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关键词:'oxazoles'
显示 1-30 共 1138 条结果 关于 "oxazoles" 范围 论文
Lulu Chen et al.
Applied microbiology and biotechnology, 100(2), 857-867 (2015-11-04)
Dental caries, a biofilm-related oral disease, is a result of disruption of the microbial ecological balance in the oral environment. Streptococcus mutans, which is one of the primary cariogenic bacteria, produces glucosyltransferases (Gtfs) that synthesize extracellular polysaccharides (EPSs). The EPSs
Jie Zhou et al.
European journal of medicinal chemistry, 68, 222-232 (2013-08-29)
A series of novel oxazole-bridged analogs of combretastatin A-4 bearing a benzo[d]-imidazole as B ring were synthesized and evaluated for antiproliferative activities against five human cancer cell lines. Among all the synthesized compounds, the N-unsubstituted benzoimidazole analog 5 and the
Daniel J Pippel et al.
The Journal of organic chemistry, 72(15), 5828-5831 (2007-06-26)
Treatment of oxazole or 5-aryl oxazoles with i-PrMgCl smoothly generates the corresponding 2-Grignard reagents, which react with Weinreb amides to provide exclusively 2-acyl oxazole products.
A J Phillips et al.
Organic letters, 2(8), 1165-1168 (2000-05-11)
[formula: see text] A mild and highly efficient cyclization of beta-hydroxy amides to oxazolines is described using DAST and Deoxo-Fluor reagents. A one-pot protocol for the synthesis of oxazoles from beta-hydroxy amides is also presented.
Shankar S Iyer et al.
Cell, 173(5), 1123-1134 (2018-05-19)
Genome-wide association studies have identified risk loci associated with the development of inflammatory bowel disease, while epidemiological studies have emphasized that pathogenesis likely involves host interactions with environmental elements whose source and structure need to be defined. Here, we identify
Haseen Ahmad et al.
European journal of medicinal chemistry, 208, 112759-112759 (2020-09-05)
Oxazole derivatives are important medicinal compounds which are inhibitors of various enzymes such as NPP1, NPP2, NPP3, tyrosine kinase, dipeptidyl-peptidase IV, cyclooxygenase-2, and protein tyrosine phosphatase. In this study, an extensive range of new biologically active biphenyl oxazole derivatives was
David A Evans et al.
Organic letters, 8(24), 5669-5671 (2006-11-17)
The ceric ammonium nitrate promoted oxidations of 4,5-diphenyloxazoles and oxazoles with various substitution patterns have been investigated. This transformation results in the formation of the corresponding imide in good yield and tolerates a wide variety of functional groups and substituents
James R Davies et al.
The Journal of organic chemistry, 70(18), 7305-7316 (2005-08-27)
[structure: see text] Various approaches to the indole bis-oxazole fragment of the marine secondary metabolite diazonamide A are described, all of which feature dirhodium(II)-catalyzed reactions of diazocarbonyl compounds in key steps. Thus, 3-bromophenylacetaldehyde is converted into an alpha-diazo-beta-ketoester, dirhodium(II)-catalyzed reaction
Gopal Chandru Senadi et al.
Organic letters, 14(17), 4478-4481 (2012-08-11)
An expedient method for a direct approach to the selective and regiocontrolled synthesis of 2-oxazolines and 2-oxazoles mediated by ZnI(2) and FeCl(3) is described. A Lewis acid promoted cyclization of acetylenic amide with various functionalities was well tolerated to give
Chung-Kyu Ryu et al.
Bioorganic & medicinal chemistry letters, 19(20), 5924-5926 (2009-09-08)
Benzo[d]oxazole-4,7-diones were synthesized and tested for in vitro antifungal activity against fungi. Among them tested, many compounds showed good antifungal activity. The results suggest that benzo[d]oxazole-4,7-diones would be potent antifungal agents.
E Vedejs et al.
