Incubation of hepatic microsomes from phenobarbital-treated rats with methyl 2-isopropyl-4-pentenoate results in rapid destruction of the microsomal cytochrome P-450. The destruction does not occur in the absence of NADPH or with methyl 2-isopropylpentanoate. Administration of methyl 2-isopropyl...
The reaction of carbanions α-to nitriles with tertiary bromoester 1 does not give cyclopropanes, whatever the reaction conditions, while Li enolate of methyl phenylacetate does, in THF or THF-Et2O. From lithiated aminonitriles 5, in THF-HMPA, the reaction leads to a mixture of SN and SN' p...
A novel series of 5,5-diaryl-2-amino-4-pentenoates was synthesized and found to be potent and selective glycine transporter type-2 reuptake inhibitors.
The reaction of Ru2Cl(μ-O2CMe)4 with trans-2-methyl-2-pentenoic acid affords the polymeric compound Ru2Cl(μ-O2CC (Me)CHEt)4 (1). This compound has polymeric structure in solid state, but is non-polymeric in solution. The reaction of 1 with OPPh3 in CH2Cl2 solution gives Ru2Cl(μ-O2CC(Me)CH...
Methyl 2-iodo-2-(phenylsulfonyl)-4-pentenoate (8)is reacted with N-BOC-allylamine to afford substituted 3-azabicyclo-[3.3.0]octanes (10) in a process which involves an initial iodine atom-transfer annulation followed by an ionic cyclization. The geminal carbomethoxy and phenylsulfonyl groups are...
Spirulina, Arthrospira platensis, contains high levels of protein and lutein. To evaluate nutritional, pigmentation, and antioxidation effects of A. platensis, a total of 900 juvenile yellow catfish (Pelteobagrus fulvidraco) were divided into 18 tanks (3 tanks/treatment, 50 fish/tank) and fed a ...
Food colorants are categorized into natural and synthetic dyes. One of the famous synthetic food dyes is Sunset Yellow FCF (E110) which belongs to the family of azo dyes and widely used in food industry. However, Sunset Yellow has positive and negative effects as well, by giving attractive physi...
The Yellow Sea coastline in East Asia, an important staging area for migratory shorebirds in the East Asian-Australasian Flyway (EAAF), is rapidly deteriorating. Conserving the declining shorebird populations that rely on the Yellow Sea requires habitat protection and management based on sound e...
The two crystal structures of 5-chloro-2-hydroxy-benzamide and 2-hydroxy-N,N-diethyl-benzamide were determined by X-ray diffraction at 100 K. The intramolecular and intermolecular hydrogen bonds were found in these structurally similar 2-hydroxy-benzamides. Analysis of the hydrogen bonding was c...
A series of 4-(1-substituted piperidin-4-yloxy) benzamides and 6-(1-substituted piperidin-4-yloxy)-3,4-dihydro-2H-isoquinolin-1-one derivatives have been synthesized and tested for their binding affinity towards H3 receptor. Most of these synthesized compounds have displayed potent binding affin...
A series of benzamide derivatives were assembled by using the privileged-fragment-merging (PFM) strategy and their SAR studies as glucokinase activators were described. Compounds 5 and 16b were identified having a suitable balance of potency and activation profile. They showed EC50 values of 28....
A novel series of hedgehog signaling pathway inhibitors has been designed based on the 4-(2-pyrimidinylamino) benzamides scaffold. The synthesis and SAR of these compounds are described. Optimization leads to the identification of compound 3c, a potent and orally available agent with improved ph...
The paper will describe the synthesis and SAR studies that led to the discovery of benzamide (reverse amide) as potent and selective human β3-adrenergic receptor agonist. Based on conformationally restricted pyrrolidine scaffold we discovered earlier, pyrrolidine benzoic acid intermediate 22 wa...
Five new compounds including three dimeric chromanones (1–3), one cyclohexenone (4) and one benzamide (5), together with four known metabolites, were isolated from the endophytic fungus Xylaria sp. PSU-H182. Their structures were determined by analysis of their spectroscopic data, and the absol...
Optically active axially chiral 2,6-disubstituted benzamides and anilides were stereoselectively prepared by utilizing planar chiral (arene)chromium complexes. Nucleophilic addition to enantiomerically pure planar chiral tricarbonyl(N,N-diethyl-2-methyl-6-formyl- (or 6-acyl)benzamide)chromium co...
A SAR study was performed on 3-substituted 2,6-difluorobenzamides, known inhibitors of the essential bacterial cell division protein FtsZ, through a series of modifications first of 2,6-difluoro-3-nonyloxybenzamide and then of its 3-pyridothiazolylmethoxy analogue PC190723. The study led to the ...
A series of fluorine substituted benzamides 1–10 was synthesised and investigated by spectroscopic methods (NMR, IR, MS) and X-ray structure analysis. The configuration of these compounds strongly depends on solvent, temperature and substitution pattern. Unexpectedly, some of these compounds fo...
SAR exploration of the central diamine, benzyl, and terminal aminoalkoxy regions of the N-cyclic azaalkyl benzamide series led to the identification of very potent human urotensin-II receptor antagonists such as 1a with a Ki of 4 nM. The synthesis and structure–activity relationships (SAR) of N...
A new, convenient, one-pot process is presented for the synthesis of 2-oxazolines in high yields (75–94%) via boron esters of N-(2-hydroxyethyl) amides. The procedure involves thermolysis of the boron esters at 240–260 °C, in the presence of solid CaO as an acid scavenger and allows the prepa...
Acid sphingomyelinase (ASM) has been shown to be involved in many physiological processes, emerging to be a promising drug target. In this study, we constructed a ligand-based pharmacophore model of ASM inhibitors and applied this model to optimize the lead compound α-mangostin, a known inhibit...
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