Synthesis and muscarinic activities of 1, 2, 4-thiadiazoles

…, S Patel, KJ Merchant, M Roe, J Saunders

Index: MacLeod; Baker; Freedman; Patel; Merchant; Roe; Saunders Journal of Medicinal Chemistry, 1990 , vol. 33, # 7 p. 2052 - 2059

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Citation Number: 50

Abstract

A series of novel 1, 2, Cthiadiazoles bearing a mono-or bicyclic amine at C5 were prepared. Quinuclidine and l-azabicyclo [2.2. l] heptane derivatives were synthesized by reaction of the lithium enolate of the 3-methoxycarbonyl compounds followed by ester hydrolysis and decarboxylation. The receptor-binding affinity and efficacy of these compounds as muscarinic ligands was assessed by radioligand binding assays using [3H]-N- ...