[Effects of H102 on the memory recognition ability and AMPK-mTOR autophagy-related pathway in AD mice].

OBJECTIVE: To study the effect of ß-sheet blocking peptide H102 on the expression of AMPK-mTOR autophagy pathway-related protein in APP/PS1 double transgenic AD mice. METHODS: Thirty male APP/PS1 transgenic male AD mice of 6 months old were randomly divided into AD group and H102 intervention group, and C57BL/6J male mice of the same age were used as control group (n=15). The mice in the HF group were administered with 5 µl (5.8 mg/kg) of H102 polypeptide solution through the nasal cavity at the same time period, and the mice in the control group and the AD group were given the same amount of blank adjuvant solution daily. The memory recognition ability was tested by a new object recognition experiment 30 days after continuous administration. Immunohistochemistry and Western blot were used to detect the expressions of phosphorylated AMP-activated protein kinase(P-AMPK),phosphorylated mammalian target of rapamycin (P-mTOR) and ratio of LC32to LC31(LC3II/I )in brain tissue. RESULTS: Compared with the control group, the new object recognition index (RI) of the AD group was significantly lower (P＜0.05), and the P-AMPK and LC3II/I ratios in the brain of the mice were significantly lower (P＜0.05). The expression of P-mTOR protein was increased significantly (P＜0.05). Compared with the AD group, the RI of the H102 intervention group was increased significantly (P＜0.05), and the P-AMPK and LC3II/I ratios in the brain tissue of the mice were increased significantly (P＜0.05). The expression of P-mTOR protein was decreased significantly (P＜0.05). CONCLUSION: H102 can improve the recognition and memory ability of AD mice by activating the AMPK-mTOR autophagy-related pathway.

NH3⋠H2O: The Simplest Nitrogen-Containing Ligand for Selective Aerobic Alcohol Oxidation to Aldehydes or Nitriles in Neat Water.

Aqueous ammonia (NH3⋅H2O) has been shown to serve as the simplest nitrogen-containing ligand to effectively promote copper-catalyzed selective alcohol oxidation under air in water. A series of alcohols with varying electronic and steric properties were selectively oxidized to aldehydes with up to 95 % yield. Notably, by increasing the amount of aqueous ammonia in neat water, the exclusive formation of aryl nitriles was also accomplished with good-to-excellent yields. Additionally, the catalytic system exhibits a high level of functional group tolerance with -OH, -NO2, esters, and heteroaryl groups all being amenable to the reaction conditions. This one-pot and green oxidation protocol provides an important synthetic route for the selective preparation of either aldehydes or nitriles from commercially available alcohols.

Research progress of optic neuritis epidemiology / 国际眼科杂志(Guoji Yanke Zazhi)

Optic neuritis is one of the most important neuro-ophthalmologic diseases which cause vision loss in young adults. There are obvious differences in the prevalence of optic neuritis in different countries and regions. Through the review of the related literature at home and abroad in recent years, this article summarizes the etiology and epidemiological characteristics of optic neuritis. lt is expected to provide reference and comparison for the epidemiological investigation of cross regional, multi-center cooperation.

Benzyl (E)-3-(2-methyl-benzyl-idene)dithio-carbazate.

The title compound, C(16)H(16)N(2)S(2), was obtained from the condensation reaction of benzyl dithio-carbazate and 2-methyl-benzaldehyde. The asymmetric unit contains two independent mol-ecules. In both mol-ecules, the methyl-phenyl ring and the dithio-carbazate fragment are located on opposite sides of the C=N bond, showing an E conformation. In each mol-ecule, the dithio-carbazate fragment is approximately planar, the r.m.s deviations being 0.018 and 0.025 Å. The mean plane of dithio-carbazate group is oriented at dihedral angles of 7.9 (3) and 68.24 (12)°, respectively, to the methyl-phenyl and phenyl rings in one mol-ecule, while the corresponding angles in the other mol-ecule are 10.9 (3) and 69.76 (16)°. Inter-molecular N-H⋯S hydrogen bonding occurs in the crystal structure to generate inversion dimers for both molecules.

(E)-N'-[1-(Thio-phen-2-yl)ethyl-idene]benzohydrazide.

The title compound, C(13)H(12)N(2)OS, was obtained from the condensation reaction of 2-acetyl-thio-phene and benzohydrazide. In the mol-ecule, the formohydrazide fragment is approximately planar (r.m.s deviation = 0.0146 Å) and the mean plane is oriented at dihedral angles of 24.47 (11) and 28.86 (13)°, respectively, to the phenyl and thio-phene rings. The thio-phene and phenyl rings make a dihedral angle of 53.21 (8)°. The benzamide fragment and thio-phene ring are located on the opposite sides of the C=N bond, showing an E conformation. Classical inter-molecular N-H⋯O hydrogen bonds and weak C-H⋯O inter-actions are present in the crystal structure: three such bonds occur to the same O-atom acceptor.

Catalyst-free preparation of 1,2,4,5-tetrasubstituted imidazoles from a novel unexpected domino reaction of 2-azido acrylates and nitrones.

