Synthesis and evaluation of alkoxy-phenylamides and alkoxy-phenylimidazoles as potent sphingosine-1-phosphate receptor subtype-1 agonists

In the design of potent and selective sphingosine-1-phosphate receptor agonists, we were able to identify two series of molecules based on phenylamide and phenylimidazole analogs of FTY-720. Several designed molecules in these scaffolds have demonstrated selectivity for S1P receptor subtype 1 versus 3 and excellent in vivo activity in mouse. Two molecules PPI-4621 (4b) and PPI-4691 (10a), demonstrated dose responsive lymphopenia, when administered orally.     

Weathering of Granite from the Damma Glacier Area: The Contribution of Cyanogenic Bacteria

The dissolution potential of five cyanogenic bacteria was studied at 25°C during 32 days using granite material from the Damma glacier (Central Alps, Switzerland) as the sole source of nutrients. The bacterial species Pseudomonas fluorescens and Pseudomonas sp. CCOS 191 were the most effective to exudate various organic acids and consequently mobilized Fe. The molecular mechanisms include both, proton-promoted and ligand-promoted dissolution, preferentially at pH below 5 and in the pH range between 5.0 and 5.8, respectively. In addition, bacterially produced cyanide plays a minor role through the formation of soluble hexacyanoferrate complexes. To our knowledge, this study is the first that reveals the direct measurement of metal-cyanide complexes formed during biotic granite weathering.     

Choice of Smoothing Parameters for Direct Kernels in Discrimination

Direct kernels, due to LAUDER (1983), as an alternative to the indirect kernel method in discriminant analysis are considered. It is shown that direct kernels may be based on any kernel function known in discrete density estimation. The choice of smoothing parameters is based on general loss functions and a family of loss functions which are specific for the discrimination problem is introduced. Examples with distance dependent and distance independent smoothing parameters are given to illustrate the applicability.     

Cloning of the genes encoding urease from Proteus vulgaris and sequencing of the structural genes

A fragment of chromosomal DNA from proteus vulgaris encoding urease was cloned and expressed in Escherichia coli. A 3 kbp region was sequenced and revealed three open reading frames with homology to jack bean (Canavalia ensiformis) urease. The smallest protein (11 kDa) was homologous to the N-terminus of the plant enzyme and the largest polypeptide (61 kDa) corresponded to the C-terminus. The large protein contained conserved regions and a cysteine residue which is known to be catalytically important in the plant enzyme. A protein of 12 kDa showed homology to residues 132 to 237 of jack bean urease.     

Rye bread and synthetic bread odorants – effective trap bait and lure for German cockroaches

Bread‐in‐beer and bread‐in‐water are prevalent home recipe trap baits for attracting German cockroaches (GCRs), Blattella germanica (L.) (Dictyoptera: Blattellidae), which are significant urban pests. Our objectives were to (1) test the attractiveness of these baits, (2) study the underlying factors of GCR attraction, and (3) determine whether a blend of synthetic bread odorants could replace bread in a trap lure. In large‐arena laboratory experiments with laboratory‐reared GCR males, traps baited with rye bread not only captured eightfold more males than unbaited control traps but also most males released into bioassay arenas. Neither beer nor water enhanced the attractiveness of bread. Bread crust as a bait was more effective than bread crumbs. As Porapak Q headspace volatile extracts of rye bread attracted GCRs, all rye bread odorants in extracts were identified by gas chromatography‐mass spectrometry. Synthetic rye bread odorants and other known bread odorants were then assembled into a master blend. This master blend, and even partial blends lacking certain groups of organic volatiles such as aldehydes and ketones, proved very attractive to GCRs. We conclude that rye bread could be used as an effective bait in retainer traps or, laced with insecticide, as a food source in bait stations. A lure of synthetic bread odorants may eventually replace bread as bait, but the minimum number of essential odorants for that lure has yet to be determined.