1018667-18-9Relevant articles and documents
Synthesis of enantiopure 1-azaspiro[4.5]dec-6-en-8-ones from l-proline derivatives
Diaba, Faiza,Ricou, Eva,Bonjoch, Josep
, p. 1437 - 1443 (2006)
An enantioselective synthesis of protected 1-azaspiro[4.5]dec-6-en-8-one derivatives was achieved using an alkylidene carbene 1,5-CH insertion reaction as the key step.
Discovery of a series of novel compounds with moderate anti-hepatitis C virus NS3 protease activity in vitro
Shi, Fangyuan,Zhang, Yingjie,Xu, Wenfang
, p. 5539 - 5545 (2015)
The hepatitis C virus (HCV) NS3/4A protease that plays an important role in the viral life cycle has been proven to be an excellent target for the discovery of anti-HCV drugs. Enlightened by some P2-triazole and amide compounds, which had been found as HCV NS3 protease inhibitors, we designed and synthesized a series of novel compounds by incorporating different amino acid residues in P1/P1′ and P3/P3′ position to develop novel antiviral agents. The result of enzyme inhibition assay indicated that all the designed compounds showed moderate anti-HCV NS3 protease activity. On the basis of the biological result, a detailed structure-activity relationship (SAR) was derived and discussed.
Exploration of labeling by near infrared dyes of the polyproline linker for bivalent-type CXCR4 ligands
Nomura, Wataru,Aikawa, Haruo,Taketomi, Shohei,Tanabe, Miho,Mizuguchi, Takaaki,Tamamura, Hirokazu
, p. 6967 - 6973 (2015)
We have previously used poly-l-proline linkers for the development of bivalent-type ligands for the chemokine receptor, CXCR4. The bivalent ligands with optimum linkers showed specific binding to CXCR4, suggesting the existence of CXCR4 possibly as a dime
Importance of ring puckering versus interstrand hydrogen bonds for the conformational stability of collagen
Erdmann, Roman S.,Wennemers, Helma
, p. 6835 - 6838 (2011)
Mismatch is fine: Proline derivatives with a ring pucker mismatching that of natural collagen but with favorable torsional angles along the peptide chain are readily tolerated within the collagen triple helix (see picture). In contrast, a competition between intramolecular and interstrand H bonds destabilizes the collagen triple helix. Copyright
Antibacterial and anti-TB tat-peptidomimetics with improved efficacy and half-life
Bhosle, Govind S.,Nawale, Laxman,Yeware, Amar M.,Sarkar, Dhiman,Fernandes, Moneesha
, p. 358 - 369 (2018)
Non-natural antimicrobial peptides are ideal as next-generation antibiotics because of their ability to circumvent the problems of drug resistance and in vivo instability. We report novel all-α- and α,γ-mixed Tat peptide analogues as potential antibacterial and anti-TB agents. These peptides have broad spectrum antibacterial activities against Gram-positive (MICs 0.61 ± 0.03 to 1.35 ± 0.21 μM with the peptide γTatM4) and Gram-negative (MICs 0.71 ± 0.005 to 1.26 ± 0.02 μM with γTatM4) bacteria and are also effective against active and dormant forms of Mycobacterium tuberculosis, including strains that are resistant to rifampicin and isoniazid. The introduction of the non-natural amino acids of the study in the Tat peptide analogues results in increased resistance to degradation by proteolysis, significantly increasing their half-life. The peptides appear to inhibit bacteria by a membrane disruption mechanism, and have only a low cytotoxic effect on mammalian cells.
MELANOCORTIN-4 RECEPTOR AGONISTS
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Paragraph 91-94, (2021/05/15)
The present invention relates to a compound exhibiting excellent agonist activity against melanocortin receptors. More specifically, the present invention relates to a compound of Formula 1, a pharmaceutical composition comprising the compound as an activ
