Synthesis and structure-activity relationships of 1-acyl-4-((2-methyl-3-pyridyl) cyanomethyl) piperazines as PAF antagonists

E Carceller, M Merlos, M Giral, C Almansa…

Index: Carceller, Elena; Merlos, Manuel; Giral, Marta; Almansa, Carmen; Bartroli, Javier; et al. Journal of Medicinal Chemistry, 1993 , vol. 36, # 20 p. 2984 - 2997

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Citation Number: 39

Abstract

The most interesting compounds, 26 (UR-12460, PAG ICs0= 0.040 pM, HYP, IDm= 0.021 mg/kg iv, MOR, IDW= 0.30 mg/kg PO) and 58 (UR-12519, PAG ICW= 0.041 pM, HYP, IDW= 0.015 mg/kg iv, MOR, IDw= 0.044 mg/kg PO), compare favorably with WEB-2086. Compounds 26 and 58 were also tested in active anaphylactic shock (AAS) and endotoxin- induced mortality (EIM) tests. On the basis of these data, compounds 26 and 58 have ...