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ZrOCl2 · 8 H2O and HfOCl2 · 8 H2O are highly effective, water-tolerant, and reusable homogeneous catalysts for direct ester condensation be-tween equimolar amounts of carboxylic acids and alcohols. Notably, zirconium(IV) salts such as ZrOCl2 · 8 H2O and Zr(OAc)x(OH)y are potential green catalysts due to their low toxicity, commercial availability at low cost, ease of handling, high catalytic activity, and reusability.

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A general method is described for the formation of furanoid and pyranoid glycals.Thus, lithium-ammonia reduction of the corresponding 1-chloro-2,3-O-isopropylidene furanoid and pyranoid carbohydrate derivatives affords the desired glycals in 87-92percent yields.Several examples that reveal the scope of this process are described .The formation of C-glycosides from the glycal esters through application of the ester enolate Claisen rearrangement is explored.The characteristics and stereochemistry of this process in both the acyclic and cyclic series of glycal derivatives are described.

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A novel method has been established for the construction of C-S bonds using redox-active esters with disulfides in the presence of Ru-photoredox catalyst. This method exhibits remarkable functional group tolerance across a wide scope of substrates. Under mild conditions, a structurally diverse array of aryl alkyl sulfides is successfully and efficiently obtained through decarboxylative cross-coupling.

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Tetrandrine, a lead anti-tumor compound with a bis-benzyltetrahydroisoquinoline skeleton isolated from medicinal plant Stephania tetrandra. In order to obtain active anti-tumor agents and evaluate their structure-activity relationships, a series of novel tetrandrine derivatives were designed and synthesized in this study. Their anti-tumor activities against human hepatocellular carcinoma cell lines (HMCC97L and PLC/PRF/5) were also evaluated. The bioassay results showed that the derivatives exhibited moderate to strong inhibition against the two cell lines. Among them, compound 31 showed prominent cytotoxicity with IC50 = 1.06 muM (15.8 folds than that of tetrandrine, and 30.3 folds than that of Sorafenib). Further studies on the mechanisms demonstrated that the in vitro anti-tumor activity of compound 31 was predominantly due to the inducement of apoptosis of HCC cells. Compound 31 was capable of initiating endoplasmic reticulum stress-associated apoptotic cell death, and the activation of JNK as well as caspase pathways were probably involved. Our results suggest that compound 31, a new 14-position substituted amide tetrandrine derivative, might be a potential candidate for developing novel anti-HCC drugs in the coming future.

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Provided herein are methods of treatment for kidney stones, e.g., for controlling or inhibiting the formation of calcium oxalate kidney stones by inhibiting the production of glyoxylate and/or oxalate, treatment of primary hyperoxaluria, etc. In some embodiments, methods comprise administering to a subject in need thereof, in combination, an inhibitor of hydroxyproline dehydrogenase (HYPDH), an inhibitor of glycolate oxidase (GO), and/or another agent for the treatment of kidney stones. Compositions for such use or the use of active agents in the manufacture of a medicament for the treatment of kidney stones are also provided.

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New research progress on 166591-85-1 in 2021. Recommanded Product: 2-(tert-Butoxycarbonyl)-1,2,3,4-tetrahydroisoquinoline-1-carboxylic acid, Catalysts function by providing an alternate reaction mechanism that has a lower activation energy than would be found in the absence of the catalyst. In some cases, the catalyzed mechanism may include additional steps.In a article, 166591-85-1, molcular formula is C15H19NO4, introducing its new discovery.

Described is the use in the treatment of either male or female sexual dysfunction of selective antagonists of the alpha1B-adrenergic receptor and the pharmaceutical compositions containing them as compounds capable of helping the sexual act avoiding at the same time excessive side effects due to acute hypotension.

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Significance: Proline catabolism refers to the 4-electron oxidation of proline to glutamate catalyzed by the enzymes proline dehydrogenase (PRODH) and l-glutamate gamma-semialdehyde dehydrogenase (GSALDH, or ALDH4A1). These enzymes and the intermediate metabolites of the pathway have been implicated in tumor growth and suppression, metastasis, hyperprolinemia metabolic disorders, schizophrenia susceptibility, life span extension, and pathogen virulence and survival. In some bacteria, PRODH and GSALDH are combined into a bifunctional enzyme known as proline utilization A (PutA). PutAs are not only virulence factors in some pathogenic bacteria but also fascinating systems for studying the coordination of metabolic enzymes via substrate channeling. Recent Advances: The past decade has seen an explosion of structural data for proline catabolic enzymes. This review surveys these structures, emphasizing protein folds, substrate recognition, oligomerization, kinetic mechanisms, and substrate channeling in PutA. Critical Issues: Major unsolved structural targets include eukaryotic PRODH, the complex between monofunctional PRODH and monofunctional GSALDH, and the largest of all PutAs, trifunctional PutA. The structural basis of PutA-membrane association is poorly understood. Fundamental aspects of substrate channeling in PutA remain unknown, such as the identity of the channeled intermediate, how the tunnel system is activated, and the roles of ancillary tunnels. Future Directions: New approaches are needed to study the molecular and in vivo mechanisms of substrate channeling. With the discovery of the proline cycle driving tumor growth and metastasis, the development of inhibitors of proline metabolic enzymes has emerged as an exciting new direction. Structural biology will be important in these endeavors.

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The present invention relates to compounds of formula (I) or pharmaceutically acceptable derivatives thereof, useful in the treatment or prophylaxis of CCR5-related diseases and disorders, for example, in the inhibition of HIV replication, the prevention or treatment of an HIV infection, and in the treatment of the resulting acquired immune deficiency syndrome (AIDS).

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The present invention relates to an improved process for the preparation of Alfuzosin of formula (I). The process involves utilizing intermediate of formula (Ia) wherein S represents acid residue of organic acids like acetic acid, oxalic acid, succinic acid, methane sulfonic acid, p-toluene sulfonic acid and the like. The present invention also relates to novel Amorphous form of Alfuzosin of formula (I).

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A series of indazole arylsulfonamides were synthesized and examined as human CCR4 antagonists. Methoxy- or hydroxyl- containing groups were the more potent indazole C4 substituents. Only small groups were tolerated at C5, C6, or C7, with the C6 analogues being preferred. The most potent N3-substituent was 5-chlorothiophene-2-sulfonamide. N1 meta-substituted benzyl groups possessing an alpha-amino-3-[(methylamino)acyl]- group were the most potent N1-substituents. Strongly basic amino groups had low oral absorption in vivo. Less basic analogues, such as morpholines, had good oral absorption; however, they also had high clearance. The most potent compound with high absorption in two species was analogue 6 (GSK2239633A), which was selected for further development. Aryl sulfonamide antagonists bind to CCR4 at an intracellular allosteric site denoted site II. X-ray diffraction studies on two indazole sulfonamide fragments suggested the presence of an important intramolecular interaction in the active conformation.

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