1. Academic Validation
  2. Synthetic studies of neoclerodane diterpenes from Salvia divinorum: preparation and opioid receptor activity of salvinicin analogues

Synthetic studies of neoclerodane diterpenes from Salvia divinorum: preparation and opioid receptor activity of salvinicin analogues

  • J Med Chem. 2007 Jul 26;50(15):3596-603. doi: 10.1021/jm070393d.
Denise S Simpson 1 Peter L Katavic Anthony Lozama Wayne W Harding Damon Parrish Jeffrey R Deschamps Christina M Dersch John S Partilla Richard B Rothman Hernan Navarro Thomas E Prisinzano
Affiliations

Affiliation

  • 1 Division of Medicinal & Natural Products Chemistry, College of Pharmacy, The University of Iowa, Iowa City, Iowa 52242, USA.
Abstract

Further modification of salvinorin A (1a), the major active component of Salvia divinorum, has resulted in the synthesis of novel neoclerodane diterpenes with Opioid Receptor affinity and activity. We report in this study that oxadiazole 11a and salvidivin A (12a), a photooxygenation product of 1a, have been identified as the first neoclerodane diterpenes with kappa antagonist activity. This indicates that additional structural modifications of 1a may lead to analogues with higher potency and utility as drug abuse medications.

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