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  • Title: [Azoles. 12. Pyrazole carbolic acid thioamides].
    Author: Bernard M, Bober M, Krzysztofik B, Skoczna J, Stochla K, Szymczak-Meyer L, Westfal I, Wrzeciono U.
    Journal: Pharmazie; 1984 Jul; 39(7):464-6. PubMed ID: 6436841.
    Abstract:
    Morpholids, N-methylpiperazids, piperidids and pyrrolidids of 5-methyl, 3,5-dimethyl-1-phenyl-4-pyrazolthioacetic acid and 3,5-dimethyl-1-phenyl-4-pyrazolcarbonic acid 4-12 are obtained by the Willgerodt-Kindler procedure. The oxothioamids 13-19 result as the intermediate products of the synthesis of thioamids 4-10. The compounds 4, 5, 8, 9, 11, 14 and 17 do not respond to Mycobacterium tuberculosis H37Rv. The thioamids 4, 8 and 11 are of slight toxicity (LD50 greater than 2.8 g/kg, albino-Swiss mice) and inhibit the Carrageenin oedema of the Wistar rat claw minor than phyenylbutazon and indometacin.
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