Three-Dimensional Structure of Recombinant Thermophilic Ribokinase from Thermus speсies 2.9 in Complex with Adenosine Diphosphate

Crystallography Reports - The three-dimensional structure of recombinant thermophilic ribokinase from Thermus speсies 2.9 was determined at 2.4 Å resolution using crystals, which were...     

Microwave-assisted three-component synthesis of 7-aryl-2-alkylthio-4,7-dihydro-1,2,4-triazolo[1,5-a]-pyrimidine-6-carboxamides and their selective reduction

Multicomponent reactions (MCRs) and microwave-assisted organic synthesis (MAOS) have been used as key methods for the synthesis of fused dihydropyrimidine derivatives. The three-component condensation of 3-amino-5-alkylthio-1,2,4-triazoles with aromatic aldehydes and acetoacetamides under microwave irradiation was developed as a rapid and efficient solution-phase method for the high-yielding preparation of 7-aryl-2-alkylthio-4,7-dihydro-1,2,4-triazolo[1,5-a]pyrimidine-6-carboxamide libraries. In addition, the selective reduction of the formed dihydrotriazolopyrimidines to trans-trans-2-alkylthio-7-aryl-4,5,6,7-tetrahydro-1,2,4-triazolo[1,5-a]pyrimidine-6-carboxamides was established. The described synthetic protocols provide rapid access to novel and diversely substituted dihydroazolopyrimidine libraries.     

Ultrasonic-promoted three-component synthesis of some biologically active 1,2,5,6-tetrahydropyrimidines

Multicomponent reactions and organic synthesis with ultrasonic activation have been used as key methods for the synthesis of tetrahydropyrimidine derivatives. The three-component condensation of 1,3-diarylprop-2-en-1-one with ammonia and aldehydes/acetone or N-substituted gamma-pyridones under ultrasonic irradiation was developed as a rapid and efficient solution-phase method for the high-yielding preparation of 2-aryl(hetaryl)-4,6-diaryl-1,2,5,6-tetrahydropyrimidines and 2,4-diaryl-1,5,9-triazaspiro[5.5]undec-1-enes. The described synthetic protocol provides rapid access to novel and diversely substituted tetrahydropyrimidines libraries. The simple, primary biological screening showed 98% of inhibitory activity against Mycobacterium tuberculosis for one of tetrahydropyrimidines synthesized.     

Sura-wind radar: Studies of nonlinear effects using VHF-wave occultion of the ionosphere

We present experimental results on reception of VHF signals of the transmitting facility “Sura” of the Radiophysical Research Institute by the NASA spacecraft WIND. The experiments were performed during daytime during the summer seasons 1997–1998. The dependence of power and spectral characteristics of the VHF radio waves on the power of the sounding radiation is analyzed. We find that, in a wide range of effective powers of the VHF radiation from about 40 kW to 160 MW, the phenomena observed in the radiation received onboard WIND (such as focusing, scintillations, or frequency deviations of signals) does not usually depend on the operation mode of the “Sura” facility. At the same time, broadening of the radiation pattern of the facility and decrease of the mean level of the received signal by about 6 dB toward the direction of maximum of the radiation pattern were observed at the peak radiation power of the facility. The experimental results are compared to present concepts on effects of self-focusing instability and nonlinear defocusing of VHF radio waves in the ionospheric plasma. Translated from Izvestiya Vysshikh Uchebnykh Zavedenii, Radiofizika, Vol. 42, No. 8, pp. 799–809, August 1999.     

Calix[4]arene alpha-aminophosphonic acids: asymmetric synthesis and enantioselective inhibition of an alkaline phosphatase

[structure: see text] Chiral calix[4]arene alpha-aminophosphonic acids were obtained through diastereoselective Pudovik-type addition of sodium ethyl phosphites to the chiral calixarene imines, removal of chiral auxiliary groups, and mild dealkylation of phosphonate fragments. The diacids obtained show inhibitory activity toward porcine kidney alkaline phosphatase that depends considerably on the absolute configuration of the alpha-carbon atoms.     

Features of 3-amino-5-methylisoxazole in heterocyclizations involving pyruvic acids

Chemistry of Heterocyclic Compounds - The chemical properties of 3-amino-5-methylisoxazole in the reactions involving pyruvic acid derivatives are reported. The multicomponent condensation of...