Pseudomonas aeruginosa strain 1001 produces an esterase (EstA) that can hydrolyse the racemic methyl ester of β-acetylthioisobutyrate to produce the (D)-enantiomer, which serves as a precursor of captopril, a drug used for treatment of hypertension. We show here that PA2949 from P. aeruginosa PA01, a homologue of EstA, can efficiently be expressed in an enzymatically active form in E. coli. The...

The title compound, C(33)H(29)N(3)O(5), was synthesized by the reaction of racemic trans-2-benzyl-3-(2-fur-yl)-1-oxo-1,2,3,4-tetra-hydro-isoquinoline-4-carboxylic acid, l-tryptophan methyl ester and diisopropylcarbodiimide in dry dichloro-methane. The furan ring is disordered over two positions in a 0.859 (14):0.141 (14) ratio. In the 1,2,3,4-tetra-hydro-iso-quin-oline ring system, the heterocy...

The title compound, C(11)H(23)NO(5)P(+)·I(-), consists of an eight-membered cationic heterocyclic ring in a boat-chair conformation. The ring features a tetra-alkyl-ammonium N and a methyl-phospho-nate P atom. A -CH(2)(CO)OC(2)H(5) ester side chain at the C adjacent to oxygen produces two chiral centers at that substituted C atom and the P atom, both of which were determined to have absolute R,...

The L,L-Phe-Leu-Cu(II), L,L-Leu-Phe-Cu(II), L,L-Phe-Met-Cu(II), and L,L-Met-Phe-Cu(II) systems were studied using molecular modelling. The results obtained, which are in good agreement with results obtained by potentiometric studies show a significant increase in stability of copper complexes, when an aromatic residue is located in C-terminal (compared to the L,L-dipeptides containing the same ...

The relaxant effect of the methyl ester of rosuvastatin was evaluated on aortic rings from male Wistar rats (250-300 g, 6 rats for each experimental group) with and without endothelium precontracted with 1.0 µM phenylephrine. The methyl ester presented a slightly greater potency than rosuvastatin in relaxing aortic rings, with log IC50 values of -6.88 and -6.07 M, respectively. Unlike rosuvasta...

The crystal structures of several designed peptide hairpins have been determined in order to establish features of molecular conformations and modes of aggregation in the crystals. Hairpin formation has been induced using a centrally positioned (D)Pro-Xxx segment (Xxx = (L)Pro, Aib, Ac6c, Ala; Aib = α-aminoisobutyric acid; Ac6c = 1-aminocyclohexane-1-carboxylic acid). Structures of the peptides...

The synthesis of racemic and enantiomerically pure N-p-methylbenzyl-3- and N-p-chlorobenzylbenzamidoquinuclidinium bromides (6-8 and 9-11, respectively) is described. These compounds were prepared from racemic or enantiomerically pure 3-benzamidoquinuclidines 3-5 using the appropriate quaternization reagents: p-methyl- benzyl bromide (1) and p-chlorobenzyl bromide (2).