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The title compounds were synthesized by the efficient route previously explored for the synthesis of enantiomeric pairs of thiolactomycin and its 3-demethyl derivative. These studies were carried out to prove the flexibility of the previously explored synthetic route to natural thiolactomycin (TLM) 1 and to examine the structure-activity relationship on the 5-position of 1. While all of the synthesized congeners lacked in vitro antibacterial activity, these studies led us to find 5-(alk-2-enyl)-TLM (ent-4d) which exhibits mammalian type I fatty acid synthase (FAS) inhibitory activity equal to that of C75, a potent inhibitor reported previously. It was also found that 5-[(E)-cycloalk-2- enylidenemethyl]-TLM (ent-5c) exhibited slightly less potent mammalian type I FAS inhibitory activity than C75.

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Reference£º
Oxazolidine – Wikipedia,
Oxazolidine | C3H1961NO – PubChem

 

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Compounds having the formula are useful for treating conditions which arise from or are exacerbated by angiogenesis. Also disclosed are pharmaceutical compositions comprising the compounds, methods of treatment using the compounds, methods of inhibiting angiogenesis, and methods of treating cancer.

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Reference£º
Oxazolidine – Wikipedia,
Oxazolidine | C3H1549NO – PubChem

 

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Synthesis and antibacterial activity of dihydro-1,2-oxazine and 2-pyrazoline oxazolidinones: Novel analogs of linezolid

The synthesis and antibacterial activity of oxazolidinones containing dihydro-1,2-oxazine and 2-pyrazoline ring systems are described. Linezolid analogs utilizing dihydro-1,2-oxazines as morpholine mimics were prepared utilizing a nitrosoamine/diene 4+2 cycloaddition strategy. Pyrazolidine, hexahydro-pyridazine, and 2-pyrazoline analogs more closely related to eperezolid were also prepared. The most active of these new oxazolidinones were the dihydro-1,2-oxazine 6 and the 2-pyrazoline 20 both of which had potency similar to linezolid against a panel of Gram-positive bacteria.

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Reference:
Oxazolidine – Wikipedia,
Oxazolidine | C3H1283NO – PubChem

 

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In homogeneous catalysis, the catalyst is in the same phase as the reactant. The number of collisions between reactants and catalyst is at a maximum.In a patent, 102029-44-7, name is (R)-4-Benzyl-2-oxazolidinone, introducing its new discovery. Product Details of 102029-44-7

The Influence of Solubilizing Chain Stereochemistry on Small Molecule Photovoltaics

Three stereochemically pure isomers and two isomeric mixtures of a solution-processable diketopyrrolopyrrole-containing oligothiophene (SMDPPEH) have been used to study the effect of 2-ethylhexyl solubilizing group stereochemistry on the film morphology and bulk heterojunction (BHJ) solar cell characteristics of small molecule organic photovoltaics. The different SMDPPEH stereoisomer compositions exhibit nearly identical optoelectronic properties in the molecularly dissolved state, as well as in amorphous films blended with PCBM. However, for films in which SMDPPEH crystallization is induced by thermal annealing, significant differences in molecular packing between the different stereoisomer formulations are observed. These differences are borne out in photovoltaic device characteristics for which unannealed devices show very similar behavior, while after annealing the RR- and SS-SMDPPEH enantiomers show blue-shifted peak EQE relative to the SMDPPEH isomer mixtures. Unannealed devices made from the most crystalline stereoisomer, meso RS-SMDPPEH, are not completely amorphous, and show improved photocurrent generation as a result. Unlike the other compounds, after thermal annealing the RS-SMDPPEH devices show reduced device performance. The results reveal that the chirality of commonly used 2-ethylhexyl solubilizing chains can have a significant effect on the morphology, absorption, and optimum processing conditions of small molecule organic thin films used as photovoltaic device active layers.

