CKD-497 inhibits NF-kB signaling and ameliorates inflammation and pulmonary fibrosis in ovalbumin-induced asthma and particulate matter-induced airway inflammatory diseases.

Air pollution, allergens, and bacterial infections are major contributors to pathological respiratory disorders worldwide. CKD-497, derived from the rhizome of and the fruits of , is known for its ability to relieve cough and facilitate phlegm expectoration. However, its protective action against allergic asthma and fine dust-induced lung inflammation, along with its underlying mechanisms, have not been thoroughly investigated.

Pharmacokinetics and bioequivalence of tofacitinib 5 mg in healthy Korean male subjects.

Objective: Tofacitinib is an oral Janus kinase (JAK) inhibitor marketed as an immunomodulator that can effectively treat rheumatoid arthritis. This study aimed to compare the pharmacokinetics and evaluate the bioequivalence of tofacitinib free base (CKD-374) with those of tofacitinib citrate (Xeljanz).

Materials And Methods: A randomized, open-label, single-dose, 2-sequence, 2-period crossover study was conducted in healthy Korean male subjects.

The mechanical characteristics and performance evaluation of a newly developed silicone airway stent (GINA stent).

Central airway obstruction (CAO) can be attributed to several benign or malignant conditions. Although surgery is the preferred therapeutic option for the management of CAO, bronchoscopic treatment can be performed in scenarios where the surgical procedure is not possible. Recent years have witnessed several improvements in the field of bronchoscopic treatment, especially with regard to airway stents.

Constituents from Solidago virgaurea var. gigantea and their inhibitory effect on lipid accumulation.

In this study, the anti-adipogenic activities of compounds isolated from Solidago viraurea var. gigantea (SG) extracts were investigated using Oil Red O staining in the 3T3-L1 cell line. Four known compounds including 3,5-di-O-caffeoylquinic acid (5), protocatechuic acid (6), chlorogenic acid (7), and kaempferol-3-O-rutinoside (8), and four undescribed compounds including (1R,2S,3S,5R,7S)-methyl 7-((cinnamoyloxy)methyl)-2,3-dihydroxy-6,8-dioxabicyclo[3.

Crystal structure of bis-[2-(1-benzimidazol-2-yl-κ )aniline-κ]bis-(nitrato-κ)cadmium(II).

In the title compound, [Cd(NO)(CHN)], the Cd atom lies on a twofold rotation axis and is coordinated by four N atoms and two O atoms, provided by two bidentate 2-(1-benzimidazol-2-yl)aniline ligands, and two nitrato O atoms, forming a distorted octa-hedral geometry [range of bond angles around the Cd atom = 73.82 (2)-106.95 (8)°].

Crystal structure of 2,3-bis-(4-methyl-phen-yl)benzo[]quinoxaline.

The title compound, CHN, was obtained during a search for new π-extended ligands with the potential to generate efficient phosphors with iridium(III) for organic light-emitting devices (OLEDs). The benzoquinoxaline ring system is almost planar (r.m.

Crystal structure of aqua-(1-pyrazole-κ)(pyridine-2,6-di-carboxyl-ato-κ,,)copper(II) dihydrate.

In the title compound, [Cu(CHNO)(CHN)(HO)]·2HO, the Cu atom is coordinated by three O atoms and two N atoms, provided by a tridentate pyridine-2,6-di-carboxyl-ate (pdc), one pyrazole and one water ligand, forming a slightly distorted square-pyramidal geometry [range of O-Cu-O and O-Cu-N bond angles = 79.55 (8)-166.22 (10)°].

Practical and Sustainable Synthesis of Optically Pure Levocabastine, a H₁ Receptor Antagonist.

A practical and sustainable method for the synthesis of levocabastine hydrochloride (), a H₁ receptor antagonist for the treatment of allergic conjunctivitis, that can be applied to the industrial production of the compound has been developed. Substantial improvements over the previously reported procedure are achieved via efficient preparation of an optically active key intermediate () without chiral resolution and with a more effective detosylation, which complements the previous procedure. Notably, our process requires no chromatographic purification and provides levocabastine hydrochloride in greater than 99.

