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PubMed1984

[Azoles. 12. Pyrazole carbolic acid thioamides].

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.

Animals↗
PubMed1982

[Effect of 3-(4-chlorphenyl-) 1-phenyl-1H-pyrazole-4-acetic acid (lonazolac-Ca), diclofenac-Na and indomethacin on the gastrointestinal blood loss].

According to a Latin Square-2 block study design gastrointestinal blood loss after medication with lonacolac-Ca (200 mg t.i.d.), diclofenac-Na (50 mg t.i.d.) and indomethacin (50 mg t.i.d.) was investigated in 6 healthy volunteers. Blood loss was estimated by measuring 51Cr-labelled erythrocytes in the faeces. Each active substance was taken for one week in randomized order, followed by a 7-day period of placebo administration (wash-out period). Stool samples were collected daily, also during placebo periods. Average weekly blood loss was 13.76 ml after lonacolac-Ca, 12.57 ml after diclofenac-Na and 23.687 ml after indomethacin. Blood loss was significantly lower with lonazolac-Ca and diclofenac-Na than with indomethacin (p less than 0.001). There is no difference statistically between the two former substances.

Anti-Inflammatory Agents↗
PubMedDate not supplied

[Effect of the structural characteristics of the alkyl derivatives of imidazole and pyrazole dicarboxylic acid diamides on body respiratory functions].

It has been ascertained that alkyl derivatives of imidazoledicarboxylic acid diamides produce different effect on respiration and acid-base balance (ABB) of animal body. Antiphein and ethymisole stimulate respiration and change ABB. Ethirazol does not affect respiration, producing only insignificant changes in the respiratory component of ABB. Differences in the biological activity of the test drugs may be related to the structure or position of the alkyl radical in the heterocyclic ring.

Acid-Base Equilibrium↗