Possible role of some groups in the structure and function of HIV-1 protease as revealed by molecular modeling studies

AbstractRetroviral proteases belong to the class of aspartic proteases. A molecular model of HIV-1 protease has been built on the basis of the consensus template specific for the domains of these enzymes. The template region comprises more than a half of the HIV-1 protease monomer structure, it includes the active site, formed at the junction of the two monomers, binding pockets of the enzyme, and some other molecular segments. These regions can be more conveniently described than other parts of the structure. Some properties of the HIV-1 protease molecule are discussed, as well as of probable inhibitors. The properties of the model structure are in good agreement with the recent results of crystallographic studies of Rous sarcoma virus protease

Fragmentation and Multifragmentation of 10.6A GeV Gold Nuclei

We present the results of a study performed on the interactions of 10.6A GeV gold nuclei in nuclear emulsions. In a minimum bias sample of 1311 interac- tions, 5260 helium nuclei and 2622 heavy fragments were observed as Au projec- tile fragments. The experimental data are analyzed with particular emphasis of target separation interactions in emulsions and study of criticalexponents. Multiplicity distributions of the fast-moving projectile fragments are inves- tigated. Charged fragment moments, conditional moments as well as two and three -body asymmetries of the fast moving projectile particles are determined in terms of the total charge remaining bound in the multiply charged projectile fragments. Some differences in the average yields of helium nuclei and heavier fragments are observed, which may be attributed to a target effect. However, two and three-body asymmetries and conditional moments indicate that the breakup mechanism of the projectile seems to be independent of target mass. We looked for evidence of critical point observable in finite nuclei by study the resulting charged fragments distributions. We have obtained the values for the critical exponents gamma, beta and tau and compare our results with those at lower energy experiment (1.0A GeV data). The values suggest that a phase transition like behavior, is observed.Comment: latex, revtex, 28 pages, 12 figures, 3tables, submitted to Europysics Journal

Synthesis and pesticidal activity of 1,2,3,4-tetrahydroquinoline derivatives

Some new 4-methyl-1,2,3,4-tetrahydroquinolines containing propyl, phenyl and pyridyl radicals at the C-2 position were synthesized from readily available N-aryl-N-alkenylamines. The latter and the tetrahydroquinolines obtained were tested for bactericidal, fungicidal, and herbicidal activities. Among the tetrahydroquinolines tested, those containing an α-, Β-, or γ-pyridyl substituent have found to be most potent as fungicides. © 1995, Plenum Publishing Corporation. All rights reserved

Synthesis and pesticidal activity of 1,2,3,4-tetrahydroquinoline derivatives

Some new 4-methyl-1,2,3,4-tetrahydroquinolines containing propyl, phenyl and pyridyl radicals at the C-2 position were synthesized from readily available N-aryl-N-alkenylamines. The latter and the tetrahydroquinolines obtained were tested for bactericidal, fungicidal, and herbicidal activities. Among the tetrahydroquinolines tested, those containing an α-, Β-, or γ-pyridyl substituent have found to be most potent as fungicides. © 1995, Plenum Publishing Corporation. All rights reserved

SYNTHESIS AND BIOLOGICAL-ACTIVITY OF 1,2,5-TRIMETHYL-4-N-ARYLIMINO(AMINO)PIPERIDINES AND 4-(N-ARYL-N-ETHOXYCARBONYL)AMINOPIPERIDINES

Some urethanes containing gamma-N-piperidyl substituents were synthesized fron the respective 4-N-arylimino(amino)piperidines and ethylchloroformate. The starting materials and the resultant ethyl-N-(1,2,5-trimethylpiperidyl-4)-N-aryl (hetaryl) carbamates were tested for bactericidal, fungicidal, and herbicidal activities which were shown to be related to the structure of the compounds in question. Some ethyl-N-(1,2,5-trimethylpiperidyl-4)-N-aryl-carbamates had action on the central nervous system. The compounds under study had no profound analgetic effect. The structure of the compounds was evidenced by spectral assays. The parameters for NMR- and mass-spectra are also outlined

Synthesis and biological activity of 1,2,5-trimethyl-4-N-arylimino)amino)- and 4-(N-aryl-N-ethoxycarbonyl)aminopiperidines

[No abstract available

Synthesis and biological activity of 1,2,5-trimethyl-4-n-arylimino (amino)- and 4-(N-aryl-N-ethoxycarbonyl)-aminopiperidines

[No abstract available

SYNTHESIS AND BIOLOGICAL-ACTIVITY OF 1,2,5-TRIMETHYL-4-N-ARYLIMINO(AMINO)PIPERIDINES AND 4-(N-ARYL-N-ETHOXYCARBONYL)AMINOPIPERIDINES

Some urethanes containing gamma-N-piperidyl substituents were synthesized fron the respective 4-N-arylimino(amino)piperidines and ethylchloroformate. The starting materials and the resultant ethyl-N-(1,2,5-trimethylpiperidyl-4)-N-aryl (hetaryl) carbamates were tested for bactericidal, fungicidal, and herbicidal activities which were shown to be related to the structure of the compounds in question. Some ethyl-N-(1,2,5-trimethylpiperidyl-4)-N-aryl-carbamates had action on the central nervous system. The compounds under study had no profound analgetic effect. The structure of the compounds was evidenced by spectral assays. The parameters for NMR- and mass-spectra are also outlined

Synthesis and biological activity of 1,2,5-trimethyl-4-N-arylimino)amino)- and 4-(N-aryl-N-ethoxycarbonyl)aminopiperidines

[No abstract available