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Synthesis of some dibenzodiazepinone derivatives as potent and m2‐selective antimuscarinic compounds
Author(s) -
Cohen Victor I.,
Jin Biyun,
Gitler Miriam S.,
De Cruz Rosanna A. La,
Rzeszotarski Waclaw J.,
Zeeberg Barry R.,
Baumgold Jesse,
Reba Richard C.
Publication year - 1994
Publication title -
journal of heterocyclic chemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.321
H-Index - 59
eISSN - 1943-5193
pISSN - 0022-152X
DOI - 10.1002/jhet.5570310416
Subject(s) - chemistry , piperidine , selectivity , muscarinic acetylcholine receptor , stereochemistry , cholinergic , ring (chemistry) , receptor , medicinal chemistry , organic chemistry , biochemistry , medicine , catalysis
Two series of 5‐[[4‐[4‐(dialkylamino)butyl]‐l‐cyclohexyl]acetyl], and 5‐[(dialkylamino)acyl]‐10,11‐dihydro‐5 H ‐ dibenzo[ b,e ][1,4]diazepin‐11‐ones were synthesized as potential m2‐selective ligands 1,2. Their affinity and selectivity for the muscarinic cholinergic receptor m ‐AChR subtypes were determined. Replacing a nitrogen with CH in the piperidine ring of 5‐[[4‐[4‐(dialkylamino)butyl]‐l‐piperidinyl]acetyl]‐10,11‐dihydro‐5 H ‐dibenzo‐[ b,e ][1,4]diazepin‐11‐ones 3 significantly altered the affinity and selectivity to the muscarinic receptor subtypes.