Ureas sulfonyl

Glipi de. GHpi2ide (l-cyclohexyl-3[ -[2-(5-methylpyra2inecarboxamido)eth5l]phenyl]sulfonyl]urea), mol wt 445.55, forms crystals from ethanol, mp 208—209°C. It is known commercially as Glucotrol. 

Sulfaphenazole (684) and sulfazamet (685) are both examples of relatively short acting sulfonamides (B-80MI40406) and their antibacterial activity has been tested against Escherichia coli, the former being more effective than the latter. Sulfaphenazole also displaces sulfonyl ureas from protein binding sites on human serum albumin and consequently increases the concentration of the free (active) drug and produces a more intense reaction that may result in hypoglycemia. 

This sulfonyl urea, prepared from an amino acid and p-tosyl isocyanate in 20-80% yield, is cleaved by alcohols (95% aq. EtOH, n-PrOH, or -BuOH, 100°, 1 h, 95% yield). It is stable to dilute base, to acids (HBr/AcOH or cold CF3CO2H), and to hydrazine. ... 

Endo-amlnoborneol HCI o-Methyl-N-p-toluene sulfonyl urea... 

Chemical Name 1-cyclohexyl-3-[ [p-[2-(5-methylpyrazinecarboxamido)ethyl] phenyl] -sulfonyl] urea... 

Alcohol or substances with disulfiram effect (e.g. mushrooms, griseofulvin,sulfonyl urea)... 

The sulfonyl urea sulfometuron methyl is stable at neutral or alkaline pH values, but is hydrolyzed at pH 5 to methyl 2-aminosulfonylbenzoate that is cyclized to saccharin (Figure 1.21) (Harvey et al. 1985). The original compound is completely degraded to CO2 by photolysis. 

The method based on immunosorbents coupled on-line with liquid chromatography-atmospheric pressure chemical ionization mass spectrometry [109], discussed in section 9.4.2.1, has been applied to the determination of substituted urea type herbicides. Supercritical fluid extraction with methanol modified carbon dioxide has been applied to the determinants of sulfonyl urea herbicides in soil [261],... 

The Ar-(3-cyclopropyl-2,4-pyrimidyl)- 96a and hT-(3-cydopropyl-2,4,6-tri-azinyl)-AT-aryl sulfonyl ureas 96b (R = halo-, amino-, alkoxyalkyl and cycloalkyl X = CH, N) are useful as plant growth regulators and herbicides. At 500 g per ha the cyclopropyltriazine derivative 96 b (R = OMe, Ar = 2-carbomethoxy-phenyl) killed Abutilon species and Sivapis alba or prevented germination without affecting wheat, Eq. (37) [128]. 

Reaction of 274 with 2-thiophenesulfonyl chloride gave 275 (86EUP 150974) and with p-toluenesulfonyl isocyanate gave the sulfonyl urea 276... 

Health and Safety Factors. Malononiirilc is usually available as a solidified melt in plastic-lined drums. Remclting has to he done carefully because spontaneous decomposition can occur at elevated temperatures, particularly above lOO C. in the presence of impurities such as alkalies, ammonium, and zinc sails. Occupational exposure to malononitrile mainly occurs by inhalation of vapors and absorption through the skin. Malononitrile has a recommended workplace exposure limn of 8 mg/m Uses. Malononitrile is extensively used in the life sciences industry The most important products ate vitamin B (thiamine) and bensulfuron-melhyl. a sulfonyl urea herbicide. Most other product uses fall under the. V-containing heterocycles. 

What are the criteria for regarding a compound as a TS analog The observation that the binding affinity of an inhibitor is greater than that of a substrate, i.e., X, < XM, is insufficient as many potent inhibitors bind differently to an enzyme than the substrate examples are methotraxate, inhibiting dihydrofolate reductase (DHFR) X] = 0.15 pM (Werkheiser, 1961), and sulfonyl urea herbicides, inhibiting acetolactate synthase (ALS) at picomolar levels. 

Sulfonylurea herbicides and metabolites C02-methanol Using Ci8 solid phase extraction disk High-performance liquid chromatography with UV detection. Dimethyl sulfonyl ureas determined by GC with detection by electron capture or N-P or MS. [162,163]... 

Sulfonylureas bind to a 140 kDa high-affinity sulfonyl-urea receptor that is associated with a B cell inward rectifier ATP-sensitive potassium channel. Binding of a sulfonylurea inhibits the efflux of potassium ions through the channel (Figure 41-2) and results in depolarization. Depolarization, in turn, opens a voltage-gated calcium channel and results in calcium influx and the release of preformed insulin. 

Acarbose is a glucopyranose derivative that acts by inhibiting intestinal a-gluco-sidase. This delays carbohydrate absorption and reduces the postprandial (1.5 hours after food) blood glucose levels and is used in combination with other sulfonyl-ureas. Acarbose may cause GI disturbances, flatulence, abdominal distortion, diarrhea, and pain. Acarbose should be avoided during pregnancy, as it affects the fetus. Acarbose is contraindicated in inflammatory bowel disease and hepatic dysfunction. 

Uses herbicide, oilseed rape Trade names Muster (DuPont) Type sulfonyl urea... 

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