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Synthesis of novel piperidine-4-carboxamide derivatives as antibacterial agents has elevated impact on medicinal field. In the present work, ten new compounds were synthesized and screened toward their antibacterial studies. The structures of these compounds were characterized and analyzed by spectral studies such as IR, mass and 1H NMR and compounds 6a and 6c-6h, were observed to possess potent antimicrobial activity.

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Piperidine – Wikipedia,
Piperidine | C5H8017N – PubChem

 

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The invention relates to (hetero)cyclic compounds as S1P modulators, pharmaceutical compositions comprising such compounds, and uses thereof in the treatment, alleviation or prevention of diseases or disorders mediated by an S1P receptor.

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A series of xanthine derivatives as potent dual ligands targeting DPP-IV and GPR119 was discovered through an approach of the merged pharmacophores of GPR119 agonists and DPP-IV inhibitor linagliptin. Systematic optimization of general structure 5 led to the identification of compound 20i with selective DPP-IV inhibition, good GPR119 agonism activity and favorable metabolic stability. Docking study was performed to elucidate the potent DPP-IV inhibition of 20i. Compound 20i may serve as a tool compound for further design of anti-diabetic drugs targeting both DPP-IV and GPR119.

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An assay employing a fluorescently labeled split and pool peptide library has been applied to the discovery of a new class of octapeptide catalysts for the kinetic resolution of secondary alcohols. A highly diverse library of peptide-based catalysts was synthesized on solid-phase synthesis beads such that each individual bead was co-functionalized with (i) a uniform loading of a pH-sensitive fluorophore and (ii) a unique peptidebased catalyst. The library was then screened for activity in acylation reactions employing (±)-sec-phenylethanol as the substrate and acetic anhydride as the acylation agent. From the most active catalysts, a lead peptide (4) was identified that provides a selectivity-factor (krel) of 8.2 upon resynthesis and evaluation under homogeneous conditions. A “directed” second-generation split and pool peptide library was synthesized such that the new peptide sequences in the library were biased toward the lead structure. Random samples of the second generation library were screened in single bead assays that revealed several new peptide-based catalysts that afford improved selectivities in kinetic resolutions. Peptide catalyst 13 proves effective for the kinetic resolution of sec-phenylethanol (krel = 20), as well as eight other secondary alcohols of a broad substrate scope (krel = 4 to > 50).

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Aliphatic amines strongly coordinate, and therefore easily inhibit, the activity of transition-metal catalysts, posing a marked challenge to nitrogen-hydrogen (N?H) insertion reactions. Here, we report highly enantioselective carbene insertion into N?H bonds of aliphatic amines using two catalysts in tandem: an achiral copper complex and chiral amino-thiourea. Coordination by a homoscorpionate ligand protects the copper center that activates the carbene precursor. The chiral amino-thiourea catalyst then promotes enantioselective proton transfer to generate the stereocenter of the insertion product. This reaction couples a wide variety of diazo esters and amines to produce chiral a-alkyl a?amino acid derivatives.

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Chemistry is traditionally divided into organic and inorganic chemistry. SDS of cas: 2971-79-1. The former is the study of compounds containing at least one carbon-hydrogen bonds.In a patent,Which mentioned a new discovery about 2971-79-1

The invention discloses a method for improving the water solubility of tryptanthrin, belonging to the technical field of cosmetics. The chromone is modified under the condition that the reactive group of the amine ketone is not changed; and the tryptamine is adopted as an intermediate to modify the tryptanthrone. The invention further discloses a method for synthesizing the mono-bromochromone derivative and N – benzylic ring – N N-alkanoic acid tryptanthrin derivative as well as a preparation method and application. N -benzyl ring – N N-alkanoic acid tryptanthrin derivative has excellent indoleamine -2, 3 – dioxygenase (IDO) inhibitor activity, and the like. The invention has wide application prospect, and can be used for treating diseases of cancer, ‘s disease, depression, cataract and the like with IDO-mediated pathologic characteristics of the tryptophan metabolic pathway. Under the condition that the active group of the amine ketone is not changed, the solubility. The method has the advantages, such as simple operation, mild conditions and the like, and is easy for industrial production. (by machine translation)

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Obovatol, a novel lignan isolated from the leaf and stem bark of Magnolia obovata Thunb exhibits many important biological activities. To discover natural-product-based potential fungicides with novel structural skeletons, a series of Mannich base derivatives were prepared by the C-4-aminomethylated modification of obovatol and all synthesized compounds were evaluated for antifungal activities in vitro against several phytopathogenic fungi using the spore germination method and the mycelium growth rate method. Furthermore, their structures were also characterized by 1H NMR, 13C NMR, and HR-MS, and compound 2k was further analyzed by single-crystal X-ray diffraction. Among all of the derivatives, compounds 2b (IC50 = 28.68 mug/mL) and 2g (IC50 = 16.90 mug/mL) demonstrated greater inhibition of Botrytis cinerea spore germination than two positive controls, hymexazol and difenoconazole. Compounds 2c, 2f, and 2g displayed potent mycelial growth inhibition of B. cinerea with an average inhibition rate (AIR) of >90% at a concentration of 100 mug/mL. Additionally, the structure-activity relationships (SARs) suggested that the introduction of a diethylamino, pyrrolyl, 1-methyl-piperazinyl or 1-ethyl-piperazinyl groups on the C-4 position of obovatol may be more likely to yield potential antifungal compounds than the introduction of 4-phenyl-piperazinyl or 4-phenyl-piperidinyl groups.

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The present invention relates generally to compounds represented in Formula I, pharmaceutical compositions comprising them and methods of treating of diseases or disorders related to the function of the calcium sensing receptor. The invention also relates to processes for making such compounds and to intermediates useful in these processes. [image]

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The important role of Methyl piperidine-4-carboxylate

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Compounds of formula (I): or a pharmaceutically acceptable salt thereof, wherein: W is arylene, heteroarylene or formula (a) each L is independently alkylene, alkenylene, alkynylene, a direct bond, arylene, cycloalkylene, alkylene-arylene, alkylene-C=O or-C=O; each X is independently an N-containing heteroarylene, N-containing cycloalkylene or NR; Y is N-containing heteroaryl, N-containing cycloalkyl, NR2, OR1, CN or CO2R; Z1 is formula (b); are useful in therapy, particularly in the therapy of neurodegeneration and cancer.

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Piperidine – Wikipedia,
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2-Amino-4-azaindoles have been identified as a structurally novel class of BKCa channel openers. Their synthesis from 2-chloro-3-nitropyridine is described together with their in vitro properties assessed by 86Rb+ efflux and whole-cell patch-clamp assays using HEK293 cells stably transfected with the BKCa alpha subunit. In vitro functional characterization of BKCa channel opening activity was also assessed by measurement of relaxation of smooth muscle tissue strips obtained from Landrace pig bladders. The preliminary SAR data indicate the importance of steric bulk around the 2-amino substituent.

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