A new indolizinium alkaloid from marine-derived Streptomyces sp. HNA39.

A new indolizinium alkaloid, named as cyclizidine J (1), was identified from Gause's liquid fermentation of marine-derived Streptomyces sp. HNA39. Its structure was elucidated by extensive NMR spectroscopic methods, HRESIMS data, and ECD calculations. To our best knowledge, compound 1 was a unique cyclizidine-type alkaloid that contain a chlorine atom substituted at position C-8. Unfortunately, biological evaluation of 1 exhibited no active against PC-3 cancer cell line, BRD4, and ROCK2 protein kinase.

Fluoroquinolone derivatives and their anti-tubercular activities.

Tuberculosis (TB) remains one of the most widespread and leading deadliest diseases, around one-third of the world's population harbor a latent infection by Mycobacterium tuberculosis (MTB), and 5-10% eventually develop an active TB. The emergency of MTB new virulent forms as well as the co-infection between MTB and HIV alarming the serious problem in TB control and demanding the need for new drugs more potent than earlier with safe ADME profile. Fluoroquinolones are emerged as a large family of synthetic broad spectrum antibiotics, and some of them were recommended as the second-line agents for the treatment of TB mainly in cases involving resistance or intolerance to first-line anti-TB therapy by WHO. Numerous of FQs derivatives have been synthesized for seeking for new anti-TB agents, and some of them exhibited promising potency. This review aims to summarize the recent advances made towards the discovery of FQs derivatives as anti-TB agents and the structure-activity relationship of these derivatives.

Antiplasmodial and antimalarial activities of quinolone derivatives: An overview.

Malaria remains one of the most deadly infectious diseases globally. Considering the growing spread of resistance, development of new and effective antimalarials remains an urgent priority. Quinolones, which are emerged as one of the most important class of antibiotics in the treatment of various bacterial infections, showed potential in vitro antiplasmodial and in vivo antimalarial activities, making them promising candidates for the chemoprophylaxis and treatment of malaria. This review presents the current progresses and applications of quinolone-based derivatives as potential antimalarials to pave the way for the development of new antimalarials.

[A retrospective analysis of 97 drunk driving cases].

OBJECTIVE: Based on a retrospective analysis of the drunk driving cases, to explore the drunk drivers' personnel composition, occurrence time and psychology. METHODS: As a result of punishment of the drunk driving by criminal law for one year from May 1st, 2011 to April 30th, 2012, 91 drunk driving cases were statistically analyzed the easy-happening time of drunk driving, the drunk drivers' age, gender, occupational characteristics, domicile and psychological factors. RESULTS: In 97 drunk driving cases, 26-40 years old, non-local domiciled and non-professional male drivers were prone to drunk driving at night from 22:00 to 5:00. CONCLUSION: The behavior of drunk driving is relevant to time, age, genders and occupation. The psychological characteristics of most drivers are fluky, making-life-easy, competitive and peacockish.

[Progress on suxamethonium chloride analysis].

Abstract: Suxamethonium chloride is a depolarizing muscle relaxant used in general anesthesia. In overdose, it causes adverse reactions such as bradycardia, arrhythmia, cardiac arrest, and death. The article reviews the progress on testing methods of suxamethonium chloride such as infrared spectroscopy, chemical color reaction, chemical titration, enzyme electrode, chromatography and mass spectrometry.

[Micellar liquid chromatography and its application in toxicological analysis].

Micellar liquid chromatography (MLC) is a reversed phase liquid chromatography with mobile phases containing surfactant above its critical micellar concentration (CMC). The basic mechanism and advantages of MLC in physicochemical analysis were reviewed, and its applications in analysis of drugs, barbiturates, benzodiazepines were chiefly introduced in this paper. MLC is a potential method to toxicological analysis due to strong selectivity, wide application scope and easy biological samples, etc.

(E)-Methyl N'-[1-(2-hydroxy-phen-yl)ethyl-idene]hydrazinecarboxyl-ate.

The mol-ecule of the title compound, C(10)H(12)N(2)O(3), adopts a trans configuration with respect to the C=N bond. The dihedral angle between the benzene ring and the hydrazinecarboxyl-ate plane is 8.98 (7)°. Intra-molecular O-H⋯N and C-H⋯N hydrogen bonds are observed. Mol-ecules are linked into chains along the c axis by N-H⋯O hydrogen bonds. In addition, C-H⋯π inter-actions are observed.

3-(3-Chloro-prop-yl)-7,8-dimeth-oxy-2,3,4,5-tetra-hydro-1H-3-benzazepin-2-one at 125 K.

In the title compound, C(15)H(20)ClNO(3), the seven-membered ring adopts a distorted boat-sofa conformation; the methyl-ene C atoms of this ring are coplanar with the benzene ring. Both meth-oxy groups are almost coplanar with the attached benzene ring [C-C-O-C = 6.5 (2) and -13.5 (3)°]. An intra-molecular C-H⋯O hydrogen bond is observed in the mol-ecular structure. In the crystal structure, a C-H⋯π inter-action involving the benzene ring is observed.

