The derived QSAR models further validate the binding model of sulfonylurea compounds and AHAS, and provide a very useful tool in the next virtual screening.
Nine novel sulfonylurea compounds were synthesized． Their structures were confirmed by elemental analysis, IR and HNMR． The results of bioassay indicated that 〖2－(4－methylamino－6－isopropoxyl－2－triazinyl)aminocarbonylaminosulfonyl〗benzoic acid methyl ester showed good herbicidal activity．
Alkoxy group and fluorine atom were introduced onto the carbon chain of the substituent of the pyrimidine ring, and 12 novel sulfonylurea compounds with mono substituent in the pyrimidine ring were synthesized. The structures of all compounds were confirmed by 1 H NMR and elemental analysis.
Syntheses,Structure and SAR Study on Sulfonylurea Compounds(Ⅲ) ──Crystal and Molecular Structure of N-[2'-(4,6-dimethyl)pyrimidinyl]-2-ethyl Carboxylate-benzene Sulfonylurea
Syntheses, Structure and SAR Study on Sulfonylurea Compounds(Ⅴ)─Crystal and Molecular Structure of N-[2-(4-Ethyl)triazinyl]-2-nitrobenzene Sulfonylurea
Syntheses, Structures and SAR Study of Sulfonylurea Compounds(Ⅵ) --Crystal and Molecular Structure of N-〔2-(4-methyl)pyrimidinyl〕-2-Methylcarboxylate-benzyl sulfonylurea
Syntheses, Structure and SAR Study on Sulfonylurea Compounds( Ⅱ )——Crystal and Molecular Structure of N-[2-(4-methyl)pyrimdinyl]-2-ethyl carboxylate-benzene sulfonyiurea
Sytheses, Structure and SAR Study on New Sulfonylurea Compounds(Ⅰ)——Crystal and Molecular Structure of N-(2'-pyrimidinyl)-2-ethyl Carboxylate-benzene Sulfonyl urea
There are two parts in this paper, acute toxicity QSAR study of phenylsulfonyl carboxylate compounds and herbicidal activities QSAR study of sulfonylurea compounds.
The ten sulfonylurea compounds above mentioned were measured in fortified soil at(0.01-1.0) mg/kg levels. Average recoveries were in the range of(80.2%-104.5%) with relative standard deviations(RSDs) of(0.02%-14.9%).
Using the density functional theory method, the theoretical quantum chemical descriptors of twenty-three sulfonylurea compounds were calculated at B3LYP/6-31G(d) theoretical level.
2. Three synthetics were employed here for the synthesis of the different structural of sulfonylurea compounds by which the common intermediates can be made good use of.
Small and diverging effects were obtained with sulfonylurea compounds: whereas carbutamide caused slight stimulation, tolbutamide and glipizide had no effect, and glibenclamide was an inhibitor.
The technique of Sephadex gel filtration was employed to characterize the effect of some sulfonylurea compounds, ioglycamic acid, and suramin on the binding of phenprocoumon to bovine serum albumin.
Seventeen new sulfonylurea compounds were synthesized.Their structures were confirmed by elemental analysis,￣1HNMR,and IR,and their molecular and crystal structures were discussed. The data of their herbicidal activity were reported, and the structureactivity relationship(SAR)was studied accordingly.
13 sulfonylurea compounds were synthesized .among them 8 compounds are firstly re-ported. The structure of the compounds were confired by 1H NMR, 1R,MS and elemental analysis.Most of the compounds have herbicidal properties. Some of them have a good herbicidal activity.
The effects of glyburide and glipizide on insulin secretion were studied in pancreatic monolayer cultured β cells of neonatal rats by a perfusion system in TCM199 medium containing 16.7mmol/L glucose,0.4～1mmol/L glyburide or glipizide were added to stimulate insulin release in rnonolayer cells for a total of 7 days,Glyburide induced stronger response of B cells.In contrast,the peak of insulin release induced by glipizide was lower and appeared later than that of glyburide.The stimulatory effects of eith...
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