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At least 289 records · Page 16Linked to original sources
PubMed1992

Gamma-pyrone compounds. II: Synthesis and antiplatelet effects of tetraoxygenated xanthones.

Norathyriol and its analogues, 1,3,5,6-, 3,4,5,6-, 3,4,6,7- and 2,3,6,7-tetrahydroxyxanthone, were synthesized from benzophenone precursors by Friedel-Crafts acylation and subsequent base-catalyzed cyclization to eliminate methanol. Both 3,4,6,7- and 2,3,6,7-tetrahydroxyxanthone tetraacetate showed potent anti-platelet aggregation effects on arachidonic acid-induced platelet aggregation. 3,4,6,7-Tetrahydroxyxanthone tetraacetate and 1,3,5,6-tetrahydroxyxanthone showed potent and significant anti-platelet aggregation effects on collagen-induced platelet aggregation.

Adenosine Diphosphate↗
PubMed1993

gamma-Pyrone compounds. IV: Synthesis and antiplatelet effects of mono- and dioxygenated xanthones and xanthonoxypropanolamine.

Xanthodilol, mono- and dioxygenated xanthones, and 1,3-, 2,3-, 3,4-, 3,5-, 1,6-, 2,6- and 3,6-dioxygenated xanthones were synthesized from benzophenone precursors by Friedel-Crafts acylation and subsequent base-catalyzed cyclization to eliminate methanol. 3-Hydroxy-xanthone, xanthodilol, 2,3-dihydroxyxanthone diacetate, and 3,4-dihydroxyxanthone and its diacetate showed potent antiplatelet effects on arachidonate- and collagen-induced aggregation. 3,5-Dihydroxyxanthone and its diacetate, 1,6-dimethoxyxanthone, and 3,6-dihydroxyxanthone and its diacetate showed potent antiplatelet effects on arachidonate-induced aggregation.

Adenosine Diphosphate↗
PubMed1994

gamma-Pyrone compounds. 5. Synthesis and antiplatelet effects of xanthonoxypropanolamines and related compounds.

A series of simple xanthonoxypropanolamines and related compounds were synthesized. 3-[3-(Cyclopropylamino)propoxy]-xanthone showed same potent antiplatelet effects as norathyriol tetraacetate on arachidonate-induced aggregation. 3-[3-(Cyclohexylamino)-2-hydroxypropoxy]xanthone showed more potent antiplatelet effects than norathyriol tetraacetate on collagen-induced aggregation. The various amino groups of the oxypropanolamine or oxypropylamine side chains of the synthesized compounds regulated the antiplatelet effects.

Animals↗
PubMed1986

The effect of coumarin (5,6 benzo-alpha-pyrone) on elicited members of the mononuclear system in dogs with chronic secondary lymphedema.

The effect of coumarin is investigated on the morphological features of members of the mononuclear phagocytic system (MPS) attaching to subcutaneously (s.c.) implanted coverslips in "normal" and chronically lymphedematous tissues. In untreated "normal" tissues there was no attachment suggesting that the presence of lymphedema elsewhere influences MPS activity. Coumarin restored attachment proportions to those found in normal tissues of dogs with no lymphedema. In lymphedema, coumarin significantly increased the proportion of macrophages which were round with less than ten pseudopods (new recruits) and the proportion with distinct pseudopods combined with more than ten vacuoles (active elicited members of the MPS). Coumarin resulted in a significant decline in the proportion of macrophages which were round and with more than ten apparently lipid-containing vacuoles, suggesting a facilitation of their removal to other sites.

Animals↗
PubMed1988

A double-blind, cross-over trial of O-(beta-hydroxyethyl)-rutosides (benzo-pyrones) in the treatment of lymphoedema of the arms and legs.

A randomised, double-blind, cross-over trial was performed on 26 patients with postmastectomy lymphoedema of the arm, and 14 with lymphoedema of the leg. For 6 months, patients took 0-(beta-hydroxyethyl)-rutosides (oxerutin; "Paroven", "Venoruton", Zyma) in doses of 3 g/day, or the placebos; then they took the reverse. Measurements (volume, circumferences, tonometry and skin temperature) were made monthly. The active drug reduced the volumes of the limbs (p less than 0.05 to 0.01) and their circumferences (p less than 0.05 to 0.001). It increased the softness of the limbs, as shown by the increases in the tonometry values (p less than 0.01 to 0.001). There was a lowering of the elevated skin temperatures (p less than 0.05 to 0.001). Patients reported increased comfort and freedom of movement, a lessening of their bursting pains, heaviness and tension (p less than 0.05 to 0.01), and an increased mobility of their limbs (p less than 0.0001). Most patients (70%) preferred the active drug (p less than 0.0001). An increase in general well-being was reported by 97% of patients when taking the active drug compared with 4% for placebo (p less than 0.0001).

Arm↗
PubMed2006

Racemic and chiral sulfoxides as potential prodrugs of 4-pyrone COX-2 inhibitors.

The preparation of the sulfoxide analogues 7, 8, and 9 and their enantiomerically pure forms is discussed as well as their ability to act as prodrugs of the potent and selective sulfone-containing COX-2 inhibitors 1, 2, and 3. Sulfoxide derivatives 7 and 9 were shown to be rapidly transformed in vivo into the corresponding sulfone derivatives 1 and 3, after oral administration to rats.

Animals↗