3-(3-Chloro-prop-yl)-7,8-dimeth-oxy-1H-3-benzazepin-2(3H)-one at 125†K.

In the title compound, C(15)H(18)ClNO(3), the seven-membered ring has a mirror plane passing through the methyl-ene C atom and bis-ecting the C=C bond. It adopts a bent conformation, inter-mediate between the boat and chair forms. Both meth-oxy groups are coplanar with the attached benzene ring [C-C-O-C = -0.5 (3) and 2.2 (3)°]. In the crystal structure, inversion-related mol-ecules are linked via C-H⋯O hydrogen bonds and π-π inter-actions involving the benzene ring [centroid-centroid distance = 3.6393 (12)Å].

2-(1-Adamant-yl)-4-bromo-anisole at 123†K.

IN THE TITLE COMPOUND [SYSTEMATIC NAME: 2-(1-adamantyl)-4-bromo-1--methoxy-benzene], C(17)H(21)BrO, two weak intra-molecular C-H⋯O hydrogen bonds influence the mol-ecular conformation. The crystal packing exhibits C-H⋯π inter-actions, with a relatively short inter-molecular C⋯Cg contact of 3.568 (5) Å, where Cg is the centroid of the benzene ring. The crystal studied exhibited inversion twinning.

(E)-Methyl N'-(4-hydroxy-benzyl-idene)hydrazinecarboxyl-ate.

In the title compound, C(9)H(10)N(2)O(3), the hydroxy group and the C=N-N unit are coplanar with the benzene ring. The benzene rings of inversion-related mol-ecules are stacked with their centroids separated by a distance of 3.7703 (9) Å, indicating weak π-π inter-actions. In the crystal structure, C-H⋯O, O-H⋯O, N-H⋯O and C-H⋯O hydrogen bonds link molecules into a infinite two-dimensional network along the a axis.

1-Acetyl-5,6-dimethoxy-indoline at 123 K.

In the title compound, C(12)H(15)NO(3), all C, N and O atoms lie in a mirror plane. An intramolecular C-H⋯O hydrogen bond is present.

Methyl N'-[(E)-1-phenyl-ethyl-idene]hydrazinecarboxyl-ate.

The mol-ecule of the title compound, C(10)H(12)N(2)O(2), adopts a trans configuration with respect to the C=N bond. The dihedral angle between the phenyl ring and the hydrazine carboxylic acid mean plane is 25.23 (9)°. In the crystal structure, mol-ecules are linked into chains by N-H⋯O hydrogen bonds and C-H⋯π inter-actions.

Ethyl N'-[(E)-4-hydroxy-benzyl-idene]hydrazinecarboxyl-ate at 123†K.

The mol-ecule of the title compound, C(10)H(12)N(2)O(3), adopts a trans configuration with respect to the C=N bond. The dihedral angle between the benzene ring and the hydrazinecarboxyl-ate plane is 14.6 (1)°. Mol-ecules are linked into a three-dimensional network by O-H⋯O, N-H⋯O and C-H⋯O hydrogen bonds, and by C-H⋯π inter-actions.

Methyl N'-[(E)-4-hydr-oxy-3-methoxy-benzyl-idene]hydrazinecarboxyl-ate.

The mol-ecule of the title compound, C(10)H(12)N(2)O(4), adopts a trans configuration with respect to the C=N double bond. The dihedral angle between the benzene ring and the hydrazinecarboxyl-ate mean plane is 36.54 (6)°. The mol-ecules are linked into a two-dimensional network by inter-molecular O-H⋯O, N-H⋯O and O-H⋯N hydrogen bonds, and by aromatic π-π stacking inter-actions [ring-centroid separation 3.7689 (9) Å].

(E)-Methyl N'-(4-bromo-benzyl-idene)-hydrazinecarboxyl-ate at 123 K.

The title compound, C(9)H(9)BrN(2)O(2), crystallizes with two independent but essentially identical mol-ecules in the asymmetric unit. Each mol-ecule adopts a trans configuration with respect to the C=N bond. In one of the mol-ecules, the dihedral angle between the benzene ring and the hydrazinecarboxylic acid plane is 24.9 (2)°, and that in the other mol-ecule is 16.1 (2)°. The mol-ecules are linked into a three-dimensional network via inter-molecular N-H⋯O, C-H⋯O, C-H⋯N and C-H⋯Br hydrogen bonds. An intramolecular N-H⋯O hydrogen bond is also present.

(E)-Methyl N'-(2-hydroxy-benzyl-idene)-hydrazinecarboxyl-ate at 123 K.

In the title mol-ecule, C(9)H(10)N(2)O(3), the hydrazinecarboxylic acid mean plane and the benzene ring form a dihedral angle of 11.1 (1)°. In the crystal structure, inter-molecular N-H⋯O hydrogen bonds link the mol-ecules into chains extending along the b axis. An intra-molecular O-H⋯N hydrogen bond is also present.