90282-81-8Relevant academic research and scientific papers
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.
Design and synthesis of tryptophan containing peptides as potential analgesic and anti-inflammatory agents
Suhas,Gowda, D.Channe
, p. 535 - 540 (2012/09/22)
A new series of smaller peptides with tryptophan at C-terminal and varying N-protected amino acids/peptides were designed, synthesized and characterized by analytical and spectroscopic techniques. Analgesic and anti-inflammatory properties of these peptides were carried out in vivo using tail-flick method and carrageenan-induced paw edema method, respectively, at different doses and different time intervals. Most of the peptides synthesized displayed enhanced activity, and particularly tetra and hexapeptides 29-31 were found to be even more potent than the reference standards used. Moreover, some peptides have exhibited promising activity even after 24h of administration, whereas the reference standards were active only up to 3h. Further, the compounds did not present any ulcerogenic liability.
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.
Studies of Bitter Peptides from Casein Hydrolyzate. IV. Relationship between Bitterness and Hydrophobic Amino Acids Moiety in the C-Terminal of BPIa (Arg-Gly-Pro-Pro-Phe-Ile-Val)
Otagiri, Ken,Shigenaga, Toshiaki,Kanehisa, Hidenori,Okai, Hideo
, p. 90 - 96 (2007/10/02)
In the synthetic studies of bitter peptide BPIa (Arg-Gly-Pro-Pro-Phe-Ile-Val), we sythesized several BPIa analogs to elucidate the participation of the hydrophobic amino acids moiety in the C-terminal in the bitter taste exhibited by BPIa.The syntheses of
