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Biomedical subjects

G Y Paris

Publications and source records attributed to G Y Paris.

8 recordsLinked to original sources
PubMed1980

Pharmacological studies in the rat with [2-(1,3-didecanoyloxy)-propyl]2-acetyloxybenzoate (A-45474): an aspirin pro-drug with negligible gastric irritation.

A triglyceride of aspirin, A-45474: [2-(1,3-didecanoyloxy)-propyl]2-acetyloxybenzoate, was developed to reduce the direct gastric irritant properties of aspirin. Studies in the rat show that oral administration of A-45474 produces anti-inflammatory activity comparable to aspirin with negligible gastric irritation. Compared with aspirin, plasma salicylate levels of A-45474 appeared less rapidly and were more sustained. It is concluded that incorporation of aspirin in the 2-position of a triglyceride bearing n-decanoyl groups in the 1- and 3-positions markedly reduces the gastric irritating properties of aspirin while maintaining its pharmacological effects.

Administration, Oral↗
PubMed1980

Glycerides as prodrugs. 3. Synthesis and antiinflammatory activity of [1-(p-chlorobenzoyl)-5-methoxy-2-methylindole-3-acetyl]glycerides (indomethacin glycerides).

Mono-, bis-, and tris[1-(p-chlorobenzoyl)-5-methoxy-2-methylindole-3-acetyl]glycerides and 1,3-dialkanoyl-2-[1-(p-chlorobenzoyl)-5-methoxy-2-methylindole-3-acetyl]glycerides were synthesized and evaluated for antiinflammatory activity in the rat paw carrageenin edema assay. Three of the most active compounds (4, 18a, and 18e) were tested in the rat adjuvant arthritis model and found to be essentially equivalent in activity to indomethacin. On a molar basis, the acute gastric irritating properties of 18a and 18e were seven to eight times less than indomethacin, resulting in a 2.5- to 3-fold improvement in the ratio of antiedema activity to ulcerogenicity.

Animals↗
PubMed1980

Glycerides as prodrugs. 2. 1,3-Dialkanoyl-2-(2-methyl-4-oxo-1,3-benzodioxan-2-yl)glycerides (cyclic aspirin triglycerides) as antiinflammatory agents.

A series of 1,3-dialkanoyl-2-(2-methyl-4-oxo-1,3-benzodioxan-2-yl)glycerides ("cyclic aspirin triglycerides") was synthesized. They demonstrated essentially all the systemic antiinflammatory activity associated with aspirin in the carrageenin-induced rat paw edema test. Examination of the rat stomachs showed that the 1,3-didecanoyl derivative did not cause gastric lesions.

Animals↗
PubMed1979

Glycerides as prodrugs. 1. Synthesis and antiinflammatory activity of 1,3-bis(alkanoyl)-2-(O-acetylsalicyloyl)glycerides (aspirin triglycerides).

A series of 1,3-bis(alkanoyl)-2-(O-acetylsalicyloyl)glycerides (aspirin triglycerides) having aspirin at the 2 position of glycerol and fatty acids at the 1 and 3 positions was prepared. The compounds were administered orally and tested for efficacy in the rat paw edema test, and the stomachs were examined for the presence of lesions. The results showed that the members of this series in which the fatty acids are of intermediate chain length (C4-C12) do not cause gastric lesions and have essentially all the systemic activity associated with aspirin.

Animals↗