Synthesis and Preliminary Pharmacological Investigation of New  N ‐Substituted‐ N ‐[ω‐(ω‐phenoxy‐alkylpiperazin‐1‐yl)alkyl]guanidines as Non‐Imidazole Histamine H 3  Antagonists | Zendy

Staszewski Marek | Zendy; Walczyński Krzysztof | Zendy

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Synthesis and Preliminary Pharmacological Investigation of New N ‐Substituted‐ N ‐[ω‐(ω‐phenoxy‐alkylpiperazin‐1‐yl)alkyl]guanidines as Non‐Imidazole Histamine H 3 Antagonists

Author(s) -

Staszewski Marek,

Walczyński Krzysztof

Publication year - 2012

Publication title -

archiv der pharmazie

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 0.468

H-Index - 61

eISSN - 1521-4184

pISSN - 0365-6233

DOI - 10.1002/ardp.201100428

Subject(s) - histamine , imidazole , guanidine , chemistry , stereochemistry , in vitro , histamine receptor , histamine h2 receptor , biological activity , receptor , alkyl , chemical synthesis , medicinal chemistry , antagonist , pharmacology , biochemistry , organic chemistry , biology

Novel, potent non‐imidazole histamine H 3 receptor antagonists were prepared. Detailed structure–activity studies revealed that N ‐(4‐trifluoromethylbenzyl)‐ N ‐[4‐(7‐phenoxyheptylpiperazin‐1‐yl)butyl]guanidine (pA 2 = 8.49 ± 0.05), 1h , and N ‐(4‐nitrobenzyl)‐ N ‐[4‐(7‐phenoxyheptylpiperazin‐1‐yl)butyl]guanidine (pA 2 = 8.43 ± 0.05), 1l , exhibit high affinity for the H 3 histamine receptor. The most potent antagonists in this series, 1e , 1h , and 1l , were also in vitro tested as H 1 receptor antagonists, showing weak H 1 ‐antagonistic activity with pA 2 = 6.70 ± 0.09, pA 2 = 6.46 ± 0.09, and pA 2 = 6.65 ± 0.11, respectively.

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