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📜L-Norleucine Methyl Ester置于三乙胺,Lithium Hydroxide体系中,用 四氢呋喃,二氯甲烷,水 作为反应溶剂,化学反应 5.08H,反应生成 N-苄氧羰基-L-己氨酸
参考文献:新型二肽型 Sars-Cov 3Cl 蛋白酶抑制剂的设计,合成和生物学评价:构效关系研究
标题:新型二肽型 Sars-Cov 3Cl 蛋白酶抑制剂的设计,合成和生物学评价:构效关系研究
摘要:这项工作描述了低分子量肽 Sars-Cov 3Cl 蛋白酶抑制剂的设计,合成和评估.抑制剂的设计基于有效的三肽 Z-Val-Leu-Ala(Pyrrolidone-3-yl)-2-Benzothiazole (8 ; Ki = 4.1 Nm),其中 P3 缬氨酸单元被多种不同的部分.所得系列二肽型抑制剂对 3Cl Pro表现出中等至非常好的抑制活性.特别是,化合物26M和26N对k I表现出非常好的抑制活性.值分别为 0.39 和 0.33 μm.这些低分子量化合物对于进一步开发具有药物特性的强效肽模拟物抑制剂具有吸引力.进行了对接研究以模拟化合物26M与 Sars-Cov 3Cl 蛋白酶的结合相互作用.对具有强效抑制活性的拟肽化合物的初步 Sar 研究揭示了几个提高抑制活性的结构特征:(i)在 S1' 位置的苯并噻唑弹头,(II)在 S1 位置的 γ-内酰胺单元,(iii) S2-位的适当疏水亮氨酸部分,和
DOI:10.1016/j.Ejmech.2013.05.005

专利信息

专利号:US-4772587-A
优先权日:1985-04-16
标题:Dipeptide derivative of fatty acid
发明人：TANAKA TAKAHARU; HIGUCHI NAOKI; SAITOH MASAYUKI; HASHIMOTO MASAKI
权利人:SUNTORY LTD
摘要:A novel compound that exhibits inhibitory activity against prolyl endopeptidase and a method for chemical synthesis of said compound, as well as its use as a prolyl endopeptidase inhibitor and an anti-amnesic agent that contains said compound as the active ingredient are provided.

专利号:US-9090661-B2
优先权日:2009-03-27
标 题:Inhibitors of hepatitis C virus replication
发明人：COBURN CRAIG A; MCCAULEY JOHN A; LUDMERER STEVEN W; LIU KUN; VACCA JOSEPH P; WU HAO; HU BIN; SOLL RICHARD; SUN FEI; WANG XINGHAI; YAN MAN; ZHANG CHENGREN; ZHENG MINGWEI; ZHONG BIN; ZHU JIAN
权利人:MERCK SHARP & DOHME
摘要:The present invention relates to compounds of formula (I) that are useful as hepatitis C virus (HCV) NS5A inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5A activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.

专利号:US-7354923-B2
优先权日:2001-08-10
标 题 :Piperazine melanocortin-specific compounds
发明人：SHARMA SHUBH D; SHI YI-QUN; WU ZHIJUN; RAJPUROHIT RAMESH
权利人:PALATIN TECHNOLOGIES INC
摘要:Melanocortin receptor-specific piperazine or ketopiperazine compounds having the structure: n nand stereoisomer and pharmaceutically acceptable salts thereof, where X is CH 2 or Câ•?O, R 1 , R 2 , and R 3 are as described in the specification, preferably where R 3 is a D-amino acid with at least one substituted or unsubstituted phenyl or naphthyl aromatic ring, and where R 3 optionally further includes an amine capping group, a second amino acid residue or a second amino acid residue with an amine capping group, which compounds are agonists, antagonists or mixed agonists and antagonists at one or more melanocortin receptors, and having utility in the treatment of melanocortin receptor-related disorders and conditions. Methods of synthesis of compounds of structure (I), pharmaceutical compositions containing a compound of structure (I) and methods relating to the use thereof are also disclosed.

专利号:US-2023226197-A1
优先权日:2020-06-18
标 题:Composition and method for new therapeutic agents including guanidinium-presenting dendrimers and branched structures
发明人：WENDER PAUL; CEGELSKI LYNETTE; BRCIC JASNA; CHOSY MADELINE; RAHN HARRISON P; Sun jiuzhi
权利人:UNIV LELAND STANFORD JUNIOR
摘要:The design, synthesis, and biological evaluation of a new family of highly effective conjugate compounds, including dendrimeric moieties and branched structures, are described. Pharmaceutical compositions including the subject dendrimeric conjugates and methods of using the same are also provided. Methods of using the subject dendrimeric conjugates include delivering a cargo moiety conjugated to the dendrimeric moieties and branched structures to a cell under suitable conditions. In certain embodiments, the cell is a bacterial cell population, and the subject compounds reduce the bacterial cell population. In certain embodiments of the methods, the subject compound is capable of eradicating one or more of Gram-positive bacteria, mycobacteria, and Gram-negative bacteria. In certain embodiments of the methods, the subject compound is capable of eradicating bacterial biofilms. Methods of using the subject dendrimeric conjugates include treating a subject for a disease or condition. In certain embodiments, the disease or conditions an infectious disease.