[Salts of 5-methylpyrazole-3-carboxylic acid with basically substituted adenine derivatives. Identification and lipolysis inhibitory activity (author's transl)].
5-Methylpyrazole-3-carboxylic acid forms salts with basically substituted adenine bases of type (4) or (5), which have significantly more lipolysis inhibitory activity than the free acid itself. The substance tested, 6-amino-9-[2-hydroxy-3-(N-methyl-N-2-hydroxyethyl)-aminopropyl]-purine-5-methyl pyrazole-3-carboxylate (16), causes a significant reduction of serum FFA levels in fasted rats, even at the very low dosage of 0.150 mg/kg b.w., whereas the free 5-methylpyrazole-3-carboxylic-acid shows significant activity in this model only at doses of 2 mg/kg b.w. and above. The salt also shows similar activity on serum triglycerides. The effect on FFA, triglyceride and cholesterol levels, respectively, in fasted rats lasts for at least 8 h.
D000225:Adenine / Q000031:analogs & derivatives*; D000818:Animals; D002625:Chemistry, Organic; D008066:Lipolysis / Q000187:drug effects; D008297:Male; D055601:Organic Chemistry Phenomena; D011720:Pyrazoles / Q000494:pharmacology; D051381:Rats
D011720:Pyrazoles; D000225:Adenine; C005210:5-methylpyrazole-3-carboxylic acid
Salze der 5-Methylpyrazol-3-carbonsäure mit basisch substituierten Adenin-Derivaten. Darstellung und lipolysehemmende Wirkung.