70462-58-7Relevant articles and documents
Synthesis of 5(S)-Methyl-L-Proline Containing Peptidomimetic Compounds and their In Vitro Evaluation for Dipeptidyl Peptidase-4 Inhibition
Gajjar, Anuradha K.,Pathak, Chirag D.
, p. 350 - 365 (2022/05/12)
Background: Type 2 diabetes mellitus (T2DM), which is the epidemic of the 21st century, has affected millions of people worldwide. Traditional methods available for the treatment are associated with various side effects. Among the newer therapies, DPP-4 (Dipeptidyl peptidase-4) inhibition has been a promising therapy for the past decade with the scope of further development, especially in peptidomimet-ics. Objective: 5(S)-methyl-L-proline containing peptidomimetic compounds were designed in the previous work. The designed compounds were synthesized and characterized by spectral methods, such as mass spectrometry,1H NMR, and13C NMR (Nuclear magnetic resonance) spectroscopy. The purity of the final compounds was determined by high-performance liquid chromatography (HPLC). The synthesized compounds were in vitro evaluated for their DPP-4 inhibitory activity. Methods: Compounds were peptide in nature and were synthesized using the conventional synthesis ap-proach, where peptide synthesis was done using an acid-amine coupling reagent. They were evaluated through fluorimetric enzyme-based assay using a DPP-4 inhibitor screening kit. Moreover, the CLARIO-star microplate reader instrument was used to measure fluorescence. Results: 5(S)-methyl-L-proline containing 13 compounds were synthesized. All of them were characterized for structural integrity using spectral methods. They had HPLC purity of more than 95% and were evaluated for DPP-4 inhibition. Compounds 1, 7, 10, 11, 14 and 17 were found to have good inhibition than others. These compounds were further evaluated at different concentrations to develop a linear corre-lation coefficient (R2). Conclusion: Six compounds were found to have good DPP-4 inhibition, hence it further opens the possi-bility of developing DPP-4 inhibitor-containing 5(S)-methyl-L-proline.
An improved route for the synthesis of Rolloamide B
Elagawany, Mohamed,Ibrahim, Mohamed A.
supporting information, p. 3837 - 3840 (2016/08/02)
A high yielding method for the synthesis of the cyclic heptapeptide Rolloamide B has been described. An effective isobutyl chloroformate (IBCF) mediated direct coupling reaction was introduced to improve the synthetic route towards Rolloamide B. Furthermo
Design and synthesis of tryptophan containing peptides as potential analgesic and anti-inflammatory agents
Suhas,Gowda, D.Channe
scheme or table, 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.
