CAS: 198561-04-5; Fmoc-Phe(4-Br)-Oh

相似化合物

14091-15-7 198545-76-5 24250-84-8

上下游产品

H-p-BrPhe-OH N-(9H-fluoren-2-ylmethoxycarbonyloxy)succinimide Cph-Cha-Dap-Glu-Bph-Leu N-[(9H-fluoren-9-ylmethoxy)carbonyl]-N-methyl-4-bromo-L-phenylalanine 9H-fluoren-9-ylmethyl (S)-4-(4-bromo)-benzyl-5-oxo-1,3-oxazolidine-3-carboxylate

L-4-溴苯丙氨酸,9-芴甲基-N-琥珀酰亚胺基碳酸酯置于sodium Carbonate体系中,用 水,丙酮 用作溶剂,化学反应 2.0H,以97%的收率获得4-溴-N-Fmoc-L-苯基丙氨酸
参考文献:受自然启发的药物设计:自动剪裁的蛋白酶抑制剂模板的晶体学检测.
标题:受自然启发的药物设计:自动剪裁的蛋白酶抑制剂模板的晶体学检测.
摘要:从头开始发现药物仍然是寻找治疗相关靶蛋白的有效和选择性调节剂的挑战.在这里,我们揭示了x射线晶体学法意外发现的肽配体1,它是由治疗靶点mmp-13通过部分自降解和随后基于结构的优化自动构建为高效的选择性β-片层的拟肽抑制剂,衍生自金属蛋白酶的内源性组织抑制剂.事实证明,结合非蛋白原性氨基酸和环化策略是timp拟肽模拟设计的关键.优化的环肽4(zhawoc7726)具有21 N M Ic 50的膜渗透性mmp-13的选择性和相对于多药理学方法的诱人的选择性,包括抗癌靶标mmp-2(ic 50:170 N M)和mmp-9(ic 50:140 N M).
Doi:10.1002/anie.201812348

专利信息

专利号:WO-2013057186-A1
优先权日:2011-10-19
标题 :Photolabile linker for the synthesis of hydroxamic acids
发明人：NIELSEN THOMAS E; QVORTRUP KATRINE
权利人:UNIV DANMARKS TEKNISKE
摘要:The present invention relates to a photolabile hydroxamate linker based on the o - nitroveratryl group and its application for multistep solid-phase synthesis and controlled photolytic release of hydroxamic acids. The invention provides a method for producing a solid support comprising a hydroxylamine - functionalized photolabile linker, and the so produced hydroxylamine - functionalized photolabile solid support. The invention further provides a method for synthesizing a one-bead-one compound library of hydroxamic acid derivatives on a photolabile linker, as well as a method for screening a library of hydroxamic acid derivatives.

专利号:US-8338565-B2
优先权日:2008-08-20
标 题 :Macrocyclic compounds for inhibition of tumor necrosis factor alpha
发明人：LEE JINBO; BOND JULIAN F; TERRETT NICHOLAS; FAVALORO JR FRANK G; WANG DANIEL; BRIGGS TIMOTHY F; SEIGAL BENJAMIN ADAM; SUN WEI-CHUAN; HALE STEPHEN P
权利人:LEE JINBO; BOND JULIAN F; TERRETT NICHOLAS; FAVALORO JR FRANK G; WANG DANIEL; BRIGGS TIMOTHY F; SEIGAL BENJAMIN ADAM; SUN WEI-CHUAN; HALE STEPHEN P; ENSEMBLE THERAPEUTICS CORP
摘要:Disclosed herein are macrocyclic compounds and methods for their synthesis and use. In particular, macrocyclic compounds are disclosed that modulate the activity of tumor necrosis factor alpha and/or are useful in the treatment of medical conditions, such as, rheumatoid arthritis, psoriasis, and asthma.

专利号:CN-111777668-B
优先权日:2020-07-28
标题 :A kind of modified polypeptide, synthesis method and application based on marine cyclic peptide Samoamide A