Basing on common chemical reactions, thin layer chromato graphy, absouptive ultraviolet spectrum some parameters were determined for preparation containing benzodiazepine in HCM City. The efficiency of extraction of benzodiazepan in 6 self made sample: Rhino sweet drink, coca-cola, combined food, soya milk, 333 beer and urine. Results found 17 active substances of diazepine group in 131 specialities of commercial propriatary name in HCM City, where diazepam had accounted higher rate in narcotic intoxixation cases. In criminal cases involved in tranquillisant narcotics, the most common substance were diazepan, flunitrazepan, clonazepan, bromazepan, alprazolam, clorazepat, oxazepan and nor-diazepan
Benzodiazepines ; Pharmaceutical Preparations ; Chemistry

AIMTo study the quantitative structure-activity relationship ( QSAR) of 23 tetrahydroimidazobenzodiazepinone (TIBO) as anti-HIV drug.

METHODSA newly developed three-dimensional holographic vector of atomic interaction field (3D-HoVAIF) was used to describe the chemical structure of anti-HIV drug-23 TIBO, a partial least square regression (PLS) model was built.

RESULTSThe obtained model with the cumulative multiple correlation coefficient (Rcum(2)), cumulative cross-validated (Qcum(2)) and standard error of estimation (SD) were Rcum(2) = 0. 824, Qcum(2) = 0.778 and SD = 0.56, respectively. The model had favorable estimation stability and good prediction capabilities.

CONCLUSIONSatisfactory results showed that 3D-HoVAIF with definite physic-chemical meanings and easy structural interpretation for structural characterization could preferably express information related to biological activity of TIBO.

Algorithms ; Anti-HIV Agents ; chemistry ; Benzodiazepines ; chemistry ; Holography ; methods ; Imidazoles ; chemistry ; Models, Molecular ; Quantitative Structure-Activity Relationship

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.
Analgesics, Opioid/analysis* ; Barbiturates/chemistry* ; Benzodiazepines/chemistry* ; Chromatography, Liquid/methods* ; Humans ; Hypnotics and Sedatives/chemistry* ; Micelles ; Reproducibility of Results ; Sensitivity and Specificity ; Solvents/chemistry* ; Surface-Active Agents/chemistry*

AIMDesign, synthesis and evaluation of a series of 7-imidazolylalkanamido-1-carboxylalkylbenzodiazepine farnesyltransferase (FTase) inhibitors.

METHODS AND RESULTSCoupling of imidazolylalkylcarboxylic acids and 1-substituted 7-aminobenzodiazepines (5a-5c) yielded 10 new compounds (6-12, 16-18) which were biologically tested against FTase using scintillation proximity assay method.

CONCLUSIONFive target compounds were found to be potential farnesyltransferase inhibitors.

Alkyl and Aryl Transferases ; antagonists & inhibitors ; drug effects ; Benzodiazepines ; chemical synthesis ; chemistry ; pharmacology ; Farnesyltranstransferase ; Imidazoles ; chemical synthesis ; chemistry ; pharmacology ; Inhibitory Concentration 50 ; Molecular Conformation ; Molecular Structure ; Structure-Activity Relationship

OBJECTIVES: To identify the new designer drugs which are totally unknown and not in the routine testing list by the technologies such as high-resolution mass spectrometry in drug facilitated sexual assault, in order to solve the problem in actual cases. METHODS: The milky fluid from an actual case was extracted and analyzed using LC-QE, ¹H-NMR and GC-MS, respectively. The accurate masses and cluster ions isotope patterns of unknown compound were obtained by LC-QE. The molecular formula was confirmed as C₁₆H₁₂C₂N₂O based on the protons number of ¹H-NMR. The isomers diclazepam and 4-chlorodiazepam were separated and detected with GC-MS. RESULTS: The new designer benzodiazepine as diclazepam in the milky fluid was identified. The results provided direct evidence for the investigation and qualitative analysis of such cases. CONCLUSIONS The combined application of various methods, including LC-QE, ¹H-NMR and GC-MS, can be used to detect unknown new psychoactive substances.
Benzodiazepines/chemistry* ; Benzodiazepinones ; Chromatography, Liquid/methods* ; Designer Drugs/chemistry* ; Female ; Gas Chromatography-Mass Spectrometry/methods* ; Humans ; Male ; Mass Spectrometry/methods* ; Sex Offenses ; Substance Abuse Detection/methods* ; Toxicology/methods*