Crystal structure of (3,5-dimethyl-1-pyrrol-2-yl)di-phenyl-phosphine oxide.

The title compound, CHNOP, was obtained during a search for new P,N-containing ligands with the potential to generate precatalysts with chromium(III) for selective ethyl-ene oligomerization. In the crystal, mutual pairs of N-H⋯O=P hydrogen bonds link two mol-ecules into a dimer with individual mol-ecules related by a twofold rotation axis. The P=O bond length of 1.

Isolation, characterization, and in silico, in vitro and in vivo antiulcer studies of isoimperatorin crystallized from Ostericum koreanum.

Context: Ostericum koreanum (Maxim.) Kitagawa (Apiaceae) roots are traditionally used as an analgesic and antiulcer agent. However, the antiulcer potential of isoimperatorin isolated from O.

Crystal structure of 2-(4-acetyl-anilino)-2-oxoethyl 3-(4-hy-droxy-phen-yl)propionate.

In the title compound, C19H19NO5, the amide carbonyl O atom is positioned anti to the other two carbonyl O atoms. The 4-hy-droxy-hydro-cinnamate fragment is disordered over two positions with an occupancy ratio of 0.729 (12):0.

Synthesis and crystal structures of the potential tyrosinase inhibitors N-(4-acetylphenyl)-2-chloroacetamide and 2-(4-acetylanilino)-2-oxoethyl cinnamate.

Substituted benzoic acid and cinnamic acid esters are of interest as tyrosinase inhibitors and the development of such inhibitors may help in diminishing many dermatological disorders. The tyrosinase enzyme has also been linked to Parkinson's disease. In view of hydroxylated compounds having ester and amide functionalities to potentially inhibit tyrosinase, we herein report the synthesis and crystal structures of two amide-based derivatives, namely N-(4-acetylphenyl)-2-chloroacetamide, C10H10ClNO2, (I), and 2-(4-acetylanilino)-2-oxoethyl cinnamate, C19H17NO4, (II).

Synthesis, structural elucidation and bioevaluation of 4-amino-1,2,4-triazole-3-thione's Schiff base derivatives.

In this study, a series of ten triazole Schiff base derivatives 6a-j were synthesized through microwave assisted imine formation by reacting substituted amino triazole 5 with different substituted aldehydes. All the synthesized compounds were evaluated for their inhibitory activity against mushroom tyrosinase. Two of the compounds 6a and 6b among the series 6a-j were found to be highly potent tyrosinase inhibitors with IC50 values of 10.

Photoluminescence properties of a cationic trinuclear zinc(II) complex with the tetradentate Schiff base ligand 6-methyl-2-({[(pyridin-2-yl)methyl]imino}methyl)phenolate.

Metal complexes with Schiff base ligands have been suggested as potential phosphors in electroluminescent devices. In the title complex, tetrakis[6-methyl-2-({[(pyridin-2-yl)methyl]imino}methyl)phenolato-1:2κ(8)N,N',O:O;3:2κ(8)N,N',O:O]trizinc(II) hexafluoridophosphate methanol monosolvate, [Zn3(C14H13N2O)4](PF6)2·CH3OH, the Zn(II) cations adopt both six- and four-coordinate geometries involving the N and O atoms of tetradentate 6-methyl-2-({[(pyridin-2-yl)methyl]imino}methyl)phenolate ligands. Two terminal Zn(II) cations adopt distorted octahedral geometries and the central Zn(II) cation adopts a distorted tetrahedral geometry.

Crystal structure of bis-[2-(benzo-thia-zol-2-yl)phenolato-κ(2) N,O]copper(II).

In the title complex, [Cu(C13H8NOS)2], the Cu(II) atom is coordinated by two N atoms and two O atoms from two bidentate benzo-thia-zolphenolate ligands, forming a distorted tetra-hedral geometry [dihedral angle between two N-Cu-O planes: 45.1 (2)°]. The dihedral angles between the benzo-thia-zole ring systems and the phenol rings are 4.

Crystal structure of bis-[2-(1H-benzimidazol-2-yl)aniline]silver(I) nitrate.

