Pharmaceuticals. Tracking down an unidentified trace level constituent.
Explore the source record for details and available documents.
Chemical Phenomena↗
Biomedical subjects
F K Hess
Publications and source records attributed to F K Hess.
N-(4-substituted-thiazolyl)oxamic acid derivatives, a new series of potent, orally active antiallergy agents.
A series of N-(4-substituted-thiazolyl)oxamic acid derivatives were synthesized and tested for antiallergy activity in the rat PCA model. These compounds were conveniently prepared by treatment of the appropriate acetophenone with thiourea and iodine or by reaction of the chloroacetylbenzene with thiourea to give the corresponding aminothiazoles; subsequent condensation with ethyloxalyl chloride gave the thiazolyloxamates. Many of the analogues showed a 50% inhibition at less than 2 mg/kg po or less than 0.4 mg/kg iv and were significantly more potent than disodium cromoglycate, which in the rat PCA model is orally inactive and gives a 50% inhibition at 1.2 mg/kg iv. Hydrolysis of the oxamates generally resulted in enhanced activities, while substitution of the phenyl ring with a variety of substituents (e.g., 4-F, 4-OEt, and 4-NHCOCH3) did not significantly enhance the activity of the unsubstituted phenyl derivative. One of the ethanolamine salts, N-[4-(1,4-benzodioxan-6-yl)-2-thiazolyl]oxamic acid ethanolamine salt (61, PRH-836-EA), has been selected for further pharmacological evaluation.
Animals↗
Preparation of a new immunosuppressant, 4-5-bis(aminomethyl)acridine.
4,5-Bis(aminomethyl)acridine, useful as an immunosuppressant, was prepared in 31% overall yield by the reaction of acridine with N-(hydroxymethyl)phthalimide and subsequent decomposition with excess 6 N HCl. The drug was found to produce a suppression of the humoral antibody response comparable to several known immunosuppressive agents.
Acridines↗