Synthesis and biological characterization of 1-methyl-1,2,5,6-tetrahydropyridyl-1,2,5-thiadiazole derivatives as muscarinic agonists for the treatment of neurological disorders

Yang Cao, Minjia Zhang, Cindy Wu, Selina Lee, Mary Elizabeth Wroblewski, Trisha Whipple, Peter I. Nagy, Krisztina Takács-Novák, Attila Balázs, Szilárd Torös, William S. Messer

Research output: Contribution to journalArticle

24 Citations (Scopus)

Abstract

Muscarinic agonists might be useful in the treatment of neurological disorders, including Alzheimer's disease, schizophrenia, chronic pain, and drug abuse. Previous studies identified a series of bis-1,2,5-thiadiazole derivatives of 1,2,5,6-tetrahydropyridine with high activity and selectivity for muscarinic receptors. To develop compounds with improved central nervous system penetration, several new derivatives were synthesized and characterized for muscarinic receptor binding and activity. One ligand (11) exhibited agonist activity at M1, M2, and M4 receptors, a selectivity profile suggesting potential utility in the treatment of schizophrenia.

Original languageEnglish
Pages (from-to)4273-4286
Number of pages14
JournalJournal of Medicinal Chemistry
Volume46
Issue number20
DOIs
Publication statusPublished - Sep 25 2003

ASJC Scopus subject areas

  • Molecular Medicine
  • Drug Discovery

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