The Journal of organic chemistry, 65(18), 5498-5505 (2000-09-02)
Intermolecular alkylation of the aziridinyl oxazole 20 using PhSO(2)CH(2)CH(2)OTf is possible despite the presence of potentially nucleophilic aziridine nitrogen. The resulting oxazolium salt 22 reacts with BnNMe(3)(+)CN(-) to produce the azomethine ylide 24b via electrocyclic ring opening of an oxazoline
Zhong Jin
Natural product reports, 28(6), 1143-1191 (2011-04-08)
A great number of structurally diverse natural products containing five-membered heterocyclic subunits, such as imidazole, oxazole, thiazole, and their saturated congeners, are abundant in nature. These naturally occurring metabolites often exhibit extensive and pharmacologically important biological activities. The latest progress
Synthesis of 3-pyridinols. I. Reaction of 5-unsubstituted oxazoles with acrylonitrile.
T Naito et al.
Chemical & pharmaceutical bulletin, 13(7), 869-872 (1965-07-01)
Mark J Thompson et al.
The Journal of organic chemistry, 74(10), 3856-3865 (2009-04-21)
A highly versatile route to oxazole-5-amides is presented. Conversion of readily accessible oxazole-5-trifluoroacetamides into their Boc-protected 5-aminooxazole derivatives provides intermediates amenable to parallel amide synthesis utilizing a reliable, one-pot, acylation-deprotection procedure. During preparation of the N-Boc compounds from trifluoroacetamides, a
Garrett C Moraski et al.
Bioorganic & medicinal chemistry, 20(7), 2214-2220 (2012-03-07)
Tuberculosis (TB) is a devastating disease resulting in a death every 20s. Thus, new drugs are urgently needed. Herein we report ten classes of compounds-oxazoline, oxazole, thiazoline, thiazole, pyrazole, pyridine, isoxazole, imidazo[1,2-a]pyridine, imidazo[1,2-a]pyrimidine and imidazo[1,2-c]pyrimidine-which have good (micromolar) to excellent
Cécile Verrier et al.
Organic & biomolecular chemistry, 9(18), 6215-6218 (2011-07-29)
Sequential palladium-catalysed direct (het)arylation of oxazole-4-carboxylates is achieved to give rapid access to DPO and POPOP (di)carboxylate-analogs. Three novel DPO- and POPOP-type sensors with unusual Stokes shifts and high quantum yields are discovered.
Chi Wai Cheung et al.
The Journal of organic chemistry, 77(17), 7526-7537 (2012-07-31)
A copper(II)-catalyzed oxidative cyclization of enamides to oxazoles via vinylic C-H bond functionalization at room temperature is described. Various 2,5-disubstituted oxazoles bearing aryl, vinyl, alkyl, and heteroaryl substituents could be synthesized in moderate to high yields. This reaction protocol is
Carbonates: ecofriendly solvents for palladium-catalyzed direct 2-arylation of oxazole derivatives.
Julien Roger et al.
ChemSusChem, 2(10), 951-956 (2009-10-07)
Javier Mazuela et al.
Organic & biomolecular chemistry, 9(3), 941-946 (2010-12-15)
We describe the application of a new class of ligands--the phosphite-oxazole/imidazole (L1-L5a-g)--in asymmetric intermolecular Pd-catalyzed Heck reactions under thermal and microwave conditions. These ligands combine the advantages of the oxazole/imidazole moiety with those of the phosphite moiety: they are more
Horacio A Priestap et al.
Journal of natural products, 75(7), 1414-1418 (2012-07-04)
2-Methylnaphtho[1,2-d]oxazole-9-carboxylic acid was obtained by reduction of 8-nitro-1-naphthoic acid with zinc-acetic acid. This naphthoxazole is a condensation product between an 8-nitro-1-naphthoic acid reduction intermediate and acetic acid and is a lower homologue of aristoxazole, a similar condensation product of aristolochic
Wei-Jian Xue et al.
Chemical communications (Cambridge, England), 48(29), 3485-3487 (2012-01-31)
A highly efficient method for the synthesis of oxazole derivatives from methyl ketones, benzoins and ammonium acetate has been established via a novel strategy-convergent integration of two self-labor domino sequences. Owing to the simple and readily available starting materials, mild
Diana Haas et al.
