Effects of passive smoking and its duration on the prevalence of prediabetes and type 2 diabetes mellitus in Chinese women.

Several studies have shown that active smoking is a risk factor for type 2 diabetes mellitus (T2DM). However, the effects of passive smoking on T2DM remains unknown. In this study, we investigated the effects of passive smoking and its duration on the prevalence of prediabetes and T2DM. According to passive smoking status, participants were divided into Group A (passive smokers) and Group B (controls). Furthermore, Group A was divided into three subgroups according to the duration of passive smoking: Group A1 (≤10 years), Group A2 (10-20 years), and Group A3 (>20 years). We found that the prevalence of impaired glucose tolerance (IGT) in Group A (26.6%), Group A2 (28%), and Group A3 (37.8%) was significantly higher than that in Group B (19.6%), and the prevalence gradually increased with an increase in the duration of passive smoking. Multiple logistic regression analysis showed that passive smoking for >10 years was a risk factor for impaired fasting glucose (IFG), IGT, and T2DM. Therefore, passive smoking not only increases the prevalence of IGT in a time-dependent manner, but also a risk factor for IFG, IGT, and T2DM when its duration is over 10 years.

Crystal structure of 9-(4-bromo-but-yl)-9H-fluorene-9-carb-oxy-lic acid.

The title compound, C18H17BrO2, is a key inter-mediate in the synthesis of lomitapide mesylate, a microsomal triglyceride transfer protein inhibitor. Its asymmetric unit contains two independent mol-ecules with slightly different conformations; the mean planes of the 4-bromo-butyl and carboxyl-ate groups in the two mol-ecules form dihedral angles of 24.54 (12) and 17.10 (18)°. In the crystal, carboxyl-ate groups are involved in O-H⋯O hydrogen bonding, which leads to the formation of two crystallographically independent centrosymmetric dimers. Weak inter-molecular C-H⋯O inter-actions further link these dimers into layers parallel to the bc plane.

Synthesis and biological evaluation of substituted desloratadines as potent arginine vasopressin V2 receptor antagonists.

Twenty-one non-peptide substituted desloratadine class compounds were synthesized as novel arginine vasopressin receptor antagonists from desloratadine via successive acylation, reduction and acylation reactions. Their structures were characterized by 1H-NMR and HRMS, their biological activity was evaluated by in vitro and in vivo studies. The in vitro binding assay and cAMP accumulation assay indicated that these compounds are potent selective V2 receptor antagonists. Among them compounds 1n, 1t and 1v exhibited both high affinity and promising selectivity for V2 receptors. The in vivo diuretic assay demonstrated that 1t presented remarkable diuretic activity. In conclusion, 1t is a potent novel AVP V2 receptor antagonist candidate.

5-(2-Cyano-benz-yl)-4,5,6,7-tetra-hydro-thieno[3,2-c]pyridin-2-yl acetate.

In the title mol-ecule, C17H16N2O2S, the tetra-hydro-pyridine ring exhibits a half-chair conformation. The mean planes of the ester chain and benzene ring are twisted by 5.5 (1) and 81.32 (5)°, respectively, from the plane of thio-phene ring. In the crystal, weak C-H⋯O inter-actions link mol-ecules related by translation along [100] into chains.

5-(2-Chloro-benz-yl)-4,5,6,7-tetra-hydro-thieno[3,2-c]pyridin-2-yl acetate.

In the title compound, C(16)H(16)ClNO(2)S, the benzene and thio-phene rings make a dihedral angle of 72.60 (4)°. In the crystal, weak C-H⋯O inter-actions are observed.

1,3-Dimethyl-1H-indazol-6-amine.

The mol-ecular skeleton of the title compound, C(9)H(11)N(3), is almost planar, with a maximum deviation of 0.0325 (19) Šfor the amino N atom. In the crystal, N-H⋯N hydrogen bonds establish the packing.

