57734-73-3Relevant academic research and scientific papers
QUINUCLIDINE DERIVATIVE
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Paragraph 0227; 0228; 0229; 0230, (2018/03/10)
Provided is a novel therapeutic agent for chronic obstructive pulmonary disease. Provided are a quinuclidine derivative and a medicament comprising the quinuclidine derivative. wherein R1 represents a hydrogen atom, a halogen atom, a lower alkyl group, a haloalkyl group, a lower alkoxy group, or a haloalkoxy group; Y represents —C(C═O)—O—, —CH2—, or —CH2O—; m represents an integer of 1 to 5; Z represents an oxygen atom or a sulfur atom; l represents a number of 0 or 1; n represents an integer of 0 to 4; X? represents an anion; and a substituent of a quinuclidine ring represents a 1,3-bond, or 1,4-bond, provided that when m is 3, l is 1, and n is 0, R1 represents a halogen atom, a lower alkyl group, a haloalkyl group, a lower alkoxy group, or a haloalkoxy group.
Discovery of novel 1-azoniabicyclo[2.2.2]octane muscarinic acetylcholine receptor antagonists
Lainé, Dramane I.,McCleland, Brent,Thomas, Sonia,Neipp, Christopher,Underwood, Brian,Dufour, Jeremy,Widdowson, Katherine L.,Palovich, Michael R.,Blaney, Frank E.,Foley, James J.,Webb, Edward F.,Luttmann, Mark A.,Burman, Miriam,Belmonte, Kristen,Salmon, Michael
experimental part, p. 2493 - 2505 (2010/03/04)
A novel 4-hydroxyl(diphenyl)methyl substituted quinuclidine series was discovered as a very promising class of muscarinic antagonists. The structure-activity relationships of the connectivity of the diphenyl moiety to the quinuclidine core and around the ring nitrogen side chain are described. Computational docking studies using an homology model of the M3 receptor readily explained the observed structure-activity relationship of the various compounds. Compound 14o was identified as a very potent, slowly reversible M3 antagonist with a very long in vivo duration of bronchoprotection.
