Category: 16251-45-9

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(Matrix presented) This report describes a modular approach to the synthesis of stereodiversified natural product-like libraries. Monomers 2 and 3 were coupled in parallel by silyl-tethered olefin metathesis to generate all 16 stereoisomers of cis-enediols 1. All 16 stereoisomers were incorporated into chimerae having flanking peptidic segments. These chimerae exhibited a broad range of hydrophobicities, raising the possibility that stereochemical variation might be used to tune the pharmacologic properties of small molecules.

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Oxazolidine – Wikipedia,
Oxazolidine | C3H2159NO – PubChem

Chemistry can be defined as the study of matter and the changes it undergoes. Related Products of 16251-45-9. You’ll sometimes hear it called the central science because it is the connection between physics and all the other sciences, starting with biology.Related Products of 16251-45-9, Name is (4S,5R)-4-Methyl-5-phenyloxazolidin-2-one, molecular formula is C10H11NO2, introducing its new discovery.

Thrombin inhibitors are potentially useful in medicine for their anticoagulant and antithrombotic effects. We synthesized and evaluated diverse heterocycle-activated ketones based on the D-Phe-Pro-Arg, and related thrombin active-site recognition motifs, as candidate inhibitors. The peptide-based alpha-ketoheterocycles were typically prepared by either an imidate or a Weinreb amide route (Schemes 1 and 2), the latter of which proved to be more general. Test compounds were generally assayed for inhibition of human alpha-thrombin and bovine trypsin. From a structure-based design standpoint, the heterocycle allows one to explore and adjust interactions within the S1? subsite of thrombin. The preferred alpha-ketoheterocycle is a pi-rich 2-substituted azole with at least two heteroatoms proximal to the carbon bearing the keto group, and a preferred thrombin inhibitor is 2-ketobenzothiazole 3, with a potent Ki value of 0.2 nM and ca. 15-fold selectivity over trypsin. 2-Ketobenzothiazole 13 exhibited exceedingly potent thrombin inhibition (Ki = 0.000 65 nM; slow tight binding). Several alpha-ketoheterocycles had thrombin Ki values in the range 0.1-400 nM. The “Arg” unit in the alpha-ketoheterocycles can be sensitive to stereomutation under mildy basic conditions. For example, 2-ketothiazoles 4 and 59 readily epimerize at pH 7.4, although they are fairly stable stereochemically at pH 3-4; thus, suitable conditions had to be selected for the enzymatic assays. Lead D-Phe-Pro-Arg 2-benzothiazoles 3, 4, and 68 displayed good selectivity for thrombin over other key coagulation enzymes (e.g., factor Xa, plasmin, protein Ca, uPA, tPA, and streptokinase); however, their selectivity for thrombin over trypsin was modest (<25-fold). Compounds 3, 4, and 68 exhibited potent in vitro antithrombotic activity as measured by inhibition of gel-filtered platelet aggregation induced by alpha-thrombin (IC50 = 30-40 nM). They also proved to be potent anticoagulant/ antithrombotic agents in vivo on intravenous administration, as determined in the canine arteriovenous shunt (ED50 = 0.45-0.65 mg/kg) and the rabbit deep vein thrombosis (ED50 = 0.1-0.4 mg/kg) models. Intravenous administration of 3, and several analogues, to guinea pigs caused hypotension and electrocardiogram abnormalities. Such cardiovascular side effects were also observed with some nonguanidine inhibitors and inhibitors having recognition motifs other than D-Phe-Pro-Arg. 2-Benzothiazolecarboxylates 4 and 68 exhibited significantly diminished cardiovascular side effects, and benzothiazolecarboxylic acid 4 had the best profile with respect to therapeutic index. The X-ray crystal structures of the ternary complexes 3-thrombin-hirugen and 4-thrombin-hirugen depict novel interactions in the S1? region, with the benzothiazole ring forming a hydrogen bond with His-57 and an aromatic stacking interaction with Trp-60D of thrombin's insertion loop. The benzothiazole ring of 3 displaces the Lys-60F side chain into a U-shaped gauche conformation, whereas the benzothiazole carboxylate of 4 forms a salt bridge with the side chain of Lys-60F such that it adopts an extended anti conformation. Since 3 has a 10-fold greater affinity for thrombin than does 4, any increase in binding energy resulting from this salt bridge is apparently offset by perturbations across the enzyme (viz. Figure 4). The increased affinity and selectivity of 2-ketobenzothiazole inhibitors, such as 3, may be primarily due to the aromatic stacking interaction with Trp-60D. However, energy contour calculations with the computer program GRID also indicate a favorable interaction between the benzothiazole sulfur atom and a hydrophobic patch on the surface of thrombin. By the way, if you are interested in learning more fun chemistry with your kids, get your hands into one chemistry set now, and start enjoying the best part of chemistry: experiments about 16251-45-9Related Products of 16251-45-9

Reference：
Oxazolidine – Wikipedia,
Oxazolidine | C3H2153NO – PubChem

16251-45-9, The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.16251-45-9, Name is (4S,5R)-4-Methyl-5-phenyloxazolidin-2-one, molecular formula is C10H11NO2. In a Patent，once mentioned of 16251-45-9

Methods are disclosed to reduce apolipoprotein C-III (apoC-III) mRNA or protein in a subject in need thereof, comprising administering a pharmaceutically effective amount of a compound of Formula (I), or a pharmaceutically acceptable salt or ester thereof, wherein R1 and R2 are independently chosen from a hydrogen atom or linear, branched, and/or cyclic C1-C6 alkyl groups, with the proviso that R1 and R2 are not both hydrogen.