1-(4,5,6,7-Tetra-hydro-thieno[3,2-c]pyridin-5-yl)-2-{4-[3-(trifluoro-meth-yl)phen-yl]piperazin-1-yl}ethanone.

In the title mol-ecule, C(20)H(22)F(3)N(3)OS, the piperazine ring has a chair conformation, and the N-C(=O)-C-N torsion angle is -59.42 (14)°. In the crystal, weak C-H⋯O and C-H⋯π inter-actions link the mol-ecules into layers parallel to (101).

Methyl 5-chloro-2-nitro-benzoate.

In the title compound, C(8)H(6)ClNO(4), the nitro and acet-oxy groups attached to the benzene ring at neighbouring positions are twisted from its plane by 29.4 (1) and 49.7 (1)°, respectively. In the crystal, weak C-H⋯O hydrogen bonds link mol-ecules into layers parallel to (101). The crystal packing exhibits short inter-molecular C⋯O distances of 2.925 (3) Å.

2-[4-(4-Methylphenylsulfonyl)piperazin-1-yl]-1-(4,5,6,7-tetrahydrothieno[3,2-c]pyridin-5-yl)ethanone.

In the title thienopyridine derivative, C(20)H(25)N(3)O(3)S(2), the piperazine ring exhibits a chair conformation and the tetra-hydro-pyridine ring exhibits a half-chair conformation. The folded conformation of the mol-ecule is defined by the N-C-C-N torsion angle of -70.20 (2) °. Inter-molecular C-H⋯S and C-H⋯O hydrogen bonds help to establish the packing.

2-(Thio-phen-2-yl)ethyl 4-methyl-benzene-sulfonate.

In the title mol-ecule, C(13)H(14)O(3)S(2), the thio-phene and benzene rings form a dihedral angle of 13.86 (13)°. In the crystal, weak inter-molecular C-H⋯O hydrogen bonds link the mol-ecules into layers parallel to the ab plane.

Synthesis and antihistamine evaluations of novel loratadine analogues.

A series of loratadine analogues containing hydroxyl group and chiral center were synthesized. The effect of the synthesized compounds on the histamine-induced contractions of guinea-pig ileum muscles was studied. In addition, the in vivo asthma-relieving effect of the analogues in the histamine induced asthmatic reaction in guinea-pigs was determined. Most of the compounds exhibited definite H(1) antihistamine activity. The S-enantiomers, compounds 2, 4 and 8, are more potent than the R-enantiomers, compounds 1, 3 and 7. Compound 6 was the most active one among the eight synthesized compounds.

2'-Carb-oxy-meth-oxy-4,4'-bis-(3-methyl-but-2-en-yloxy)chalcone.

In the title compound, C(27)H(30)O(6), also known as sofalcone, an anti-ulcer agent used for the protection of gastric mucosa-, the two benzene rings form a dihedral angle of 6.78 (11)°. Inter-molecular O-H⋯O hydrogen bonds link the mol-ecules into centrosymmetric dimers, which are further linked by weak C-H⋯O inter-actions into ribbons propagated in [2[Formula: see text]0]. Finally, π-π inter-actions between the benzene rings [centroid-centroid distance = 3.583 (13) Å] stabilize the crystal packing.

1-(2-Nitro-benz-yl)-1H-pyrrole-2-carbaldehyde.

In the title compound, C(12)H(10)N(2)O(3), the five- and six-membered rings form a dihedral angle of 83.96 (6)°. The nitro group is twisted by 5.92 (8)° from the plane of the attached benzene ring. In the crystal, weak inter-molecular C-H⋯O hydrogen bonds link the mol-ecules into columns in the [100] direction, with a short distance of 3.725 (3) Šbetween the centroids of benzene rings inside these columns.

N-(5-Ethylsulfanyl-1,3,4-thiadiazol-2-yl)-2-(4,5,6,7-tetrahydrothieno[3,2-c]pyri-din-5-yl)acetamide.

