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Structure-activity relationships in the binding of chemically derivatized CD4 to gp120 from human immunodeficiency virus

The first step in HIV infection is the binding of the envelope glycoprotein gp120 to the host cell receptor CD4. An interfacial “Phe43 cavity” in gp120, adjacent to residue Phe43 of gp120-bound CD4, has been suggested as a potential target for therapeutic intervention. We designed a CD4 mutant (D1D2F43C) for site-specific coupling of compounds for screening against the cavity. Altogether, 81 cysteine-reactive compounds were designed, synthesized, and tested. Eight derivatives exceeded the affinity of native D1D2 for gp120. Structure-activity relationships (SAR) for derivatized CD4 binding to gp120 revealed significant plasticity of the Phe43 cavity and a narrow entrance. The primary contacts for compound recognition inside the cavity were found to be van der Waals interactions, whereas hydrophilic interactions were detected in the entrance. This first SAR on ligand binding to an interior cavity of gp120 may provide a starting point for structure-based assembly of small molecules targeting gp120-CD4 interaction.

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Oxazolidine – Wikipedia,
Oxazolidine | C3H1144NO – PubChem

 

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(1S)-(-)- N -Trifluoromethylthio-2,10-camphorsultam and its derivatives: Easily available, optically pure reagents for asymmetric trifluoromethylthiolation

A family of easily scalable, shelf-stable, optically pure reagents (1S)-(-)-N-trifluoromethylthio-2,10-camphorsultam 1a-c was successfully developed. In particular, compound 1c was shown to be an efficient reagent that is capable of transferring chirality to other prochiral nucleophiles such as beta-ketoesters, oxindoles and benzofuranones with good to excellent enantioselectivities.

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Oxazolidine – Wikipedia,
Oxazolidine | C3H1195NO – PubChem

 

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Efficient and Mild Ullmann-Type N-Arylation of Amides, Carbamates, and Azoles in Water

A simple, sustainable, efficient, mild, and low-cost protocol was developed for d-glucose-assisted Cu-catalyzed Ullmann reactions in water for amides, carbamates, and nitrogen-containing heterocycles. The reaction was compatible with diverse aryl/heteroaryl iodides, giving highly substituted pyridine, indole, or indazole rings. This method offers an attractive alternative to existing protocols, because the reaction proceeds in aqueous media, occurs at or near ambient temperature, and provides the N-arylated products in good to high yields.

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Oxazolidine – Wikipedia,
Oxazolidine | C3H355NO – PubChem

 

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Zinc-Catalyzed Stereo- and Regioselective 1,4-Hydrative Fluorination of 3-En-1-ynamides with Selectfluor

Zinc-catalyzed 1,4-oxofluorinations of 3-en-1-ynamides with Selectfluor in acetonitrile/water proceeded with high regio- and stereoselectivity, giving E-configured gamma-fluoro-alpha,beta-unsaturated amides efficiently. Our control experiments indicate that kinetically unstable C-bound zinc dienolates are chemically reactive to undergo SE2?-electrophilic fluorinations whereas the detectable O-bound dienolates preferably undergo protodemetalation reactions instead.

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Oxazolidine – Wikipedia,
Oxazolidine | C3H653NO – PubChem

 

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Solution and solid-phase synthesis of trifluoromethyl peptides and mimetics

This paper reviews the solution-phase synthesis of trifluoromethyl (Tfm)-analogues of bioactive peptides, such as RGD-peptides and the aspartyl protease inhibitor pepstatin, and the solution/solid-phase synthesis of Tfm-substituted retro- and retro-inverso peptides and hydroxamates.

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Oxazolidine – Wikipedia,
Oxazolidine | C3H369NO – PubChem

 

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PESTICIDAL COMPOSITIONS AND RELATED METHODS

A pesticidal composition comprises at least one compounds selected from a compound of formula, or any agriculturally acceptable salt thereof, wherein R1, R2, R3, R4, R5, R6, R7, R8, Q, Z, L, La, and x are as described herein. A method of controlling pests comprises applying the pesticidal composition near a population of pests.

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Oxazolidine – Wikipedia,
Oxazolidine | C3H265NO – PubChem

 

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An intermolecular hydroamination of allenamides with arylamines catalyzed by cationic Au(I) salts

(Figure presented) An intermolecular hydroamination of allenamides with arylamines has been achieved under mild Au(I) catalysis conditions delivering allylamino E-enamides stereoselectively and in high yield. The reaction is made possible via a convenient method for conjugated N-acyliminium formation.

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Oxazolidine – Wikipedia,
Oxazolidine | C3H609NO – PubChem

 

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Preparation of N-substituted imidazolidinones and N-substituted 2-thionimidazolidinones

The invention is a process for the preparation of N-substituted imidazolidinones and N-substituted 2-thionimidazolidinones which comprises contacting an oxazolidinone with a compound containing a nitrogen directly bonded to a carbonyl or a thiocarbonyl group in the presence of a Lewis acid catalyst or the hydrate of a Lewis acid catalyst under conditions such that an N-substituted imidazolidinone or N-substituted 2-thionimidazolidinone is prepared. The compound containing a nitrogen directly bonded to a carbonyl or a thiocarbonyl group is an isocyanate or isothiocyanate or a compound wherein the nitrogen is reactive and the carbonyl or thiocarbonyl group is further bonded to a substituent by a bond which is clevable under the reaction conditions. The Lewis acid catalyst corresponds to the formula wherein M is a group IB-VIIIB, IIIA or IVA element with the proviso that M is not C or Si; X is a halogen; and n is 2, 3 or 4.

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Oxazolidine – Wikipedia,
Oxazolidine | C3H251NO – PubChem

 

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NITROGEN-CONTAINING HETEROCYCLYL SUBSTITUTED IMIDAZOQUINOLINES AND IMIDAZONAPHTHYRIDINES

Imidazoquinoline and imidazonaphthyridine compounds having a nitrogen-containing heterocyclyl substituent at the 5-, 6-, 7-, or 8-position, pharmaceutical compositions containing the compounds, intermediates, and methods of making and methods of use of these compounds as immunomodulators, for modulating cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases are disclosed.

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Reference£º
Oxazolidine – Wikipedia,
Oxazolidine | C3H168NO – PubChem

 

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Reference of 497-25-6, 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.497-25-6, Name is Oxazolidin-2-one, molecular formula is C3H5NO2. In a article£¬once mentioned of 497-25-6

Glaucoma treatment

A method and a composition for treating or reducing and/or controlling intraocular pressure comprising administering an effective amount of a renin inhibiting compound of the formula: STR1 where A is a substituent; W is CO or CHOH and U is CH2 or NR2 wherein R2 is hydrogen or loweralkyl; with the proviso that when W is CHOH then U is Ch2 ; R1 is loweralkyl, cycloalkyl methyl, benzyl, (alpha, alpha)-dimethylbenzyl, 4-hydroxybenzyl, 4-methoxybenzyl, halobenzyl, (1-naphthyl)methyl, (2-naphthyl)methyl, 1-bezyloxyethyl, phenethyl, phenoxy, thiophenoxy or anilino; R3 is loweralkyl, loweralkenyl, ((alkoxy)alkoxy)loweralkyl, (thioalkoxy)alkyl, benzyl or heterocyclic ring substituted methyl; and R4 is substituted hydroxyalkyamino.

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Reference£º
Oxazolidine – Wikipedia,
Oxazolidine | C3H226NO – PubChem