Non-imidazole histamine H3 ligands, Part IV: SAR of 1-[2-thiazol-5-yl-(2-aminoethyl)]-4-n-propylpiperazine derivatives

Add time:07/12/2019    Source:sciencedirect.com

A series of 1-[[2-thiazol-5-yl-(2-aminoethyl)]-4-n-propyl]piperazine derivatives have been prepared and in vitro tested as H3-receptor antagonists (the electrically evoked contraction of the guinea pig jejunum). It appeared that by comparison of homologous pairs the 1-[[2-thiazol-5-yl-(2-methyl-2-phenylalkylaminoethyl)]-4-n-propyl]piperazine derivatives (4c1–4c3) have slightly higher activity than their 1-[2-thiazol-5-yl-(2-methyl-2-alkylaminoethyl)]-4-n-propylpiperazine analogues (4b1–4b3). In the 2-methylalkylamide series (4a1–4a3) a somewhat lower activity was observed. The most potent compound of the series is the 1-[2-thiazol-5-yl-(2-methyl-2-phenylpropylaminoethyl)]-4-n-propylpiperazine (4c2) with pA2 = 8.27 (its alkyl analogue (4b2) showed pA2 = 7.53 and the corresponding amide (4a2) displayed pA2 = 7.36).Selected compounds (4b1, 4b2, 4c1 and 4c2) were also tested (in vitro) for H1 antagonistic effects in vitro applying standard methods (guinea pig ileum). None showed any H1 antagonistic activity (pA2 < 4).

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