Il Farmaco

Non-imidazole histamine H 3 ligands. Part I. Synthesis of 2-(1-piperazinyl)-and 2-(hexahydro-1H-1, 4-diazepin-1-yl) benzothiazole derivatives as H 3-antagonists with …

K Walczyński, R Guryn, OP Zuiderveld, H Timmerman

Index: Walczynski, Krzysztof; Guryn, Roman; Zuiderveld, Obbe P.; Timmerman, Henk Farmaco, 1999 , vol. 54, # 10 p. 684 - 694

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Citation Number: 63

Abstract

New 2-(1-Piperazinyl)-and 2-(hexahydro-1H-1, 4-diazepin-1-yl) benzothiazoles were prepared and tested as H1-and H3-receptor antagonists. A number of compounds showed weak H1-antagonistic activity, with pA2 values ranging from 5.5 to 6.1. The simple alkyl substituted, 2-[1-(4-methyl and 4-ethyl) piperazinyl] analogues show increasing, moderate H3-antagonistic activity (pA2= 6.0, and pA2= 7.0). The compounds with 4-phenylalkyl ...