Biginelli reaction of ethyl acetoacetate, thiourea and the appropriate aromatic aldehyde was used to produce ethyl 4-aryl-6-methyl-2-thioxo-1,2,3,4-tetrahydropyrimidine-5-carboxylates, that reacted with bromomalononitrile to give ethyl 3-amino-5-aryl-2-cyano-7-methyl-5H-thiazolo[3,2-a]pyrimidine-6-carboxylates rather than the isomeric 7H-thiazolo[3,2-a]pyrimidines. Thiazolopyrimidine derivative...

The curtius rearrangement of Ethyl 1 (2 – azido – 2 oxoethyl) – 6 – methyl – 2 – oxo – 4 – (3 – substituted) 1, 2, 3, 4 – tetrahydropyrimidine -5 – carboxylate prepared from the readily accessible 4 (1 – substituted) – 5 ethoxy carbonyl – 6 methyl] 3, 4 – dihydropyrimidine – 2 (1H) – one was investigated in presence of ethanol, substituted phenols and substituted amines. The resulting carbamate...

approved: T. Mark Zabriskie L-pipecolic acid (L-PA), a six carbon imino acid, is an intermediate of lysine degradation in various organisms including bacteria, yeast, fungi and mammals. In primates, the oxidation of L-PA by the enzyme L-pipecolate oxidase (L-PO) is the rate determining step of L-lysine degradation in the central nervous system. This thesis describes efforts to probe the L-PO me...

Many bacteria amass compatible solutes to fend-off the detrimental effects of high osmolarity on cellular physiology and water content. These solutes also function as stabilizers of macromolecules, a property for which they are referred to as chemical chaperones. The tetrahydropyrimidine ectoine is such a compatible solute and is widely synthesized by members of the Bacteria. Many ectoine produ...

Human neutrophil elastase (HNE) is a key protease for matrix degradation. High HNE activity is observed in inflammatory diseases. Accordingly, HNE is a potential target for the treatment of pulmonary diseases such as chronic obstructive pulmonary disease (COPD), acute lung injury (ALI), acute respiratory distress syndrome (ARDS), bronchiectasis (BE), and pulmonary hypertension (PH). HNE inhibit...