Synthesis and benzodiazepine receptor activity of some 4,5-dihydro-1H-pyrazolo[4,3-c][1,8]naphthyridine derivatives. - Suppr | 超能文献

Synthesis and benzodiazepine receptor activity of some 4,5-dihydro-1H-pyrazolo[4,3-c][1,8]naphthyridine derivatives.

作者信息

Da Settimo A, Primofiore G, Da Settimo F, Simorini F, Barili P L, Senatore G, Martini C, Lucacchini A

机构信息

Istituto Chimica Farmaceutica e Tossicologica, Università di Pisa, Italy.

出版信息

Drug Des Discov. 1994 Jun;11(4):307-28.

Abstract

The preparation of 5-substituted 1-aryl-4,5-dihydro-1H-pyrazolo[4,3- c][1,8] naphthyridines by reaction of 5-substituted 3-hydroxymethylene-2,3-dihydro-1,8-naphthyridin-4(1H)-ones with various phenylhydrazines is described. The benzodiazepine binding activity of these compounds was evaluated in vitro. Only the 5-methyl substituted derivatives showed affinity for the benzodiazepine receptor, with K1 values ranging from 2.9 to 0.195 microM for the para-phenyl substituted compounds. A hypothesis of interaction of these ligands with the receptor site is reported.

摘要

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