A highly efficient and convenient method for the synthesis of 1,2,4,5-tetrasubstituted imidazoles from readily accessible 2-azido acrylates and nitrones has been developed. This reaction proceeded under mild conditions without the assistance of any metal, acid, or base.

Benzyl 3-[(E)-1-(pyrazin-2-yl)ethyl-idene]dithio-carbazate.

The title compound, C(14)H(14)N(4)S(2), was obtained from a condensation reaction of benzyl dithio-carbazate and acetyl-pyrazine. The asymmetric unit contains two independent mol-ecules, in each of which the pyrazine ring and dithio-carbazate unit are approximately co-planar, the r.m.s. deviations being 0.0304 and 0.0418 Å. The mean plane is oriented with respect to the benzene ring at 49.22 (4)° in one mol-ecule and at 69.76 (7)° in the other. In the crystal, the mol-ecules are linked to each other via inter-molecular N-H⋯S hydrogen bonds, forming centrosymmetric supra-molecular dimers.

Benzyl 3-[(E)-2-nitro-benzyl-idene]dithio-carbazate.

The title compound, C(15)H(13)N(3)O(2)S(2), was obtained from a condensation reaction of benzyl dithio-carbazate and 2-nitro-benzaldehyde. In the mol-ecule, the nearly planar dithio-carbazate fragment [r.m.s deviation = 0.0264 Å] is oriented at dihedral angles of 7.25 (17) and 74.09 (9)°with respect to the two benzene rings. The nitro group is twisted by a dihedral angle of 22.4 (7)° to the attached benzene ring. The nitro-benzene ring and dithio-carbazate fragment are located on the opposite sides of the C=N bond, showing an E configuration. In the crystal, mol-ecules are linked via inter-molecular N-H⋯S hydrogen bonds, forming centrosymmetric supra-molecular dimers. Weak C-H⋯π inter-action is also observed in the crystal structure.

(E)-Benzaldehyde (2,4,6-trichloro-phen-yl)hydrazone.

The title compound, C(13)H(9)Cl(3)N(2), was obtained from a condensation reaction of benzaldehyde and 2,4,6-trichloro-phenyl-hydrazine. The mol-ecule assumes an E configuration with the phenyl ring and trichloro-phenyl ring located on opposite sides of the C=N bond. The phenyl ring is oriented at a dihedral angle of 42.58 (12)° with respect to the tricholorophenyl ring. In the crystal, the mol-ecules are linked via N-H⋯N hydrogen bonds, forming supra-molecular chains running along the c axis. π-π stacking is present between parallel trichloro-phenyl rings of adjacent mol-ecules, the face-to-face and centroid-centroid distances being 3.369 (14) and 3.724 (2) Å, respectively.

Methyl (E)-3-(2-bromo-4,5-dimeth-oxy-benzyl-idene)dithio-carbazate.

The title compound, C(11)H(13)BrN(2)O(2)S(2), was obtained from the condensation reaction of methyl dithio-carbazate and 2-bromo-4,5-dimeth-oxy-benzaldehyde. In the mol-ecule, the benzene ring and dithio-carbazate fragment are located on opposite sides of the C=N bond, showing an E conformation. The dithio-carbazate fragment is approximately planar (r.m.s deviation = 0.0281 Å) and the mean plane is oriented at a dihedral angle of 11.38 (15)° with respect to the benzene ring. In the crystal, pairs of N-H⋯S hydrogen bonds link the mol-ecules into centrosymmetric dimers.

Benzyl (E)-3-(4-meth-oxy-benzyl-idene)dithio-carbazate.

The title compound, C(16)H(16)N(2)OS(2), was obtained from a condensation reaction of benzyl dithio-carbazate and 4-meth-oxy-benzaldehyde. In the mol-ecule, the meth-oxy-phenyl ring and dithio-carbazate fragment are located on opposite sides of the C=N double bond, showing an E configuration. The dithio-carbazate fragment is approximately planar (r.m.s. deviation = 0.0052 Å); its mean plane is oriented at dihedral angles of 8.19 (15) and 85.70 (13)°, respectively, to the meth-oxy-phenyl and phenyl rings. Inter-molecular N-H⋯S hydrogen bonds and weak C-H⋯π inter-actions are observed in the crystal structure.

Benzyl (E)-3-(2-bromo-5-meth-oxy-benzyl-idene)dithio-carbazate.

The title compound, C(16)H(15)BrN(2)OS(2), was obtained from the condensation reaction of benzyl dithio-carbazate and 2-bromo-5-meth-oxy-lbenzaldehyde. In the mol-ecule, the bromo-meth-oxy-phenyl ring and dithio-carbazate fragment are located on the opposite sides of the C=N double bond, showing the E conformation. The dithio-carbazate fragment is approximately planar (r.m.s deviation 0.0187 Å); its mean plane is oriented with respect to the bromo-meth-oxy-phenyl and phenyl rings at 7.60 (12) and 60.08 (9)°, respectively. In the crystal, inversion dimers linked by pairs of N-H⋯S hydrogen bonds occur. A short Br⋯Br contact of 3.5526 (12) Šis observed in the crystal structure.