The design and synthesis of related molecules that are more effective, more selective, and less toxic than aspirin are important objectives of biomedical research.Keep reading other articles of 16251-45-916251-45-9

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Oxazolidine – Wikipedia,
Oxazolidine | C3H2113NO – PubChem

Chemistry can be defined as the study of matter and the changes it undergoes. SDS of cas: 16251-45-9. You’ll sometimes hear it called the central science because it is the connection between physics and all the other sciences, starting with biology.SDS of cas: 16251-45-9, Name is (4S,5R)-4-Methyl-5-phenyloxazolidin-2-one, molecular formula is C10H11NO2, introducing its new discovery.

Two efficient routes have been established for the preparation of both enantiomers of cis-(2-aminocyclobutyl)acetic acid, a conformationally restricted analogue of GABA. Both procedures converged on the racemic N-tert-butoxycarbonyl derivative of the target compound, which was resolved through chiral derivatization with an oxazolidinone auxiliary, which also allowed determination of the absolute configuration of the new compounds. The first route involved the homologation of cis-2-aminocyclobutanecarboxylic acid, whereas the second route employed an intramolecular photocyclization protocol, which provided an expedient, cisselective access to the lactam form of the target structure.

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Oxazolidine – Wikipedia,
Oxazolidine | C3H2142NO – PubChem

Related Products of 16251-45-9, A catalyst don’t appear in the overall stoichiometry of the reaction it catalyzes, but it must appear in at least one of the elementary reactions in the mechanism for the catalyzed reaction. 16251-45-9, Name is (4S,5R)-4-Methyl-5-phenyloxazolidin-2-one, molecular formula is C10H11NO2. In a Patent，once mentioned of 16251-45-9

The present invention provides a compound of the formula STR1 which inhibit squalene synthetase and cholesterol biosynthesis and are useful in the treatment of e.g., hyperlipidaemia, atherosclerosis, or fungal infections, processes for the preparation of the compounds of the invention, intermediates useful in these processes, and pharmaceutical compositions containing the compounds.

Balanced chemical reaction does not necessarily reveal either the individual elementary reactions by which a reaction occurs or its rate law.Related Products of 16251-45-9. In my other articles, you can also check out more blogs about 16251-45-9

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Oxazolidine – Wikipedia,
Oxazolidine | C3H2110NO – PubChem

Healthcare careers for chemists are once again largely based in laboratories, although increasingly there is opportunity to work at the point of care, helping with patient investigation. Application In Synthesis of (4S,5R)-4-Methyl-5-phenyloxazolidin-2-one 16251-45-9

A concise, flexible, and high yielding entry into the family of amphidinolide T macrolides, a series of cytotoxic natural products of marine origin, has been developed. All individual members, except amphidinolide T3 (3), derive from compound 39 as a common synthetic intermediate which is formed from three building blocks of similar size and complexity. The fragment coupling steps involve a highly diastereoselective SnCl4 mediated reaction of the furanosyl sulfone derivative 11 with the silyl enol ether 18 and a palladium-catalyzed Negishi type coupling reaction between the polyfunctional organozinc reagent derived from iodide 32a and the enantiopure acid chloride 24b. The 19-membered macrocyclic ring is then formed by a high yielding ring closing metathesis (RCM) reaction of diene 33 catalyzed by the “second generation” ruthenium carbene complex 34. The efficiency of the RCM transformation stems, to a large extent, from the conformational bias introduced by the syn-syn-configured stereotriad at C12-C14 of the substrate which constitutes a key design element of the synthesis plan. The use of Nysted’s reagent 38 in combination with TiCl4 was required for the olefination of the sterically hindered ketone group in 36, whereas more conventional alkene formations were unsuccessful for this elaboration. Finally, it is shown that the inversion of a single and seemingly remote stereocenter (C12) in one of the building blocks not only affects the efficiency and stereochemical outcome of the RCM step but also exerts a significant influence on the course of the acyl-Negishi reaction, allowing a radical manifold to compete with productive cross coupling.

