Pharmacological activity in the group of new substituted thiazoloacetic and thiazinocarboxyl acid derivatives.
37 newly synthesized compounds in the group of thiazoloacetic and thiazinocarboxyl aciderivatives with the possibly immunotropic, antiinflammatory and probably central activity were studied. A number of them was not resorbed and only 21 agents were immunopharmacologically investigated. The correlations between the biological activity and chemical structure were confirmed. Among acyl derivatives of thiazoloacetic acid the compounds containing two carboxyl radicals at C2 and C5 revealed the most interesting activity. For 2-N-aralkylo-alfa-sulfonic derivatives of thiazoloacetic acid, the distinct immunosuppressive activity with antiinflammatory component was found. The group of 16 derivatives of thiazinocarboxyl acid had the chemical structure correlated with the immunotropic activity (immunosuppressive or immunostimulative) and antiinflammatory component. Immunosuppressive activity was manifested, in the first place, by the derivatives containing radicals--ethyl, butyl, methoxyphenyl and two groups of cyclohexyl. The compound with allylimino group showed, however, the most immunostimulating activity. The antiinflammatory activity was correlated especially with radicals--cyclohexyl, chlorophenyl and allylimino.
D000818:Animals; D000893:Anti-Inflammatory Agents; D000917:Antibody Formation / Q000187:drug effects; D006168:Guinea Pigs; D007156:Immunologic Memory / Q000187:drug effects; D007166:Immunosuppressive Agents; D007928:Lethal Dose 50; D008213:Lymphocyte Activation / Q000187:drug effects; D051379:Mice; D051381:Rats; D012397:Rosette Formation; D013329:Structure-Activity Relationship; D013843:Thiazines / Q000494:pharmacology*; D013844:Thiazoles / Q000494:pharmacology*
D000893:Anti-Inflammatory Agents; D007166:Immunosuppressive Agents; D013843:Thiazines; D013844:Thiazoles