3-Chloro-N-(4-hydr-oxy-3-methoxy-benz-yl)-2,2-dimethyl-propanamide.

In the mol-ecular structure of the title compound, C(13)H(18)ClNO(3), the amide group is nearly perpendicular to the benzene ring, making a dihedral angle of 85.66 (9)°. The C=O bond distance of 1.242 (3) Šand the C-N bond distance of 1.333 (3) Šsuggest electron delocalization in the amide fragment. Inter-molecular O-H⋯O and N-H⋯O hydrogen bonding helps to stabilize the crystal structure.

(E)-3-(3-Chloro-phen-yl)-N-(4-hy-droxy-3-meth-oxy-benz-yl)acryl-amide.

In the title compound, C(17)H(16)ClNO(3), the 4-hy-droxy-3-meth-oxy-benzyl group is planar [maximum atomic deviation = 0.0138 (16) Å] and is nearly perpendicular to the chloro-benzene ring, making a dihedral angle of 84.67 (4)°. The chloro-benzene and amide groups are located on the opposite sides of the C=C bond, showing an E configuration. The relatively long C=O bond distance of 1.2364 (19) Šand the short C-N bond distance of 1.341 (2) Šsuggest electron delocalization in the amide fragment. Inter-molecular O-H⋯O, N-H⋯O and weak C-H⋯O hydrogen bonding is present in the crystal structure.

N-(4-Hydr-oxy-3-methoxy-benz-yl)benzamide.

In the mol-ecular structure of the title compound, C(15)H(15)NO(3), the two benzene rings are twisted with respect to each other, making a dihedral angle of 75.11 (10)°. In the amide fragment, the C=O and C-N bond distances are 1.248 (3) and 1.321 (3) Å, respectively, indicating electron delocalization. A partially ovelapped arrangement between parallel hydroxy-methoxy-benzene rings is observed in the crystal structure, and the face-to-face distance of 3.531 (16) Šsuggests the existence of weak π-π stacking. N-H⋯O and O-H⋯O hydrogen bonding is also present in the crystal structure.

N'-[(E)-3-Indol-3-ylmethyl-ene]isonicotino-hydrazide monohydrate.

Crystals of the title compound, C(15)H(12)N(4)O·H(2)O, were obtained from a condensation reaction of isonicotinylhydrazine and 3-indolylformaldehyde. The mol-ecule assumes an E configuration, with the isonicotinoylhydrazine and indole units located on the opposite sites of the C=N double bond. In the mol-ecular structure the pyridine ring is twisted with respect to the indole ring system, forming a dihedral angle of 44.72 (7)°. Extensive classical N-H⋯N, N-H⋯O, O-H⋯O and O-H⋯N hydrogen bonding and weak C-H⋯O inter-actions are present in the crystal structure.

Benzyl 3-[(E)-benzyl-idene]dithio-carbazate.

Crystals of the title compound, C(15)H(14)N(2)S(2), were obtained from a condensation reaction of benzyl dithio-carbazate and benzaldehyde. The mol-ecule assumes an E configuration about the N=C double bond. The phenyl ring of the thio-ester group is nearly perpendicular to the dithio-carbazate plane, with a dihedral angle of 84.60 (5)°. In the crystal structure, inter-molecular N-H⋯S hydrogen bonding links adjacent mol-ecules to form a centrosymmetric supra-molecular dimer.

Methyl 3-[(E)-1-(4-amino-phen-yl)ethyl-idene]dithio-carbazate.

The title compound, C(10)H(13)N(3)S(2), was obtained from a condensation reaction of methyl dithio-carbazate and 4-amino-acetophenone. In the crystal structure, the nearly planar mol-ecule assumes an E configuration, the benzene ring and dithio-carbazate group being located on opposite sides of the N=C bond. C-H⋯π inter-actions and N-H⋯S hydrogen bonding are present in the crystal structure.

Benzyl 3-[(E)-furfuryl-idene]dithio-carbazate.

In the title compound, C(13)H(12)N(2)OS(2), the mol-ecule assumes an E configuration, with the furan ring and dithio-carbazate units located on opposite sides of the N=C double bond. In the crystal structure, mol-ecules are linked via two inter-molecular N-H⋯S hydrogen bonds to form centrosymmetric dimers.

(E)-2-Furyl methyl ketone 2,4-dinitro-phenyl-hydrazone.

Crystals of the title compound, C(12)H(10)N(4)O(5), were obtained from a condensation reaction of 2,4-dinitro-phenyl-hydrazine and 2-furyl methyl ketone. The mol-ecule displays a nearly planar structure, and the furan ring is slightly twisted by a dihedral angle of 12.62 (6)° with respect to the phenyl-hydrazone plane. The face-to-face separation of 3.287 (7) Šbetween parallel benzene rings of adjacent mol-ecules indicates the existence of π-π stacking between dinitro-phenyl rings in the crystal structure.