Therefore, this conceptually novel strategy might open impressive avenues to establish green and sustainable chemistry platforms.In my other articles, you can also check out more blogs about 16251-45-9Application In Synthesis of (4S,5R)-4-Methyl-5-phenyloxazolidin-2-one

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Oxazolidine – Wikipedia,
Oxazolidine | C3H2136NO – PubChem

Reference of 16251-45-9, The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.16251-45-9, Name is (4S,5R)-4-Methyl-5-phenyloxazolidin-2-one, molecular formula is C10H11NO2. In a Patent，once mentioned of 16251-45-9

The present invention relates to lipid compounds of the general formula (I): wherein R1 is selected from a C10-C22 alkyl, a C10-C22 alkenyl having 1-6 double bonds, and a C10-C22 alkynyl having 1-6 triple bonds;R2 and R3 are the same or different and may be selected from a group of different substituents; and X represents a carboxylic acid or a derivative thereof, such as a carboxylic ester, a carboxylic anhydride or a carboxamide; or a pharmaceutically acceptable salt, solvate, solvate of such salt or a prodrug thereof. The invention also relates to pharmaceutical compositions and lipid compositions comprising such compounds, and to such compounds for use as medicaments or for use in therapy, in particular for the treatment of diseases related to the cardiovascular, metabolic and inflammatory disease area.

Sometimes chemists are able to propose two or more mechanisms that are consistent with the available data. Reference of 16251-45-9, If a proposed mechanism predicts the wrong experimental rate law, however, the mechanism must be incorrect.Welcome to check out more blogs about 16251-45-9, in my other articles.

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Oxazolidine – Wikipedia,
Oxazolidine | C3H2111NO – PubChem

Chemistry is traditionally divided into organic and inorganic chemistry. Computed Properties of C10H11NO2, The former is the study of compounds containing at least one carbon-hydrogen bonds.In a patent，Which mentioned a new discovery about 16251-45-9

The total synthesis of C25-benzyloxy epothilone C is described. A sequential Suzuki-Aldol-Yamaguchi macrolactonization strategy was utilized employing a novel derivatized C8-C12 fragment. The C25-benzyloxy analog exhibited significantly reduced biological activity in microtubule assembly and cytotoxicity assays. Molecular modeling simulations indicated that excessive steric bulk in the C25 position may reduce activity by disrupting key hydrogen bonds that are crucial for epothilone binding to beta-tubulin.

The design and synthesis of related molecules that are more effective, more selective, and less toxic than aspirin are important objectives of biomedical research.Keep reading other articles of 16251-45-9Computed Properties of C10H11NO2

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Oxazolidine – Wikipedia,
Oxazolidine | C3H2166NO – PubChem

Healthcare careers for chemists are once again largely based in laboratories, although increasingly there is opportunity to work at the point of care, helping with patient investigation. Recommanded Product: (4S,5R)-4-Methyl-5-phenyloxazolidin-2-one 16251-45-9

The total synthesis of tambromycin (1), a recently isolated tetrapeptide, is reported. This unusual natural product possesses a highly modified tryptophan-derived indole fragment fused to an alpha-methylserine-derived oxazoline ring, and a unique noncanonical amino acid residue named tambroline (11). A convergent synthesis of tambromycin was achieved by a 13-step route that leveraged recent developments in the field of C-H functionalization to prepare the complex indole fragment, as well as an efficient synthesis of tambroline that featured a diastereoselective amination of homoproline.

The result showed that such a combination of chemo- and biocatalysis improved the catalytic yield more than two times compared with that of sole metal catalysis.I hope my blog about 16251-45-9 is helpful to your research. Recommanded Product: (4S,5R)-4-Methyl-5-phenyloxazolidin-2-one

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Oxazolidine – Wikipedia,
Oxazolidine | C3H2183NO – PubChem

Synthetic Route of 16251-45-9, As a society publisher, everything we do is to support the scientific community – so you can trust us to always act in your best interests, and get your work the international recognition that it deserves. 16251-45-9, Name is (4S,5R)-4-Methyl-5-phenyloxazolidin-2-one, molecular formula is C10H11NO2. In a Article，once mentioned of 16251-45-9

alpha-N-Acylamino acids have been developed as useful reagents for the preparation of optically pure alpha-aminoalkylaryl ketones.Protection of the amino group as either the ethoxycarbonyl or benzenesulfonyl derivative allows alanine to serve as an effective educt for the chirally specific synthesis of a variety of structures containing the phenylethylamine backbone.Benzene undergoes Friedel-Crafts acylation with the N-acylalanine acid chloride.Catalyst complexation with oxagenated aromatics, however, prohibits acylation of aryl ethers.An arylmetallo reaction scheme overcomes this problem and also affords regiospecificity not attainable in conventional acylations.As examples, optically pure ephedrines and amphetamines were directly synthesized without recourse to resolution since the chirality of the amino acid educt was entirely conserved throughout the process.

Because a catalyst decreases the height of the energy barrier, its presence increases the reaction rates of both the forward and the reverse reactions by the same amount.Read on for other articles about 16251-45-9

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Oxazolidine – Wikipedia,
Oxazolidine | C3H2147NO – PubChem