Arzneimittel-Forschung 1981-01-01

[Salts of 5-methylpyrazole-3-carboxylic acid with basically substituted adenine derivatives. Identification and lipolysis inhibitory activity (author's transl)].

K Credner, M Tauscher, L Jozić, G Brenner

Index: Arzneimittelforschung 31(12) , 2096-100, (1981)

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Abstract

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.