2. Academic Validation
  3. Design and synthesis of m1-selective muscarinic agonists: (R)-(-)-(Z)-1-Azabicyclo[2.2.1]heptan-3-one, O-(3-(3'-methoxyphenyl)-2-propynyl)oxime maleate (CI-1017), a functionally m1-selective muscarinic agonist

Design and synthesis of m1-selective muscarinic agonists: (R)-(-)-(Z)-1-Azabicyclo[2.2.1]heptan-3-one, O-(3-(3'-methoxyphenyl)-2-propynyl)oxime maleate (CI-1017), a functionally m1-selective muscarinic agonist

  • J Med Chem. 1998 Jul 2;41(14):2524-36. doi: 10.1021/jm960683m.
H Tecle 1,  S D Barrett,  D J Lauffer,  C Augelli-Szafran,  M R Brann,  M J Callahan,  B W Caprathe,  R E Davis,  P D Doyle,  D Eubanks,  W Lipiniski,  T Mirzadegan,  W H Moos,  D W Moreland,  C B Nelson,  M R Pavia,  C Raby,  R D Schwarz,  C J Spencer,  A J Thomas,  J C Jaen
Affiliations

Affiliation

  • 1 Parke-Davis Pharmaceutical Research, Division of Warner-Lambert Company, Ann Arbor, Michigan 48106-1047, USA.
PMID: 9651157 DOI: 10.1021/jm960683m
Abstract

The synthesis and SAR of a series of (Z)-(+/-)-1-azabicyclo[2.2. 1]heptan-3-one, O-(3-aryl-2-propynyl)oximes are described. The biochemistry and pharmacology of 24Z (PD 142505) and its enantiomers are highlighted. 24Z is functionally an m1-selective muscarinic agonist. Efficacy and m1 selectivity reside in the R enantiomer, (R)-24Z (CI-1017).

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