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Seventeen biarylcarboxybenzamide derivatives were prepared for the study of their agonistic/antagonistic activities to the vanilloid receptor (VR1) in rat DRG neurons. The replacement of the piperazine moiety of the lead compound 1 with phenyl ring showed quite enhanced antagonistic activity. Among the prepared derivatives, N-(4-tert-butylphenyl)-4-pyridine-2-yl-benzamide (2, IC 50 = 31 nM) and N-(4-tert-butylphenyl)-4-(3-methylpyridine-2-yl) benzamide (3g, IC50 = 31 nM), showed 5-fold higher antagonistic activity than 1 in 45Ca2+-influx assay.

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Tetrahydroisoquinoline – Wikipedia,
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A series of heterometallic Zr3Pd3-trigonal bipyramidal compounds (1-4) was synthesized by two-component coordination-driven self-assembly of cis-protected palladium(II) 90 acceptors with trinuclear carboxylate-bridged zirconocene-based tripodal metallo-ligands. To avoid multiple product formation using two different metal acceptors, we chose trinuclear Zr(IV) metallo-ligands as donors. All the compounds were characterized by NMR and single crystal X-ray diffraction. Among the compounds, the water-soluble compound 2 is capable to encapsulate aromatic guests such as naphthalene and 2-naphthaldehyde. The encapsulation of the guests was confirmed by NMR and UV-vis spectrometry. The binding constants as well as corresponding Gibbs free energy changes were calculated separately from the 1H NMR titration of compound 2 with guests (naphthalene/2-naphthaldehyde).

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Tetrahydroisoquinoline – Wikipedia,
1,2,3,4-Tetrahydroisoquinoline | C9H11N – PubChem

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Aminomethyl tetrahydronaphthalene biphenyl carboxamide MCH-R1 antagonists with greater selectivity over hERG were identified. SAR studies addressing two distinct alternatives for structural modifications leading to improve hERG selectivity are described.

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Tetrahydroisoquinoline – Wikipedia,
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Compound 7 was identified as the active metabolite of 6 by HPLC and mass spectral analysis. Modification of lead compound 7 by transformation of its N-oxide 6-6 biaryl ring system and fused aromatics produced a series of non-basic fXa inhibitors with excellent potency in anti-fXa and anticoagulant assays. The optimized compounds 73b and 75b showed sub to one digit micromolar anticoagulant activity (PTCT2). Particularly, anti-fXa activity was detected in plasma of rats orally administered with 1 mg/kg of compound 75b.

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Tetrahydroisoquinoline – Wikipedia,
1,2,3,4-Tetrahydroisoquinoline | C9H11N – PubChem

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PYRROLIDINE OR THIAZOLIDINE CARBOXYLIC ACID DERIVATIVES, PHARMACEUTICAL COMPOSITION AND METHODS FOR USE IN TREATING METABOLIC DISORDERSAS AS AGONISTS OF G- PROTEIN COUPLED RECEPTOR 43 (GPR43)

The present invention is directed to novel compounds of formula (I) and their use in treating and/or preventing metabolic diseases

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Tetrahydroisoquinoline – Wikipedia,
1,2,3,4-Tetrahydroisoquinoline | C9H11N – PubChem

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Preparation of aromatic and heteroaromatic carboxylic acids by catalytic ozonolysis

A process for catalytically oxidizing alkylaromatic compounds of the formula (I) Ar?CH2?R where Ar is an optionally substituted, aromatic or heteroaromatic 5-membered or 6-membered ring or a ring system having up to 20 carbon atoms where Ar may optionally be fused to a C1-C6-alkyl group in which up to 2 carbon atoms may be replaced by a heteroatom, and R is hydrogen, phenyl, benzyl or heteroaryl, where the phenyl, benzyl or heteroaryl radicals may also be joined to Ar by a bridge, or R together with Ar forms an optionally substituted ring system which may contain one or more optionally substituted heteroatoms, to the corresponding aromatic or heteroaromatic carboxylic acids in a solvent with ozone in the presence of a transition metal catalyst and optionally in the presence of an acid at a temperature between ?70 C. and 110 C. to the corresponding carboxylic acid.

