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1.
Arzneimittelforschung ; 51(4): 304-9, 2001.
Article in English | MEDLINE | ID: mdl-11367871

ABSTRACT

The synthesis and antiviral activity of original dibromoimidazo[1,2-a]pyridines bearing a thioether side chain are reported. Molecular modeling was used to identify biophoric structural patterns that are common to 16 compounds. Structure-activity relationship (SAR) studies identified hydrophobicity (logP) as the most important factor for activity. From these SAR studies, the antiviral activity could be predicted.


Subject(s)
Antiviral Agents/chemical synthesis , Antiviral Agents/pharmacology , Imidazoles/chemical synthesis , Imidazoles/pharmacology , Pyridines/chemical synthesis , Pyridines/pharmacology , Anti-HIV Agents/chemical synthesis , Anti-HIV Agents/pharmacology , Antineoplastic Agents/chemical synthesis , Antineoplastic Agents/pharmacology , Giant Cells/drug effects , Giant Cells/virology , HIV-1/drug effects , Humans , Magnetic Resonance Spectroscopy , Models, Molecular , Molecular Conformation , Quantitative Structure-Activity Relationship
2.
J Org Chem ; 65(20): 6572-5, 2000 Oct 06.
Article in English | MEDLINE | ID: mdl-11052104

ABSTRACT

The influence of base and solvent in Suzuki cross-coupling reaction on various 2-substituted-3-iodoimidazo[1,2-a]pyridines was reported. The reactivity was largely influenced by nature of the substituent. Optimized yields and shortened times of reaction were obtained using strong bases in DME.


Subject(s)
Cyclooxygenase Inhibitors/chemical synthesis , Pyridines/chemical synthesis , Boronic Acids/chemistry , Cyclooxygenase Inhibitors/chemistry , Pyridines/chemistry
3.
Chem Pharm Bull (Tokyo) ; 48(7): 935-40, 2000 Jul.
Article in English | MEDLINE | ID: mdl-10923819

ABSTRACT

From a pharmacophore model of bicyclic heterocycles as aromatase inhibitors we have designed three series of imidazo[1,2-a]pyridine derivatives. The synthesis and the spectroscopy determination of various compounds are reported. The crystal data of one of these compounds (10b) was obtained. The aromatase inhibition potency was evaluated in vitro and no activity was found.


Subject(s)
Aromatase Inhibitors , Enzyme Inhibitors/chemical synthesis , Imidazoles/chemical synthesis , Pyridines/chemical synthesis , Enzyme Inhibitors/chemistry , Enzyme Inhibitors/pharmacology , Imidazoles/chemistry , Imidazoles/pharmacology , Molecular Conformation , Pyridines/chemistry , Pyridines/pharmacology , X-Ray Diffraction
4.
Planta ; 182(3): 415-9, 1990 Oct.
Article in English | MEDLINE | ID: mdl-24197193

ABSTRACT

Gas exchanges of wheat (Triticum aestivum L. cv. Courtot) shoots were measured before and during a water stress. While photosynthesis, transpiration and dark respiration decreased because of the stress, photorespiration increased initially, up to a maximum of 50% above its initial value. The CO2 concentration in the intercellular space was calculated from gas-diffusion resistances, and remained approximately constant before and during the stress. On the other hand, the CO2 concentration in the chloroplast, in the vicinity of Ribulose-1,5-biphosphate carboxylase/oxygenase (Rubisco), was evaluated from the ratio of CO2 to O2 uptake, using the known kinetic constants of the oxygenation and carboxylation reactions which compete for Rubisco. In the well-watered plants, the calculated chloroplastic concentration was slightly smaller than the substomatal concentration. During water stress, this concentration decreased while the substomatal CO2 concentration remained constant. Hypotheses to explain this difference between substomatal and chloroplastic CO2 concentrations are discussed.

5.
Adv Space Res ; 9(8): 111-6, 1989.
Article in English | MEDLINE | ID: mdl-11537379

ABSTRACT

Studies for every level of CELSS: Waste processing, food production, photosynthesis system, and so on ..., imply an automatic system to control, command and quantify gases, water and chemical compounds. Used for many years in plant physiology studies, the C23A system monitors the analysis and quantifies gases (O2, CO2. N2, ...), physical parameters (temperature, humidity, ...) and chemical compounds (NH4+, N03-, ...) on numerous experiments. In the new version, the architecture of the computing system is near of the space requirements. We have chosen a structure with three independent levels: acquisition, monitoring and supervision. Moreover, we use multiplexed analysers: IRGA, mass spectrometer and cheminal analyser. The multiplexing increases the accuracy of the measurements and could facilitate the spatialization. Thus the whole structure anticipates the entire separation between automation in space and control-command on ground.


Subject(s)
Computer Communication Networks , Ecological Systems, Closed , Life Support Systems/instrumentation , Space Flight/instrumentation , Systems Integration , Automation/methods , Carbon Dioxide/metabolism , Computer Systems , Environmental Monitoring , Plant Physiological Phenomena
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