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Reference:
Oxazolidine – Wikipedia,
Oxazolidine | C3H2103NO – PubChem

 

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Synthesis of alpha-chiral-beta,gamma-unsaturated carboxylic acid derivatives using chiral auxiliaries

We report an efficient and reliable method for the synthesis of alpha-chiral-beta,gamma-unsaturated carboxylic acid derivatives using chiral auxiliaries and vinylacetic acid. Two well-established chiral auxiliaries ((S,S)-pseudoephedrine and (R)-benzyl-oxazolidinone) were chosen to test the merits of this method. Six different electrophiles were examined in the diastereoselective alkylation with both auxiliaries. The pseudoephedrine auxiliary provided isolated yields between 61 and 85% and diastereomeric ratios all greater than 96:4. Employing the same reactions as with the pseudoephedrine derivative, the corresponding oxazolidinone auxiliary provided isolated yields between 0 and 80% with diastereomeric ratios from 80:20 to 93:7.

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Reference:
Oxazolidine – Wikipedia,
Oxazolidine | C3H1984NO – PubChem

 

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Total Synthesis of Tambromycin Enabled by Indole C-H Functionalization

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.

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Reference:
Oxazolidine – Wikipedia,
Oxazolidine | C3H2183NO – PubChem

 

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N-ALKOXYAMIDES OF 6-(TRISUBSTITUTED PHENYL)-4-AMINOPICOLINATES AND THEIR USE AS SELECTIVE HERBICIDES FOR CROPS

N-Alkoxyamides of 4-aminopicolinic acids and 6-amino-4-pyrimidinecarboxylates are selective herbicides for corn, canola and sugar beet.

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Reference:
Oxazolidine – Wikipedia,
Oxazolidine | C3H1260NO – PubChem

 

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A Novel Decalin-Based Bicyclic Scaffold for FKBP51-Selective Ligands

Selective inhibition of FKBP51 has emerged as possible novel treatment for diseases like major depressive disorder, obesity, chronic pain, and certain cancers. The current FKBP51 inhibitors are rather large, flexible, and have to be further optimized. By using a structure-based rigidification strategy, we hereby report the design and synthesis of a novel promising bicyclic scaffold for FKBP51 ligands. The structure-activity analysis revealed the decalin scaffold as the best moiety for the selectivity-enabling subpocket of FBKP51. The resulting compounds retain high potency for FKBP51 and excellent selectivity over the close homologue FKBP52. With the cocrystal structure of an advanced ligand in this novel series, we show how the decalin locks the key selectivity-inducing cyclohexyl moiety of the ligand in a conformation typical for FKBP51-selective binding. The best compound 29 produces cell death in a HeLa-derived KB cell line, a cellular model of cervical adenocarcinoma, where FKBP51 is highly overexpressed. Our results show how FKBP51 inhibitors can be rigidified and extended while preserving FKBP51 selectivity. Such inhibitors might be novel tools in the treatment of human cancers with deregulated FKBP51.

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Reference:
Oxazolidine – Wikipedia,
Oxazolidine | C3H1742NO – PubChem

 

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PYRAZOLE DERIVATIVES AS SGC STIMULATORS

There are described imidazole and pyrazole derivatives which are useful as stimulators of sGC, particularly NO-independent, heme-dependent stimulators. These compounds are also useful for treating, preventing or managing various disorders that are herein disclosed.

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Reference:
Oxazolidine – Wikipedia,
Oxazolidine | C3H1255NO – PubChem

 

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Practical asymmetric synthesis of a novel gamma-secretase inhibitor

An efficient route to gamma-secretase inhibitor hydroxyl thiophene sulfonamide 1 is described. The approach contains nine steps with an overall yield of 8%. The synthesis highlights a diastereoselective methylation using Evans’ oxazolidinone method and a chiral Strecker reaction via Davis’ sulfonimine protocol.

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Reference:
Oxazolidine – Wikipedia,
Oxazolidine | C3H2070NO – PubChem