93117-84-1Relevant academic research and scientific papers
Synthesis and in vitro muscarinic activities of a series of 3-(pyrazol- 3-yl)-1-azabicyclo[2.2.2]octanes
Plate, Ralf,Plaum, Marc J. M.,Hulst, Rob G. A. V. D.,De Boer, Thijs
, p. 449 - 454 (2007/10/03)
A series of 3-(pyrazol-3-yl)-1-azabicyclo[2.2.2]octane derivatives C (Fig. 1) was synthesized and tested for muscarinic activity in receptor binding assays using [3H]-oxotremorine-M (OXO-M) and [3H]-pirenzepine (PZ) as ligands. Potential muscarinic agonistic or antagonistic properties of the compounds were determined using binding studies measuring their potencies to inhibit the binding of OXO-M and PZ. Preferential inhibition of OXO-M binding was used as an indicator for potential muscarinic agonistic properties; this potential was confirmed in functional studies on isolated organs. (C) 2000 Elsevier Science Ltd.
OXAZOLES AND THIAZOLES FOR THE TREATMENT OF SENILE DEMENTIA
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, (2008/06/13)
1,3-Oxazole and 1,3-thiazole compounds of formula I, and their pharmaceutically acceptable salts and prodrugs: STR1 wherein X represents oxygen or sulphur;R 1 represents a non-aromatic azacyclic or azabicyclic ring system.
Synthesis and Muscarinic Activities of Quinuclidin-3-yltriazole and -tetrazole Derivatives
Wadsworth, Harry J.,Jenkins, Sarah M.,Orlek, Barry S.,Cassidy, Frederick,Clark, Michael S. G.,et al.
, p. 1280 - 1290 (2007/10/02)
The synthesis of 15 methyl or unsubstituted 1,2,3-triazoles, 1,2,4-triazoles, and tetrazoles additionally substituted with a 1-azabicyclooctan-3-yl group is described.The potency and efficacy of these compounds as muscarinic ligands were determined in radioligand binding assays using oxotremorine and quinuclidinyl benzilate.Potency and efficacy were found in compounds in which the azole moiety was attached to the azabicyclic ring either through a carbon atom or a nitrogen atom.Electrostatic potential maps of both the C-linked and the novel N-linked series of compounds were calculated.A relationship between position and depth of the electrostatic minima relative to the azabicyclic ring and the potency and efficacy of the compounds was determined.