In the title compound, C(13)H(16)N(4)OS(3), a thienopyridine-derivative, the tetra-hydro-pyridine ring exhibits a half-chair conformation, and the folded conformation of the mol-ecule is defined by the N-C-C-N torsion angle of -78.85 (16)°. The crystal packing features inter-molecular C-H⋯N, N-H⋯N and C-H⋯O hydrogen bonds.

2-Methyl-6-nitro-2H-indazole.

In the title compound, C(8)H(7)N(3)O(2), the mol-ecular skeleton is almost planar with a maximum deviation of 0.0484 (9) Šfor the methyl C atom. In the crystal, weak inter-molecular C-H⋯N and C-H⋯O hydrogen bonds help to establish the packing.

1-[4-(3-{[5-(4-Chloro-phen-yl)furan-2-yl]methyl-idene-amino}-2,5-dioxoimidazol-idin-1-yl)but-yl]-4-methyl-piperazine-1,4-diium dichloride hemihydrate.

The title compound, C(23)H(30)ClN(5)O(3) (2+)·2Cl(-)·0.5H(2)O, was synthesized by N-alkyl-ation of 1-({[5-(4-chloro-phen-yl)-2-furan-yl]methyl-ene}amino)-2,4-imidazolidinedione with 1-bromo-4-chloro-butane, and N-methyl-piperazine. In the crystal, the cations, anions and water mol-ecules are linked by O-H⋯Cl and N-H⋯Cl hydrogen bonds.

[Synthesis of thienopyridine derivatives and its anti-platelet activity in vivo].

To explore novel ADP receptor inhibitors with anti-thrombotic activity, eighteen compounds were synthesized and their structures were confirmed by 1H NMR and MS. The results showed that the activity of compound C1 was superior to ticlopidine in platelet aggregation inhibition tests in vivo and worthy for further investigation. Compounds A4, B2, C4 and C7 possessed moderate platelet aggregation inhibitory activities.

1-[4-(4-Nitro-phen-yl)piperazin-1-yl]-2-(4,5,6,7-tetra-hydro-thieno[3,2-c]pyridin-5-yl)ethanone.

The title compound, C(19)H(22)N(4)O(3)S, comprises a thienopyridine moiety which is characteristic for anti-platelet agents of the clopidogrel class of compounds. In the crystal, inversion dimers are formed through pairs of C-H⋯O inter-actions. The benzene ring plane and the nitro plane are almost coplanar, with a dihedral angle of 0.83 (2)°. The piperazine ring adopts a chair conformation.

N-(2-Chloro-pyrimidin-4-yl)-N,2-di-methyl-2H-indazol-6-amine.

In the title compound, C(13)H(12)ClN(5), which is a derivative of the anti-tumor agent pazopanib {systematic name: 5-[[4-[(2,3-di-methyl-2H-indazol-6-yl)methylamino]-2-pyrimidinyl]amino]-2-methylbenzolsulfonamide}, the indazole and pyrim-idine fragments form a dihedral angle of 62.63 (5)°. In the crystal, pairs of mol-ecules related by twofold rotational symmetry are linked into dimers through π-π inter-actions between the indazole ring systems [centroid-centroid distance = 3.720 (2) Å]. Weak inter-molecular C-H⋯N hydrogen bonds further assemble these dimers into columns propagated in [001].

(R)-[1-(2-Chloro-phen-yl)-2-meth-oxy-2-oxoeth-yl][2-(thio-phen-2-yl)eth-yl]ammonium (+)-camphor-10-sulfonate acetone monosolvate.

The title compound, C(15)H(17)ClNO(2)S(+)·C(10)H(15)O(4)S(-)·C(3)H(6)O, was synthesized by N-alkyl-ation of α-amino-(2-chloro-phen-yl)acetate with 2-thienylethyl p-toluene-sulfonate, followed by reaction with (+)-camphor-10-sulfonic acid. In the crystal, the cations and anions are linked through N-H⋯O hydrogen bonds. The thio-phene ring of the cation was found to be disordered over two sites, with refined occupancies of 0.798 (4) and 0.202 (4).