573ac21fa6ee8b4a3e46829b3 https://doi.org/10.1021/acs.jnatprod.8b00318 Zobrazit plný text záznamu