CAS: 1404-90-6; (3S,6R,7R,22R,23S,26S,36R,38Ar)-3-(2-Amino-2-Oxoethyl)-44-[[2-O-(3-Amino-2,3,6-Trideoxy-3-C-Methyl-α-L-Lyxo-Hexopyranosyl)-β-D-Glucopyranosyl]Oxy]-10,19-Dichloro-2,3,4,5,6,7,23,24,25,26,36,37,38,38A-Tetradecahydro-7,22,28,30,32-Pentahydroxy-6-[[(2R)-4-Methyl-2-(Methylamino)-1-Oxopentyl]Amino]-2,5,24,38,39-Pentaoxo-22H-8,11:18,21-Dietheno-23,36-(Iminomethano)-13,16:31,35-Dimetheno-1H,16H-[1,6,9]Oxadiazacyclohexadecino[4,5-M][10,2,16]Benzoxadiazacyclotetracosine-26-Carboxylic Acid

上下游产品

CAS号216668-88-1 N,N'-diall°C-tr...

在 10Percent Pd/c 甲酸铵,溶剂黄146体系中,用 甲醇 用作溶剂,化学反应 4.0H,以81%的收率获得万古霉素
参考文献:固相和液相合成万古霉素和具有抗万古霉素细菌活性的万古霉素类似物.
标题:固相和液相合成万古霉素和具有抗万古霉素细菌活性的万古霉素类似物.
摘要:万古霉素是抗生素糖肽家族的原型成员,是一种临床上使用的抗生素,可抗多种耐药菌菌株,包括耐甲氧西林金黄色葡萄球菌(mrsa).最近出现的对公共卫生构成日益严重威胁的万古霉素耐药性促使我们启动了一项旨在通过化学处理万古霉素结构来恢复这种重要抗生素效力的计划.在此,我们基于新型硒安全捕获连接器的设计,该技术在万古霉素固相半合成中的应用以及万古霉素文库的固相和溶液相合成,描述了合成技术的发展.这些化合物文库的生物学评估导致鉴定出许多对万古霉素耐药细菌有效的体外高效抗菌剂.除了帮助这些研究之外,预期本文所述的固相化学将增强组合化学的能力并促进化学生物学和药物化学研究.
Doi:10.1002/1521-3765(20010903)7:17<3798::Aid-Chem3798>3.0.Co;2-6

专利信息

专利号:US-11667658-B2
优先权日:2021-06-30
标 题:Chemical synthesis of the organoarsenical antibiotic arsinothricin
发明人：ROSEN BARRY P; YOSHINAGA MASAFUMI; WNUK STANISLAW F; HOWLADER MD ABU HASAN; SUZOL SK MD SAZZAD HOSSAIN
权利人:ROSEN BARRY P; YOSHINAGA MASAFUMI; WNUK STANISLAW F; HOWLADER MD ABU HASAN; SUZOL SK MD SAZZAD HOSSAIN; THE FLORIDA INTERNATIONAL UNIV BOARD OF TRUSTEES
摘要:The subject invention provides methods for the chemical synthesis of racemic arsinothricin (D,L-AST), the novel organoarsenical antibiotic. One is by condensation of the 2-chloroethyl(methyl)arsinic acid with acetamidomalonate, and the second involves reduction of the N-acetyl-protected derivative of hydroxyarsinothricin (AST-OH) and subsequent methylation of the resulting sodium salt of trivalent arsenic intermediate with methyl iodide. The enzyme AST N-acetyltransferase (ArsN1) was utilized to purify L-AST from racemic AST. This expedient chemical synthesis of AST provides a source of this novel antibiotic for future drug development.

