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

Autor:	Singh R; Medicinal Chemistry Division and Natural Product Chemistry Division , Indian Institute of Integrative Medicine (CSIR) , Canal Road , Jammu - 180001 , India.; Academy of Scientific & Innovative Research (AcSIR), at CSIR-IIIM, Jammu and CSIR-IITR , Lucknow - 226016 , India., Mandrah K; Academy of Scientific & Innovative Research (AcSIR), at CSIR-IIIM, Jammu and CSIR-IITR , Lucknow - 226016 , India.; Analytical Chemistry Laboratory, Regulatory Toxicology , Indian Institute of Toxicology Research (CSIR) , Vishvigyan Bhavan 31 , Mahatma Gandhi Marg, Lucknow - 226001 , Uttar Pradesh , India., Asati A; Academy of Scientific & Innovative Research (AcSIR), at CSIR-IIIM, Jammu and CSIR-IITR , Lucknow - 226016 , India.; Analytical Chemistry Laboratory, Regulatory Toxicology , Indian Institute of Toxicology Research (CSIR) , Vishvigyan Bhavan 31 , Mahatma Gandhi Marg, Lucknow - 226001 , Uttar Pradesh , India., Patel DK; Academy of Scientific & Innovative Research (AcSIR), at CSIR-IIIM, Jammu and CSIR-IITR , Lucknow - 226016 , India.; Analytical Chemistry Laboratory, Regulatory Toxicology , Indian Institute of Toxicology Research (CSIR) , Vishvigyan Bhavan 31 , Mahatma Gandhi Marg, Lucknow - 226001 , Uttar Pradesh , India., Goel B; Department of Pharmaceutical Engineering and Technology , Indian Institute of Technology (BHU) , Varanasi - 221005 , Uttar Pradesh , India., Vishwakarma RA; Medicinal Chemistry Division and Natural Product Chemistry Division , Indian Institute of Integrative Medicine (CSIR) , Canal Road , Jammu - 180001 , India.; Academy of Scientific & Innovative Research (AcSIR), at CSIR-IIIM, Jammu and CSIR-IITR , Lucknow - 226016 , India., Roy SK; Academy of Scientific & Innovative Research (AcSIR), at CSIR-IIIM, Jammu and CSIR-IITR , Lucknow - 226016 , India.; Analytical Chemistry Laboratory, Regulatory Toxicology , Indian Institute of Toxicology Research (CSIR) , Vishvigyan Bhavan 31 , Mahatma Gandhi Marg, Lucknow - 226001 , Uttar Pradesh , India., Jain SK; Medicinal Chemistry Division and Natural Product Chemistry Division , Indian Institute of Integrative Medicine (CSIR) , Canal Road , Jammu - 180001 , India.; Department of Pharmaceutical Engineering and Technology , Indian Institute of Technology (BHU) , Varanasi - 221005 , Uttar Pradesh , India.
Jazyk:	angličtina
Zdroj:	Journal of natural products [J Nat Prod] 2019 Jun 28; Vol. 82 (6), pp. 1710-1713. Date of Electronic Publication: 2019 May 24.
DOI:	10.1021/acs.jnatprod.8b00318
Abstrakt:	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 (IC 50 = 31.0 and 66.1 μM, respectively).
Databáze:	MEDLINE
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