90282-81-8Relevant articles and documents
Structure-Based Rationale Design and Synthesis of Aurantiamide Acetate Analogues - Towards a New Class of Potent Analgesic and Anti-inflammatory Agents
Suhas, Ramesh,Channe Gowda, Dase
, p. 850 - 862 (2012/06/04)
A series of new aurantiamide acetate analogues were synthesized by modifying its N-terminal substitution and the amino acid residue. The structure of all these compounds was established on the basis of analytical and spectral studies. All the new derivatives were evaluated in vivo for their analgesic activity by tail flick method in mice and anti-inflammatory activity against carrageenan-induced oedema in albino rats at different doses (25, 50 and 100mg/kg body weight). All the compounds exhibited significant pharmacological activity with no ulcerogenic liability. In particular, pentapeptides and tricosamers (30 amino acids) containing analogues have demonstrated high potency than the reference standards. These compounds hold promise for further development.
Kinetic studies on oxidation of Gly-Val-Gly, Gly-Phe-Ply and Ala-Val-Gly using Mn(III)
Gowda, B.K. Kempe,Rangappa,Gowda, D. Channe
, p. 1039 - 1044 (2007/10/03)
The fragments of elastin sequences, glycyl-valyl-glycine (GVG), glycyl-phenylalanyl-glycine (GFG) and alanyl-valyl-glycine (AVG) have been synthesized by classical solution phase method and characterized. Kinetics of oxidation of these tripeptides (TP) by Mn(III) has been studied in the presence of sulphate ions in acidic medium at 25°C. The reaction follows spectrophotometrically at Λmax 500 nm. A first order dependence of rate on both [Mn(III)] and [TP] has been observed. The rate is independent of concentrations of reduction product, Mn(II) and hydrogen ions. Effects of varying dielectric constant of the medium and addition of anions such as sulphate, chloride and perchlorate have been studied. Activation parameters have been evaluated using Arrhenius and Erying plots. The oxidation products are isolated and characterized. A tentative mechanism involving the reaction of TP with Mn(III) in the rate-limiting step is suggested. The effect of hydrophobicity of amino acids on the rate of oxidation is discussed.