Affiliation:
1. N.N. Vorozhtsov Novosibirsk Institute of Organiс Сhemistry, Siberian Branсh, Russian Aсademy of Sсienсes, Lavrentjev Avenue, 9, 630090 Novosibirsk, Russian Federation
Abstract
Background:
Despite a variety of drugs used to stop acute pain, problems related to their
insufficient efficacy and undesirable side effects have remained unresolved. Therefore, the search for
analgesics of new structural types, which combine high activity with low toxicity, is a topical issue.
It is known that a number of compounds with a hydrogenated 2H-chromene skeleton exhibit
significant analgesic activity in in vivo tests.
Methods:
New hydro-2H-chromenols containing monoterpenoid moieties were obtained via one-pot
synthesis by the interaction between para-menthane alcohols and commercially available
monoterpene aldehydes: Citral, hydroxycitronellal, myrtenal, and perillaldehyde. The analgesic
activity of these compounds wаs studied in the acetic acid-induced writhing test and hot plate test.
Results:
The target compounds were characterized using NMR and HR-MS. Most of them exhibited
pronounced analgesic activity.
Conclusion:
Due to high analgesic activity, (2S,4aR,8R,8aR)-2-((E)-2,6-dimethylhepta-1,5-dien-1-
yl)-4,7-dimethyl-3,4,4a,5,8,8a-hexahydro-2H-chromene-4,8-diol is considered as candidate compound
to participate in further research.
Publisher
Bentham Science Publishers Ltd.
Subject
Drug Discovery,Pharmaceutical Science,Molecular Medicine
Cited by
8 articles.
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