PMID: 6103962May 1, 1980Paper

Tricyclics with analgesic and antidepressant activity. 1. [[(Alkylamino)ethyl]thio]dibenz[b,f]oxepins and 10,11-dihydro derivatives

Journal of Medicinal Chemistry
H H OngH Kruse

Abstract

A series of [[(alkylamino)ethyl]thio]dibenz[b,f]oxepins (I) and their 10,11-dihydro derivatives (II) was synthesized and subjected to broad analgesic/CNS screening. Several analogues of both types, carrying small N-substituents and frequently a nuclear fluorine function, have been found to possess potent analgesic activity in the phenylquinone writhing assay (PQW) and the tail-flick test in mice. Many of these compounds also exhibited significant activity in antagonizing tetrabenazine-induced ptosis, as exemplified by 10b, 16b, and 18b. Results from the mouse jumping test indicated low physical dependence potential for these compounds, and further evidence for a nonnarcotic profile was provided by the absence of significant naloxone interactions with the tail-flick response. Compound 10b did not produce tolerance in mice following chronic administration in the PQW screen.

Citations

Jun 25, 2003·Neurochemistry International·Péter BarabásJulianna Kardos
Dec 20, 2013·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·David R R MorenoRicardo A Tapia
Oct 12, 2018·Organic & Biomolecular Chemistry·Niranjan PandaChandra Shekhar Purohit
Jan 1, 2021·Biomedicine & Pharmacotherapy = Biomédecine & Pharmacothérapie·Filip BorysHanna Krawczyk
Sep 19, 2012·Organic Letters·Young Lok ChoiJung-Nyoung Heo
Oct 15, 2010·Journal of Medicinal Chemistry·Massimo GianottiMark J Wigglesworth
Jan 6, 2021·The Journal of Organic Chemistry·Pondpavee TaweesakPaiboon Ngernmeesri
Dec 5, 2003·Organic Letters·M Peggy Paduraru, Peter D Wilson

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