In the cation of the title salt, [Ag(C13H11N3)2]NO3, the Ag(I) atom lies on a crystallographic inversion center and is coordinated by four N atoms from two bidentate 2-(1H-benzimidazol-2-yl)aniline ligands in a distorted square-planar geometry. The Ag-N(aniline) bond [2.729 (2) Å] is significantly longer than the Ag-N(imidazole) bond [2.

Crystal structure of 2-[bis(1H-pyrazol-1-yl)meth-yl]pyridine.

The title compound, C12H11N5, was synthesized as a potential tridentate ligand to make catalytic metal complexes. The dihedral angle between the pyrazolyl rings is 67.9 (1)°.

Crystal structure of 5-hy-droxy-methyl-2-meth-oxy-phenol.

In the title compound, C8H10O3, the hy-droxy-methyl group is twisted by 74.51 (13)° from the plane of the benzene ring to which it is connected. By contrast, the benzene and meth-oxy groups are almost coplanar, making a dihedral angle of 4.

Crystal structure of aqua-bis-[2-(1H-benzimidazol-2-yl-κN (3))aniline-κN]zinc dinitrate.

The cation of the complex title salt, [Zn(C13H11N3)2(H2O)](NO3)2, lies about a twofold rotation axis, which passes through the Zn(II) atom and the O atom of the aqua ligand. The Zn(II) atom adopts a distorted trigonal-bipyramidal geometry defined by two N atoms in axial positions [angle = 166.24 (7)°], and two N and one O atom in the equatorial plane [range of angles: 115.

Crystal structure of catena-poly[[silver(I)-{μ-2,6-bis-[(1H-pyrazol-1-yl)meth-yl]pyridine-κ(3) N (1),N (2):N (2')}] nitrate].

In the title complex, {[Ag(C13H13N5)]NO3} n , the Ag(I) atom is coordinated by three N atoms from two bidentate/monodentate pyrazolylpyridyl ligands to form a distorted trigonal-planar geometry [range of angles: 83.34 (6) (chelate ring) to 139.15 (7) °].

Crystal structure of di-chlorido-{2,6-bis-[(3-phenyl-1H-pyrazol-1-yl)meth-yl]pyridine}cobalt(II).

In the title complex, [CoCl2(C25H21N5)], the Co(II) atom is coordinated by two Cl atoms and two N atoms, provided by a tridentate pyrazolylpyridyl ligand, forming a slightly distorted tetra-hedral geometry [range of angles: 96.51 (10) (chelate ring) to 118.60 (9)°].

Kinetic and in silico studies of novel hydroxy-based thymol analogues as inhibitors of mushroom tyrosinase.

The present studies reports the synthesis of hydoxylated thymol analogues (4a-e) and (6a-c) as mushroom tyrosinase inhibitors. The title compounds were obtained in good yield and characterized by FTIR, (1)H NMR, (13)C NMR, Mass spectral data and X-ray crystallography in case of compound (6a). The inhibitory effects on mushroom tyrosinase and DPPH were evaluated and it was observed that 2-[5-methyl-2-(propan-2-yl)phenoxy]-2-oxoethyl (2E)-3-(4-hydroxyphenyl)prop-2-enoate (6b) showed tyrosinase inhibitory activity (IC50 15.

Highly active chromium(III) complexes based on tridentate pyrazolyl pyridyl ligands for ethylene polymerization and oligomerization.

A set of new chromium(III) [Cr(III)] complexes based on the tridentate ligand HC(Pz)2Py (Pz = pyrazole; Py = pyridine) and its derivatives were prepared, characterized, and evaluated for ethylene polymerization/oligomerization. X-ray single-crystal analyses of the Cr(III) complexes showed tridentate coordination on the fac-octahedral Cr sphere. Upon activation with methylaluminoxane (MAO), the precatalysts and the ligands L1-L3 mixed in situ with Cr(acac)3 were highly active and generally produced polyethylene as a major product.

Crystal structure of bis-(4-allyl-2-meth-oxy-phen-yl) terephthalate.

The asymmetric unit of the title compound, C28H26O6, contains one half-mol-ecule, with the complete molecule generated by a crystallographic inversion center. The central terephthalate and meth-oxy-benzene rings are approximately perpendicular, making a dihedral angle of 80.31 (5)°.