121148-01-4Relevant articles and documents
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
Antibacterial and anti-TB tat-peptidomimetics with improved efficacy and half-life
Bhosle, Govind S.,Nawale, Laxman,Yeware, Amar M.,Sarkar, Dhiman,Fernandes, Moneesha
supporting information, p. 358 - 369 (2018/05/22)
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.
An ionic liquid containing L-proline moiety as highly efficient and recyclable chiral organocatalyst for Michael addition
Li, Jiang,Li, Xia Bing,Ma, Sha Sha,Liu, Juan,Li, Ben Hao,Li, Bao Lin
, p. 1259 - 1264 (2016/08/12)
A novel chiral ionic liquid containing proline moiety was synthesized. It can be used as a highly efficient and recyclable chiral organocatalyst for Michael addition of cyclohexanone with (E)-β-nitroalkenes in methanol at room temperature. The Michael add