专利号:US-7301006-B2
优先权日:2002-07-16
标 题 :Methods and materials for the synthesis of modified peptides
发明人：YOUNG TRAVIS G; KIESSLING LAURA L
权利人:WISCONSIN ALUMNI RES FOUND
摘要:Methods and protected amino acids useful as building blocks (protected monomers) for the synthesis of peptides and proteins that are selectively modified at one or more side-chain hydroxyl groups. Azide-bearing protecting groups allow the selective deprotection of side-chain hydroxyl groups of amino acids after synthesis of a peptide. Reaction conditions for removal of the azide-bearing protecting group can be selected which are substantially orthogonal to those that will remove α-amino protecting groups typically employed in peptide synthesis, such that hydroxyl groups protected with the azide-bearing protecting group remain protected during synthesis of the peptide chain. Various protecting groups which are readily available can be used for protecting potentially reactive side chain groups of amino acids in the peptide or protein to be modified. Preferred side-chain protecting groups are chemically distinguishable from the azide-bearing protecting group and substantially orthogonal reaction conditions can be selected such that side-chain protection of other amino acids is maintained when the azide-bearing protecting group is removed. The use of the azide-bearing protecting group of this invention for one or more hydroxy amino acids during peptide synthesis allows the selective unmasking of those azide-protected side-chain hydroxyl groups and selective modification of the hydroxyl groups that are selectively unmasked. The methods and materials herein are particularly used in synthesis of sulfated, phosphorylated and glycosylated peptides and proteins. Kits and methods of synthesizing a modified peptide or protein using the kits are also provided.

专利号:US-12383499-B2
优先权日:2018-01-01
标题:Scale up synthesis of silicasome nanocarriers
发明人：NEL ANDRE E; MENG HUAN; LIU XIANGSHENG
权利人:UNIV CALIFORNIA
摘要:In order to facilitate the approval and commercialization of silicasome drug delivery systems (e.g. irinotecan silicasomes) it is necessary to scale up synthesis of the drug-loaded silicasomes. In this regard, it was discovered that the synthesis protocols used for laboratory synthesis of drug-loaded silicasomes (e.g., 500 mg/batch) do not scale to large scale silicasome production, because the resulting products were too heterogeneous for use as pharmaceuticals. Accordingly, new methods are provided herein that effectively afford the large-scale production of mesoporous silica nanoparticles (MSNPs) and lipid bilayer coated MSNPs (silicasomes).

专利号:US-2023398215-A1
优先权日:2020-10-28
标 题:Genetically engineered antigen-specific natural killer cells for in situ synthesis of proteins
发明人：BHATNAGAR PARIJAT
权利人:STANFORD RES INST INT
摘要:An example genetically engineered natural killer (NK) cell comprises an exogenous polynucleotide sequence that includes a receptor element, an actuator element, and an effector element. The receptor element encodes a chimeric antigen receptor (CAR) comprising an extracellular antigen binding domain operably linked to a transmembrane domain, and an intracellular signaling domain, wherein the extracellular antigen binding domain recognizes a surface antigen of a target cell. The actuator element encodes a transcription factor binding site that upregulates synthesis of an effector protein. The effector element encodes the effector protein operably linked to a signal peptide, wherein, in response to the antigen binding domain of the CAR binding to the antigen of the target cell, the engineered NK cell is configured to activate and, to synthesize and secrete the effector protein.

专利号:US-9884830-B2
优先权日:2004-05-21
标题 :Synthesis of tetracyclines and analogues thereof
发明人：MYERS ANDREW G; CHAREST MARK G; LERNER CHRISTIAN D; BRUBAKER JASON D; SIEGEL DIONICIO R
权利人:HARVARD COLLEGE
摘要:The tetracycline class of antibiotics has played a major role in the treatment of infectious diseases for the past 50 years. However, the increased use of the tetracyclines in human and veterinary medicine has led to resistance among many organisms previously susceptible to tetracycline antibiotics. The modular synthesis of tetracyclines and tetracycline analogs described provides an efficient and enantioselective route to a variety of tetracycline analogs and polycyclines previously inaccessible via earlier tetracycline syntheses and semi-synthetic methods. These analogs may be used as anti-microbial agents or anti-proliferative agents in the treatment of diseases of humans or other animals.

专利号:US-10925977-B2
优先权日:2006-10-05
标 题 :Efficient synthesis of chelators for nuclear imaging and radiotherapy: compositions and applications
发明人：YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S
权利人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S; CEIL POINT LLC; UNIV TEXAS
摘要:Novel methods of synthesis of chelator-targeting ligand conjugates, compositions comprising such conjugates, and therapeutic and diagnostic applications of such conjugates are disclosed. The compositions include chelator-targeting ligand conjugates optionally chelated to one or more metal ions. Methods of synthesizing these compositions in high purity are also presented. Also disclosed are methods of imaging, treating and diagnosing disease in a subject using these novel compositions, such as methods of imaging a tumor within a subject and methods of diagnosing myocardial ischemia.