Synthesis of some dibenzodiazepinone derivatives as potent and m2‐selective antimuscarinic compounds | Zendy

Cohen Victor I. | Zendy; Jin Biyun | Zendy; Gitler Miriam S. | Zendy; De Cruz Rosanna A. La | Zendy; Rzeszotarski Waclaw J. | Zendy; Zeeberg Barry R. | Zendy; Baumgold Jesse | Zendy; Reba Richard C. | Zendy

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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.

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