ABSTRACT
The synthesis and structure activity relationships (SAR) of a series of novel selective COX-2 inhibitors are reported. The results show that some of the 1,3,4-triaryl-3-pyrrolin-2-ones 1 are more potent as COX-2 inhibitors than celecoxib, and that lactam Id has the same selectivity.
Subject(s)
Cyclooxygenase Inhibitors/chemical synthesis , Cyclooxygenase Inhibitors/pharmacology , Prostaglandin-Endoperoxide Synthases/drug effects , Pyrroles/chemical synthesis , Pyrroles/pharmacology , Cyclooxygenase 2 , Cyclooxygenase 2 Inhibitors , Cyclooxygenase Inhibitors/chemistry , Drug Evaluation , Isoenzymes/drug effects , Pyrroles/chemistry , Structure-Activity RelationshipABSTRACT
AIM: To research the behaviour of one biliary acid (glyco-cholic) i.v. injected in patients with Gilbert's disease and in healthy controls, so that contribute to the knowledge of the pathophysiological correlate between bilirubin and biliary acids. PATIENTS AND METHODS: We include 15 patients with Gilbert's disease and 7 healthy voluntary ones. We injected i.v. glycocholic acid and obtained the clearance curve (CG-RIA Abbot method). We evaluated the possible biostatistically significant differences between the obtained values of both groups though the non-parametric method of Mann-Whitney. RESULTS: The clearance curve of both groups had a similar profile; biostatisticaly there are not significant differences between the serum values of glyco-cholic acid in both groups. CONCLUSIONS: The clearance of the glyco-cholic acid in patients with Gilbert's disease had a similar behaviour as in healthy controls, without biostatisticaly significant differences between both groups.
Subject(s)
Cholagogues and Choleretics/pharmacokinetics , Gilbert Disease/metabolism , Glycocholic Acid/pharmacokinetics , Bile/metabolism , Cholagogues and Choleretics/administration & dosage , Glycocholic Acid/administration & dosage , Humans , Injections, Intravenous , Liver/metabolismABSTRACT
Plasma levels of d-xylose one hr after a standard 5 g oral dose were measured in 82 children suspected of having celiac disease. Duodenal mucosa was obtained by intestinal biopsy in all. Among patients with normal mucosa, 95% had xylose levels above 20 mg/dl; 100% of patients with a flat mucosa had levels under 20 mg/dl. Results were independent of patients age. We conclude that this is a reliable test to screen patients suspected of having celiac disease, prior to intestinal biopsy.
