42280-29-5Relevant articles and documents
Gram-Scale Synthesis of a Hexapeptide by Fragment Coupling in a Ball Mill
Lamaty, Frédéric,Métro, Thomas-Xavier,Martinez, Jean,Rguioueg, Nadia,Subra, Gilles,Yeboue, Yves
supporting information, (2021/09/20)
Synthesis of long peptides is generally considered as a challenge to peptide chemists, in addition to producing significant amounts of toxic waste, such as DMF. Here we show that using solvent-less methods, such as ball milling, enabled the production of
Synthesis, binding affinities and metabolic stability of dimeric dermorphin analogs modified with β3-homo-amino acids
Fraczak, Oliwia,Lasota, Anika,Tymecka, Dagmara,Kosson, Piotr,Muchowska, Adriana,Misicka, Aleksandra,Olma, Aleksandra
, p. 222 - 227 (2016/04/19)
In this study, proteinogenic amino acids residues of dimeric dermorphin pentapeptides were replaced by the corresponding β3-homo-amino acids. The potency and selectivity of hybrid α/β dimeric dermorphin pentapeptides were evaluated by competeti
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
experimental part, 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.
