Non-imidazole histamine H3 ligands. Part I. Synthesis of 2-(1-piperazinyl)- and 2-(hexahydro-1H-1,4-diazepin-1-yl)benzothiazole derivatives as H3-antagonists with H1 blocking activities
| Autor: | Henk Timmerman, Krzysztof Walczyński, Roman Guryn, Obbe P. Zuiderveld |
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| Rok vydání: | 1999 |
| Předmět: |
Male
chemistry.chemical_classification Bicyclic molecule Stereochemistry Guinea Pigs Histamine Antagonists Antagonist Pharmaceutical Science Ring (chemistry) Chemical synthesis Structure-Activity Relationship Thiazoles chemistry.chemical_compound Benzothiazole chemistry Drug Discovery Histamine H1 Antagonists Animals Receptors Histamine H3 Imidazole Histamine Alkyl |
| Zdroj: | Il Farmaco. 54:684-694 |
| ISSN: | 0014-827X |
| DOI: | 10.1016/s0014-827x(99)00081-6 |
| Popis: | New 2-(1-Piperazinyl)- and 2-(hexahydro-1 H -1,4-diazepin-1-yl)benzothiazoles were prepared and tested as H 1 - and H 3 -receptor antagonists. A number of compounds showed weak H 1 -antagonistic activity, with p A 2 values ranging from 5.5 to 6.1. The simple alkyl substituted, 2-[1-(4-methyl and 4-ethyl)piperazinyl] analogues show increasing, moderate H 3 -antagonistic activity (p A 2 =6.0, and p A 2 =7.0). The compounds with 4-phenylalkyl substitution, for both the piperazinyl and the hexahydro-1 H -1,4-diazepin-1-yl homologues series, regardless of the different physicochemical properties of the para substituents at the phenyl ring, showed weak H 3 -antagonistic activity with p A 2 values ranging from 4.4 to 5.6. |
| Databáze: | OpenAIRE |
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