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Development and validation of a nonaqueous capillary electrophoretic method for the enantiomeric purity determination of a synthetic intermediate of new 3,4-dihydro-2,2-dimethyl-2H-1-benzopyrans
TLDR
The enantiomeric purity determination of a synthetic intermediate of new 3,4-dihydro-2,2-dimethyl-2H-1-benzopyrans was successfully carried out using an anionic cyclodextrin (CD) derivative combined with a chiral ionic liquid (IL). Expand
Synthesis and activity on rat aorta rings and rat pancreatic beta-cells of ring-opened analogues of benzopyran-type potassium channel activators.
Ring-opened analogues of dihydrobenzopyran potassium channel openers (PCOs) were prepared and evaluated as putative PCOs on rat aorta rings (myorelaxant effect) and rat pancreatic beta-cellsExpand
Modulation of the 6-position of benzopyran derivatives and inhibitory effects on the insulin releasing process.
TLDR
Structural-activity relationships indicated that the inhibitory effect on the insulin secreting cells was related to the lipophilicity of the molecules and to the size of the substituent located at the 6-position. Expand
Design, synthesis, and pharmacological evaluation of R/S-3,4-dihydro-2,2-dimethyl- 6-halo-4-(phenylaminocarbonylamino)-2H-1-benzopyrans: toward tissue-selective pancreatic beta-cell KATP channel
TLDR
Radioisotopic and electrophysiological investigations performed with R/S-6-chloro-4-(3-chlorophenylaminocarbonylamino)-3,4-dihydro-2,2-dimethyl-2H-1-benzopyran confirmed that the drug activated pancreatic KATP channels. Expand
New R/S-3,4-dihydro-2,2-dimethyl-6-halo-4-(phenylaminothiocarbonylamino)-2H-1-benzopyrans structurally related to (+/-)-cromakalim as tissue-selective pancreatic beta-cell K(ATP) channel openers.
TLDR
Radioisotopic and fluorimetric investigations indicated that the new drugs activated pancreatic K(ATP) channels and conformational studies suggested that the urea/thiourea dimethylchromans can be regarded as hybrid compounds between cromakalim and pinacidil. Expand
New R/S-3,4-dihydro-2,2-dimethyl-2H-1-benzopyrans as K(ATP) channel openers: modulation of the 4-position.
TLDR
Exploring a series of diversely 4-arylthiourea-substituted R/S-3,4-dihydro-2,2-dimethyl-6-halo-2H-1-benzopyrans structurally related to (+/-)-cromakalim indicated that these new compounds activated pancreatic K(ATP) channels. Expand
Chloro-substituted 3-alkylamino-4H-1,2,4-benzothiadiazine 1,1-dioxides as ATP-sensitive potassium channel activators: impact of the position of the chlorine atom on the aromatic ring on activity and
TLDR
6-chloro-3-alkylamino/cycloalkylaminos-4H-1,2,4-benzothiadiazine 1,1-dioxides appear to be more attractive than their previously described 7- chloro-substituted analogues as original drugs activating the SUR1/Kir6.2 K(ATP) channels. Expand
Design and synthesis of new potassium channel activators derived from the ring opening of diazoxide: study of their vasodilatory effect, stimulation of elastin synthesis and inhibitory effect on
TLDR
Most of the active vasorelaxant drugs, except 15k and 15t at high concentrations, did not exhibit marked inhibitory effects on the insulin releasing process and on glycaemia, suggesting a relative tissue selectivity of some of these compounds for the vascular smooth muscle. Expand
1,4,2-Benzo/pyridodithiazine 1,1-dioxides structurally related to the ATP-sensitive potassium channel openers 1,2,4-Benzo/pyridothiadiazine 1,1-dioxides exert a myorelaxant activity linked to a
TLDR
The present work highlights the critical importance of an intracyclic NH group at the 4-position, as well as an exocyclicNH group linked to the 3-position of the benzo- and pyridothiadiazine dioxides, for activity on KATP channels. Expand
4-Phenylureido/thioureido-substituted 2,2-dimethylchroman analogs of cromakalim bearing a bulky 'carbamate' moiety at the 6-position as potent inhibitors of glucose-sensitive insulin secretion.
TLDR
Radioisotopic, fluorimetric and pharmacological investigations were performed on rat pancreatic islet and rat vascular smooth muscle cells in order to decipher its mechanism of action, and it is suggested that the mechanism ofaction of 14o is rather unspecific. Expand
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