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Tetrahydroisoquinoline – Wikipedia,
1,2,3,4-Tetrahydroisoquinoline | C9H11N – PubChem

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Synthesis, structures, and magnetism of copper(II) and manganese(II) coordination polymers with azide and pyridylbenzoates

Three transition-metal coordination polymers with azide and/or carboxylate bridges have been synthesized from 4-(3-pyridyl)benzoic acid (4,3-Hpybz) and 4-(4-pyridyl)benzoic acid (4,4-Hpybz) and characterized by X-ray crystallography and magnetic measurements. Compound 1, [Cu(4,3-pybz)(N3)] n, consists of 2D coordination networks in which the uniform chains with (mu-EO-N3)(mu-COO) double bridges are cross-linked by the 4,3-pybz ligands. Compound 2, [Cu2(4,4-pybz)3(N 3)]n?3nH2O, consists of 2-fold interpenetrated 3D coordination networks with the alpha-Po topology, in which the six-connected dinuclear motifs with mixed (mu-EO-N3)(mu-COO) 2 (EO = end-on) triple bridges are linked by the 4,4-pybz spacers. Compound 3, [Mn(4,4-pybz)(N3)(H2O)2] n, contains 2D manganese(II) coordination networks in which the chains with single mu-EE-N3 bridges (EE = end-to-end) are interlinked by the 4,4-pybz ligands, and the structure also features a 2D hydrogen-bonded network in which MnII ions are linked by double triatomic bridges, (mu-EE-N3)(O-H???N) and (O-H???O)2. Magnetic studies indicated that the mixed azide and carboxylate bridges in 1 and 2 induce ferromagnetic coupling between CuII ions and that 3 features antiferromagnetic coupling through the EE-azide bridge. In addition, compound 1 exhibits antiferromagnetic ordering below 6.2 K and behaves as a field-induced metamagnet. A magnetostructural survey indicates a general trend that the ferromagnetic coupling through the mixed bridges decreases as the Cu-N-Cu angle increases.

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Tetrahydroisoquinoline – Wikipedia,
1,2,3,4-Tetrahydroisoquinoline | C9H11N – PubChem

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Metal-Organic Framework Magnets

Metal-organic frameworks represent the ultimate chemical platform on which to develop a new generation of designer magnets. In contrast to the inorganic solids that have dominated permanent magnet technology for decades, metal-organic frameworks offer numerous advantages, most notably the nearly infinite chemical space through which to synthesize predesigned and tunable structures with controllable properties. Moreover, the presence of a rigid, crystalline structure based on organic linkers enables the potential for permanent porosity and postsynthetic chemical modification of the inorganic and organic components. Despite these attributes, the realization of metal-organic magnets with high ordering temperatures represents a formidable challenge, owing largely to the typically weak magnetic exchange coupling mediated through organic linkers. Nevertheless, recent years have seen a number of exciting advances involving frameworks based on a wide range of metal ions and organic linkers. This review provides a survey of structurally characterized metal-organic frameworks that have been shown to exhibit magnetic order. Section 1 outlines the need for new magnets and the potential role of metal-organic frameworks toward that end, and it briefly introduces the classes of magnets and the experimental methods used to characterize them. Section 2 describes early milestones and key advances in metal-organic magnet research that laid the foundation for structurally characterized metal-organic framework magnets. Sections 3 and 4 then outline the literature of metal-organic framework magnets based on diamagnetic and radical organic linkers, respectively. Finally, Section 5 concludes with some potential strategies for increasing the ordering temperatures of metal-organic framework magnets while maintaining structural integrity and additional function.

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Tetrahydroisoquinoline – Wikipedia,
1,2,3,4-Tetrahydroisoquinoline | C9H11N – PubChem

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Structure-activity study on a series of alpha-glutamic acid scaffold based compounds as new ADAMTS inhibitors

A series of alpha-glutamic acid scaffold based 4-(benzamido)-4-(1,3,4- oxadiazol-2-yl) butanoic acids were designed and synthesized as new ADAMTS inhibitors. The compounds dose-dependently inhibited the enzymatic activities of ADAMTS-4 and ADAMTS-5. One of the most active compound 2h potently inhibited ADAMTS-4 and ADAMTS-5 with IC50 values of 1.2 and 0.8 muM, respectively. These inhibitors may serve as new lead compounds for further development of therapeutics to treat osteoarthritis.

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Tetrahydroisoquinoline – Wikipedia,
1,2,3,4-Tetrahydroisoquinoline | C9H11N – PubChem

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Self-assembled [2]catenane in trapezoidal metallacycles with [Cp?Ir]-corners

A series of trapezoidal metallacycles were synthesized by the selective combination of a rigid with a flexible arm. [2]Catenane 3 was obtained by self-assembly when the cavity size of the trapezoidal rings was optimised.

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1,2,3,4-Tetrahydroisoquinoline | C9H11N – PubChem