CAS: 166663-25-8; N-((2R,6S,9S,11R,12R,14As,15S,16S,20S,23S,25As)-23-((1S,2S)-1,2-Dihydroxy-2-(4-Hydroxyphenyl)Ethyl)-2,11,12,15-Tetrahydroxy-6,20-Bis((R)-1-Hydroxyethyl)-16-Methyl-5,8,14,19,22,25-Hexaoxotetracosahydro-1H-Dipyrrolo[2,1-C:2',1'-L][1,4,7,10,13,16]Hexaazacycl

上下游产品

CAS号619-44-3 4-碘苯甲酸甲酯 | CAS号63619-51-2 4-溴-4'-(戊氧基)联苯 | CAS号158938-08-0 对戊氧基三联苯甲酸 (阿尼芬净中间体)

4-碘苯甲酸甲酯置于sodium Hydroxide,四(三苯基膦)钯,硼酸三异丙酯,仲丁基锂,Potassium Carbonate,N,N'-二环己基碳二亚胺体系中,用 1,4-二氧六环,二氯甲烷,N,N-二甲基甲酰胺 用作溶剂,化学反应 17.0H,反应生成阿尼芬净
参考文献:抗真菌脂肽类棘球菌素b(ecb)的半合成化学修饰:Ecb的多芳基酰基类似物的亲脂性和几何参数的结构活性研究.
标题:抗真菌脂肽类棘球菌素b(ecb)的半合成化学修饰:Ecb的多芳基酰基类似物的亲脂性和几何参数的结构活性研究.
摘要:Echinocandin B(ecb)是由亚油酸在n端酰化的复杂环状肽组成的脂肽.Ecb的酶促脱酰作用提供了肽"核"作为无生物活性的底物,通过n端的化学酰化作用可从中产生新的ecb类似物.酰基的变化揭示了侧链的结构和物理性质,特别是其几何形状和亲脂性,在确定类似物的抗真菌效力方面起着关键作用.使用clogp值描述和比较侧链片段的亲脂性,表明抗真菌活性的表达要求> 3.5.其次,侧链的线性刚性几何形状是增强抗真菌效力的最有效形状.使用这些参数作为指导,合成了多种新型ecb类似物,其中包括结合了联苯,三联苯,四联和芳乙炔基的芳基.通常,这些类似物对葡聚糖合酶的抑制与体外和体内活性密切相关,并且同样受侧链结构的影响.这些结构变化导致在体外和体内测定中抗真菌活性的增强.这些类似物中的一些,包括ly303366(14A),通过口服途径有效.通常,这些类似物对葡聚糖合酶的抑制与体外和体内活性密切相关,
Doi:10.1021/jm00017A012

专利信息

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-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.

专利号:US-2024336559-A1
优先权日:2021-10-06
标 题 :Anti-fungals compounds targeting the synthesis of fungal sphingolipids
发明人：OJIMA IWAO; HARANAHALLI KRUPANANDAN; DEL POETA MAURIZIO; GARG ASHNA
权利人:UNIV NEW YORK STATE RES FOUND
摘要:The present invention provides a compound having the structure: n n n n n n n n n n n n wherein n R 3 , R 4 , R 5 , R 6 , and R 7 are each independently, H, halogen, CN, —CF 3 , —OCF 3 , —NO 2 , alkyl, alkenyl, alkynyl, aryl, heteroaryl, heterocycle, —OH, —OAc, —OR 13 , —COR 13 , —CH 2 OR 13 , —SH, —SR 13 , —SO 2 R 13 , —NH 2 , —NHR 13 , —NR 14 R 15 , —NHCOR 12 , or —CONR 14 R 15 ; n R 9 , R 10 , R 11 , and R 12 are each independently, H, CN, alkenyl, alkynyl, aryl, heteroaryl, cycloalkyl, heterocycloalkyl, —OAc, —COR 13 , —SH, —SR 13 , —SO 2 R 13 , —NH 2 , —NHR 13 , —NR 14 R 15 , —NHCOR 12 , or —CONR 14 R 15 ;n wherein each occurrence of R 13 is independently alkyl, alkenyl, alkynyl, aryl, or heteroaryl, wherein each occurrence of R 14 is independently —H, alkyl, alkenyl, alkynyl, aryl, or heteroaryl, wherein each occurrence of R 15 is independently —H, alkyl, alkenyl, alkynyl, aryl, or heteroaryl, n n wherein when R 14 is methyl, R 15 is not methyl; n wherein at least one of R 9 , R 10 , R 11 , and R 12 is not H; n wherein at least one of R 3 , R 4 , R 5 , R 6 , and R 7 is not H.

专利号:US-10443047-B2
优先权日:2014-05-01
标题 :Increasing cellular lipid production by increasing the activity of diacylglycerol acyltransferase and decreasing the activity of triacylglycerol lipase
发明人：TSAKRAKLIDES VASILIKI; BREVNOVA ELENA E
权利人:NOVOGY INC
摘要:Disclosed are methods and compositions for increasing the triacylglycerol content of a cell by up-regulating diacylglycerol acyltransferase and down-regulating triacylglycerol lipase. In some embodiments, a DGA1 protein is expressed and a native TGL3 gene is knocked out, thereby increasing the synthesis of triacylglycerol and decreasing its consumption, respectively.

专利号:US-12325678-B2
优先权日:2017-06-16
标 题 :Anti-fungals compounds targeting the synthesis of fungal sphingolipids
发明人：OJIMA IWAO; DEL POETA MAURIZIO; LAZZARINI CRISTINA; HARANAHALLI KRUPANANDAN; SUN YI
权利人:UNIV NEW YORK STATE RES FOUND
摘要:The present invention provides a compound having the structure: n nand use of the compound for inhibiting the growth of or killing.

专利号:US-2023364251-A1
优先权日:2020-08-06
标 题:Methods for the synthesis of protein-drug conjugates
发明人：BORCHARDT ALLEN; HUGHES ROBERT MICHAEL
权利人:CIDARA THERAPEUTICS INC
摘要:The present invention relates to intermediates and methods for synthesizing protein-drug conjugates that can be used for the treatment of diseases and related conditions.