Pharmacological activity of 3-(5-barbiturylo)-propanesulfonic acids derivatives.
Pharmacological activity of 6 newly synthetized water-soluble derivatives of barbiturylo propanosulfonic acids, was evaluated. The compounds were obtained under the conditions of the Ritter reaction. The experiments were performed with the aim to determine the anti-inflammatory and immunotropic activities as well as the central action of the new derivatives; indomethacin was a reference preparation. 5-Allyl-2,4,6-trioxo-5-hexahydropyrimidine-beta-sulfooxy+ ++-propanesulfonic acid displayed pronounced anti-inflammatory and analgesic activity accompanied by immunosuppressive effect observed in the in vitro tests. An introduction of the cyclohexyl group by nitrogen in position 1 of the barbituric ring deprived the new compound of numerous properties; its activity was preserved only in Jerne's test, PFC number was reduced by 50%. On the other hand, the presence of two cyclohexyl groups and beta-hydroxypropanesulfonic and beta-sulfatopropanesulfonic in position 5, conditioned the anti-inflammatory and immunotropic activity of the new derivative. 1,3-Dicyclohexyl-2,4,6-trioxo-hexahydropyrimidine-5, 5-di(beta-hydroxy-propanesulfonic acid) (prep. 5) as the only one in this group, almost completely suppressed the post-carageenin edema. It also diminished the number of RFC and PFC and weakened the cellular response to SRBC. The preparation also increased the viability of multipotential stem cells exposed to Rtg irradiation (the number of endogenous CFU-s increased by 50%). The preparations examined displayed various anti-inflammatory and immunotropic activity dependently on the chemical structure and in some experimental models they appeared more effective than indomethacin.
D000276:Adjuvants, Immunologic; D000476:Alkanesulfonates / Q000138:chemical synthesis / Q000494:pharmacology*; D000700:Analgesics; D000818:Animals; D000893:Anti-Inflammatory Agents; D001463:Barbiturates / Q000138:chemical synthesis / Q000494:pharmacology*; D006993:Hypnotics and Sedatives; D007213:Indomethacin / Q000494:pharmacology; D051379:Mice; D013329:Structure-Activity Relationship
D000276:Adjuvants, Immunologic; D000476:Alkanesulfonates; D000700:Analgesics; D000893:Anti-Inflammatory Agents; D001463:Barbiturates; D006993:Hypnotics and Sedatives; D007213:Indomethacin