Structure-activity relationships among di-and tetramine disulfides related to benextramine

M Alvarez, R Granados, D Mauleon…

Index: Alvarez, M.; Granados, R.; Mauleon, D.; Rosell, G.; Salas, M.; et al. Journal of Medicinal Chemistry, 1987 , vol. 30, # 7 p. 1186 - 1193

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Citation Number: 11

Abstract

The synthesis and irreversible a-blocking activity in the rat vas deferens of a series of tetra- and diamine disulfides 2-38, structural analogues of benextramine (BHC), are described. All compounds containing a central cystamine moiety displayed an irreversible a-adrenergic blockade at concentrations ranging from to 6 X lo4 M. Potency was increased in cystamines N, N'-disubstituted with 6-aminohexyl groups, especially when the outer nitrogen atoms ...