Organic letters, 15(24), 6162-6165 (2013-11-20)
A general method for the synthesis of 2,4,5-trisubstituted oxazoles has been developed. Starting from commercially available oxazole, successive metalations using TMPMgCl·LiCl or TMPZnCl·LiCl led to the corresponding magnesiated or zincated species which were stable toward ring fragmentation. Furthermore, they readily
Hikaru Fujita et al.
Chemical & pharmaceutical bulletin, 60(7), 907-912 (2012-07-14)
A method for one-pot synthesis of oxazol-5(4H)-ones has been developed using 4-(4,6-dimethoxy-1,3,5-triazin-2-yl)-4-methylmorpholinium chloride (DMT-MM), which is available for the activation of carboxylic acids in an aqueous solvent. The oxazolones were prepared by the N-acylation of amino acids with carboxylic acids
Akio Saito et al.
Molecules (Basel, Switzerland), 17(9), 11046-11055 (2012-09-15)
In the presence of trifluoromethanesulfonic acid (TfOH) or bis(trifluoromethane-sulfonyl)imide (Tf₂NH), iodosobenzene (PhI=O) efficiently promoted the reactions of dicarbonyl compounds as well as monocarbonyl compounds with nitriles to give 2,4-disubstituted and 2,4,5-trisubstituted oxazole in a single step under the mild conditions.
Nayyef Aljaar et al.
The Journal of organic chemistry, 78(1), 154-166 (2012-11-28)
Reactions between 1-nitroso-2-naphthols and α-functionalized ketones such as α-bromo-, α-chloro-, α-mesyloxy-, α-tosyloxy-, and α-hydroxy ketones under basic conditions delivered 2-substituted naphtho[1,2-d][1,3]oxazoles in a single synthetic operation. The product formation was accompanied by the unexpected loss of the C═O group from
Yuri Yamazaki et al.
Bioorganic & medicinal chemistry, 19(1), 595-602 (2010-11-26)
A new bioactive photoaffinity probe KPU-252-B1 (4) possessing a biotin tag on the oxazole ring of a potent plinabulin derivative KPU-244 (2) was synthesized via the Cu(I)-catalyzed Huisgen's cycloaddition reaction to understand the precise binding mode of the diketopiperazine-based anti-microtubule
Hirofumi Sasaki et al.
Journal of medicinal chemistry, 49(26), 7854-7860 (2006-12-22)
In an effort to develop potent new antituberculosis agents that would be effective against both drug-susceptible and drug-resistant strains of Mycobacterium tuberculosis, we prepared a novel series of optically active 6-nitro-2,3-dihydroimidazo[2,1-b]oxazoles substituted at the 2-position with various phenoxymethyl groups and
Daniele Zampieri et al.
Journal of medicinal chemistry, 52(17), 5380-5393 (2009-08-14)
Novel benzo[d]oxazol-2(3H)-one derivatives were designed and synthesized, and their affinities against sigma receptors were evaluated. On the basis of 31 compounds, a three-dimensional pharmacophore model for the sigma(1) receptor binding site was developed using the Catalyst 4.9 software package. The
Alexander G Godfrey et al.
The Journal of organic chemistry, 68(7), 2623-2632 (2003-03-29)
An improved method for the preparation of a series of oxazole-containing dual PPARalpha/gamma agonists is described. A synthetic sequence utilizing a Dakin-West reaction was devised that allows for the introduction of the oxazole ring either late in the synthetic sequence
Johanna Senger et al.
Journal of medicinal chemistry, 59(4), 1545-1555 (2015-12-15)
Histone deacetylase 6 (HDAC6) catalyzes the removal of an acetyl group from lysine residues of several non-histone proteins. Here we report the preparation of thiazole-, oxazole-, and oxadiazole-containing biarylhydroxamic acids by a short synthetic procedure. We identified them as selective
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