Enantioselective synthesis of 3(S)-hydroxy polygodial derivatives and evaluation of their vanilloid activity |
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| Authors: | Mariantonietta D&rsquo Acunto,Irene Izzo,Vincenzo di Marzo |
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| Affiliation: | a Dipartimento di Chimica, Università di Salerno, Via Ponte Don Melillo, 84084 Fisciano, Salerno, Italyb Endocannabinoid Research Group, Istituto di Cibernetica, C.N.R., Via Campi Flegrei 34, 80078 Pozzuoli NA, Italyc Endocannabinoid Research Group, Istituto di Chimica Biomolecolare del CNR, Via Campi Flegrei 34, 80078 Pozzuoli NA, Italy |
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| Abstract: | The enantioselective synthesis of 3(S)-hydroxy polygodial and its acetyl derivative is described. The construction of the 3-hydroxy drimane skeleton was based on the titanium-catalyzed radical cyclization of (10S)-10, 11-epoxy-farnesyl acetate. Only underivatized 3(S)-hydroxy polygodial showed activity in assays on VR1 vanilloid receptor in HEK cells transfected with the human VR1. |
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