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PURINE DERIVATIVES AS IMMUNOMODULATORS

The present invention includes novel compounds useful in the treatment of various disorders in particular infectious diseases, cancer, and allergic diseases and other inflammatory conditions for example allergic rhinitis and asthma, and as vaccine adjuvants

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Reference£º
Oxazolidine – Wikipedia,
Oxazolidine | C3H1626NO – PubChem

 

New explortion of (R)-4-Benzyl-2-oxazolidinone

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Stereoselective synthesis of unnatural (2S, 3S)-6-hydroxy-4-sphingenine-containing sphingolipids

6-Hydroxy-(4E)-sphingenine-containing sphingolipids are found in mammalian and bacterial membranes and have multiple intra- and intercellular functions. Most sphingolipids contain a (2S,3R)-2-amino-1,3-diol core structure, but only limited examples of unnatural (2S,3S)-2-amino-1,3-diol derivates have so far been reported. Using an underexplored hydrozirconation-transmetalation reaction and an unusual three-step-one-pot deprotection sequence, we were able to synthesize several unnatural (2S,3S)-6-hydroxy-(4E)-sphingenine-containing sphingolipids in only three (protected) or four (deprotected) consecutive steps, respectively, including a fluoresence-labeled derivative suitable for future biological studies.

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Oxazolidine – Wikipedia,
Oxazolidine | C3H1903NO – PubChem

 

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Optimization of benzoxazole-based inhibitors of Cryptosporidium parvum inosine 5?-monophosphate dehydrogenase

Cryptosporidium parvum is an enteric protozoan parasite that has emerged as a major cause of diarrhea, malnutrition, and gastroenteritis and poses a potential bioterrorism threat. C. parvum synthesizes guanine nucleotides from host adenosine in a streamlined pathway that relies on inosine 5?-monophosphate dehydrogenase (IMPDH). We have previously identified several parasite-selective C. parvum IMPDH (CpIMPDH) inhibitors by high-throughput screening. In this paper, we report the structure-activity relationship (SAR) for a series of benzoxazole derivatives with many compounds demonstrating CpIMPDH IC50 values in the nanomolar range and >500-fold selectivity over human IMPDH (hIMPDH). Unlike previously reported CpIMPDH inhibitors, these compounds are competitive inhibitors versus NAD +. The SAR study reveals that pyridine and other small heteroaromatic substituents are required at the 2-position of the benzoxazole for potent inhibitory activity. In addition, several other SAR conclusions are highlighted with regard to the benzoxazole and the amide portion of the inhibitor, including preferred stereochemistry. An X-ray crystal structure of a representative E¡¤IMP¡¤inhibitor complex is also presented. Overall, the secondary amine derivative 15a demonstrated excellent CpIMPDH inhibitory activity (IC 50 = 0.5 ¡À 0.1 nM) and moderate stability (t1/2 = 44 min) in mouse liver microsomes. Compound 73, the racemic version of 15a, also displayed superb antiparasitic activity in a Toxoplasma gondii strain that relies on CpIMPDH (EC50 = 20 ¡À 20 nM), and selectivity versus a wild-type T. gondii strain (200-fold). No toxicity was observed (LD 50 > 50 muM) against a panel of four mammalian cells lines.

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Oxazolidine – Wikipedia,
Oxazolidine | C3H1835NO – PubChem

 

Extended knowledge of (R)-4-Benzyl-2-oxazolidinone

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Design and synthesis of 3-arylpyrrolidine-2-carboxamide derivatives as melanocortin-4 receptor ligands

Based on 3-phenylpropionamides, a series of 3-arylpyrrolidine-2-carboxamide derivatives was designed and synthesized to study the effect of cyclizations as melanocortin-4 receptor ligands. It was found that the 2R,3R-pyrrolidine isomer possessed the most potent affinity among the four stereoisomers.

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Oxazolidine – Wikipedia,
Oxazolidine | C3H2054NO – PubChem

 

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The lyconadins: Enantioselective total syntheses of (+)-lyconadin A and (-)-lyconadin B

A full account of the enantioselective total syntheses of (+)-lyconadin A (1) and (-)-lyconadin B (2) is presented. Central to this venture was recognition and deployment of a key strategy-level intramolecular aldol/conjugate addition cascade that led, in a single operation, to two new carbon-carbon sigma-bonds, three new stereogenic centers, and two new rings, albeit with the incorrect stereogenicity at C(12) for the lyconadins. Correction of the C(12) stereogenicity was achieved via innovative use of a protonated intramolecular aminal. An aminoiodo olefin cyclization, in conjunction with alpha-pyridinone and 3,4-dihydropyridinone annulation protocols, permitted completion of the syntheses of (+)-lyconadin A (1) and (-)-lyconadin B (2), respectively.

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Oxazolidine – Wikipedia,
Oxazolidine | C3H1733NO – PubChem

 

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Synthesis of cyanoacetyl oxazolidinones

Carefully controlled displacement of chiral chloroacetyl imides with cyanide afforded previously unreported cyanoacetimides in good overall yield. Knoevenagel condensation of the cyanoacetimides to furnish acrylonitriles was also demonstrated. Georg Thieme Verlag Stuttgart . New York.

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Oxazolidine – Wikipedia,
Oxazolidine | C3H2072NO – PubChem

 

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Total synthesis of the highly N-methylated peptides carmabin a and dragomabin

The first total synthesis of carmabin A and dragomabin was achieved at 52.3 mg and 43.8 mg scale, respectively. The synthesis led to determination of the configuration of carmabin A and reassignment of the configuration of dragomabin at the stereogenic centre on the alkyne-bearing fragment.

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Oxazolidine – Wikipedia,
Oxazolidine | C3H2098NO – PubChem

 

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Intermolecular asymmetric reductive aldol reaction of ketones as acceptors promoted by chiral Rh(Phebox) catalyst

The conjugate reduction of cinnamates with hydrosilane and chiral Rh(Phebox-ip) catalyst in the presence of excess acetone is shown to provide the corresponding intermolecular reductive aldol product in extremely high enantioselectivity (up to 98%). Several cinnamates and crotonate substrates and several ketone acceptors were also examined.

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Oxazolidine – Wikipedia,
Oxazolidine | C3H2017NO – PubChem

 

More research is needed about (R)-4-Benzyl-2-oxazolidinone

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INHIBITORS OF THE FIBROBLAST GROWTH FACTOR RECEPTOR

Described herein are inhibitors of FGFR-4, pharmaceutical compositions including such compounds, and methods of using such compounds and compositions.

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Oxazolidine – Wikipedia,
Oxazolidine | C3H1558NO – PubChem

 

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Application of 102029-44-7, The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.102029-44-7, Name is (R)-4-Benzyl-2-oxazolidinone, molecular formula is C10H11NO2. In a Patent£¬once mentioned of 102029-44-7

CYCLOHEXYL SUBSTITUTED PYRROLIDINONES AS INHIBITORS OF 11-BETA-HYDROXYSTEROID DEHYDROGENASE 1

The present invention discloses novel compounds of Formula I: having 11 beta-HSD type 1 antagonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I, as well as methods of using the compounds and compositions to treat diabetes, hyperglycemia, obesity, hypertension, hyperlipidemia, metabolic syndrome, and other conditions associated with 11 beta-HSD type 1 activity.

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Reference£º
Oxazolidine – Wikipedia,
Oxazolidine | C3H1624NO – PubChem