Aminomethinylierung H-aktiver verbindungen in der reihe analgetischer wirkstoffe

Electrophilic attack of the active methylene group in 3-methyl-1-phenyl-5-pyrazolone (2) by s-triazine (1) leads to aminomethinylation of 2 with formation of 3-methyl-1-phenyl-4-aminomethylene-5-pyrazolone (4). Subsequent interaction of 4 with 2 explains the formation of 4,4′-methenyl-bis-[3-methyl-1-phenyl-5-pyrazolone (5). 1-Phenyl-3,5-pyrazolidinedione (6) reacts analogously with 1 forming 1-phenyl-4-aminomethylene-3,5-pyrazolidinedione (7). N,N′-Bis-indanyl-formamidine (9) results from the interaction of 2-amino-indane (8) with 1.     

Antimykotische wirkstoffe. VIII. Aufbau von dehydro-N-mannich-basen durch piperidin- und piperazinring

The three component reactions comprising the interaction of cyanamide ( 1 ) and s-triazine ( 2 ) with a secondary amine ( 5 ) leads to dehydro-N-Mannich bases ( 6 ). Of this compound class, 6a, b, and c exhibit antimycolic activity.     

1-Amino-adamantan als nucleophile substitutions-, additions- und ringspaltungskomponente : Antivirale wirkstoffe—VII

The ring cleavage occurring under the nucleophilic attack of 1-aminoadamantane (2) on s-triazine (1) leads to the formation of N,N′-bis-[1-adamantyl]-formamidine (5). 2 forms β-[2-furyl]-acrylic acid-[1-adamantyl]-amide (8) upon interacting with β-[2-furyl]-acrylic acid chloride (6). 8 exhibits remarkable antiviral activity.     

Neue chemotherapeutisch-aktive 4-trifluormethylpyrimidine

Condensation of N-(2-hydroxyethyl)-N-methylguanidine sulfate with various β-diketonesbearing 1,1,1-trifluoromethyl substituents leads to 2-[N-(2-hydroxyethyl)-methylamino]-4-trifluoromethylpyrimidine derivatives. These compounds exhibit antimycotic, trichomonazide and anti-HIV properties.     

Novel Concepts for the Immunological Detection of Bound Residues

Abstract

Immunoassays could be applied successfully to the determination of bound residues in soil and other complex matrices. Nevertheless, there was some doubt whether these assays could be regarded as quantitative and selective. We present some results, which imply that several approaches are quite promising. One approach is based on a non-competitive saturation immunoassay, which evens out the different cross-reactivities of the bound species. This may lead to a true molar sum value, which is not an equivalent concentration. For competitive assays, a method for the determination of the affinity constant(s) of the bound species is discussed. This would enable a correction for the cross-reactivity. The selectivity problem could be diminished very much, too. The application of special blocking reagents and the use of inhibition tests essentially solved the problem of non-specific binding (NSB). In addition, it could be proven experimentally that adsorbed analytes do not disturb the non-competitive assays, which have been suspected to be highly selective for covalently bound residues.     

ON THE SIGNAL-TRANSDUCTION CHAINS OF TWO Pfr- MEDIATED SHORT-TERM PROCESSES: INCREASE OF ANCHORAGE and MOVEMENT OF Mougeotia CHLOROPLASTS

Abstract— We examined two published hypotheses on the signal-transduction chain of the light-oriented chloroplast movements in the fresh-water alga Mougeotia. One hypothesis postulates a Ca²+-influx controlled by a tetrapolar gradient of phytochrome in its far-red light absorbing form (Pfr). The other hypothesis postulates anchorage sites for actin-filaments even at those areas of the plasmalemma where phytochrome is in its inactive form (Pr). Calmodulin and Ca²+-sequestering vesicles are assumed to be essential links of this transduction chain.
To test these hypotheses we have studied the effects of Ca²+-entry blockers, Ca²+ deficiency and calmodulin antagonists on chloroplast movements and on chloroplast anchorage. None of our results support the Ca²+/calmodulin hypotheses mentioned above. The results and their implications (with regard to the role of Ca²', calmodulin and anchorage sites) are discussed.     

The Optimal Shape of Riblets in the Viscous Sublayer

Our aim is to find the optimal shape of periodically distributed microstructures on surfaces of swimming bodies in order to reduce their drag. The model describes the flow in the viscous sublayer of the boundary layer of a turbulent flow. The microscopic optimization problem is reduced applying homogenization. In the reduced so-called macroscopic optimization problem we minimize the Navier constant subject to the boundary layer equations which are solved in a very small part of the original domain. Under the assumptions that the microstructures can be represented as smooth functions the sensitivity can be determined analytically. The optimization problem is then solved by a sensitivity based method (steepest descent with optimal step size) and the state equations are solved in each iteration with an external software. Our reduced model is validated by comparing the results from the homogenized model with those obtained by simulating the whole rough channel. An improved shape is found and a drag reduction up to 10% can be shown.