The reaction of furylacrylic acid with cyclopentadiene in toluene gave the expected Diels-Alder endo-and exo-adductsin -1 : 1 ratio. The adducts were separated by iodolactonization method to provide 3-endo-(2'-furyl) bicyclo 12.2.11 hept-5-ene- 2-exo-carboxylic acid and 3-exo-(2'-fury1)bicyclo 12.2.11 hept-5-ene-2-endocarboxylic acid. Esterification of these acids by MeI / HMPA gave the exp...

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...

Reaction of thionyl chloride with 7-chloro-1-cyclopropyl-6-fluoro-1,4-dihydro-4- oxoquinoline-3-carboxylic acid 1 gave acid chloride 2. Compound 2 was reacted with glycine and D-glutamic acid to afford 2-(7-chloro-1-cyclopropyl-6-fluoro-4-oxo-1,4- dihydroquinoline-3-carbonyl) aminopantandioicacid 3a and 2-(7-chloro-1-cyclopropyl-6- fluoro -4- oxo-1,4-dihydroquinoline-3-carbonyl)aminoacetica...

We discovered on the chromosome of Saccharomyces cerevisiae Sigma 1278b novel genes involved in L-proline analogue L-azetidine-2-carboxylic acid resistance which are not present in the standard laboratory strains. The 5.4 kb-DNA fragment was cloned from the genomic library of the L-azetidine-2-carboxylic acid-resistant mutant derived from a cross between S. cerevisiae strains S288C and Sigma 12...

A new fluorescent sensor based on a dimethylxanthene skeleton has beensynthesized. Because of its oxyanion hole structure, this receptor includes a suitablecavity for the association of carboxylic acids. The receptor's fluorescence is quenchedupon addition of dinitrobenzoic acid.

We recently reported the identification of a novel human adenosine A3 receptor-selective agonist, (2S,3S,4R,5R)-3-amino-5-[6-[5-chloro-2-(3-methylisoxazol-5-ylmethoxy)benzylamino]purin-9-yl]-4-hydroxytetrahydrofuran-2-carboxylic acid methylamide (CP-608,039), with 1,260-fold selectivity for the human A3 versus human A1 receptor (DeNinno et al., J Med Chem 46: 353-355, 2003). However, because th...

Partial agonists produce submaximal activation of ligand-gated ion channels. To address the question of partial agonist action at the NR1 subunit of the NMDA receptor, we performed crystallographic and electrophysiological studies with 1-aminocyclopropane-1-carboxylic acid (ACPC), 1-aminocyclobutane-1-carboxylic acid (ACBC), and 1-aminocyclopentane-1-carboxylic acid (cycloleucine), three compou...

In the title compound, C(12)H(13)ClO(4), the 1,3-dioxane ring adopts a chair conformation and the 2-chloro-benzene and methyl substituents occupy equatorial sites. The carboxyl group is in an axial inclination. In the crystal, carb-oxy-lic acid inversion dimers linked by pairs of O-H⋯O hydrogen bonds generate R(2) (2)(8) loops.