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Paradoxical inhibitory effect of cromakalim on 86Rb outflow from pancreatic islet cells.
The present data suggest that the paradoxical inhibitory effect of cromakalim on 86Rb outflow probably reflects the capacity of the drug to reduce the activity of the ATP-sensitive K+ channels and to indirectly inhibit the Ca+(+)-activated K- channels. Expand
Similarities between the effects of pinacidil and diazoxide on ionic and secretory events in rat pancreatic islets.
Pinacidil could interfere with the same target site as diazoxide; namely the beta-cell ATP-sensitive K+ channel, as well as stimulate an ouabain-resistant modality of 86Rb inflow into the islet cells. Expand
Synthesis and biological evaluation of cyclopropyl analogues of fosmidomycin as potent Plasmodium falciparum growth inhibitors.
A series of fosmidomycin analogues featuring restricted conformational mobility has been synthesized and evaluated as inhibitors of 1-deoxy-D-xylulose 5-phosphate (DOXP) reductoisomerase and asExpand
Pinacidil inhibits insulin release by increasing K+ outflow from pancreatic B-cells.
Results represent the first indication of an effect ofPinacidil on ionic and secretory events in endocrine cells and suggest that, in pancreatic islet cells, pinacidil could affect ATP-sensitive K+ channels. Expand
Divergent strategy for the synthesis of α-aryl-substituted fosmidomycin analogues
Fosmidomycin is the first representative of a new class of antimalarial drugs acting through inhibition of 1-deoxy-D-xylulose 5-phosphate ( DOXP) reductoisomerase (DXR), an essential enzyme in theExpand
Synthesis and evaluation of α,β-unsaturated α-aryl-substituted fosmidomycin analogues as DXR inhibitors
Abstract Fosmidomycin, which acts through inhibition of 1-deoxy- d -xylulose phosphate reductoisomerase (DXR) in the non-mevalonate pathway, represents a valuable recent addition to the armamentariumExpand
Divergent strategy for the synthesis of alpha-aryl-substituted fosmidomycin analogues.
This work describes a divergent strategy for the synthesis of a series of alpha-aryl-substituted fosmidomycin analogues, featuring a palladium-catalyzed Stille coupling as the key step and an alpha-(4-cyanophenyl)fosMidomycin analogue emerged as the most potent analogue in the present series. Expand
Synthesis and evaluation of alpha,beta-unsaturated alpha-aryl-substituted fosmidomycin analogues as DXR inhibitors.
This paper describes the synthesis and biological evaluation of E- and Z-alpha,beta-unsaturated alpha-aryl-substituted analogues of FR900098, a fosmidomycin congener, utilizing a Stille or a Suzuki coupling to introduce the aryl group. Expand
Effect of a new xanthine derivative on the release of insulin from rat pancreatic islets.
Data show that S 9795 inhibits glucose-induced insulin release, possibly by blocking glucose-stimulated Ca2+ inflow into the B-cell. Expand
From pigments to coloured napkins: comparative analyses of primary aromatic amines in cold water extracts of printed tissues by LC-HRMS and LC-MS/MS
The comparison between pigment analysis and CWE results shows that if the pigment purity profile is of major importance, other parameters such as pigment surface treatment, ink grinding process or ink formulation could have an important influence on the C THE AUTHORS results. Expand