CAS: 477-32-7; Cardin

📜2-甲基丁酸,(+/-)-Cis-4'-Acetylkhellactone 在 4-吡咯烷基吡啶,N,N'-二环己基碳二亚胺体系中,用 二氯甲烷作为反应溶剂,以65.2%的收率获得cis-3'-Isovaleryl-4'-Acetylkhellactone
参考文献:The Antagonistic Effects Of Khellactones On Platelet-Activating Factor,Histamine,And Leukotriene D4.
标题:The Antagonistic Effects Of Khellactones On Platelet-Activating Factor,Histamine,And Leukotriene D4.
摘要:白花前胡所含的khellactones类化合物,包括前胡素a(=pd-Ia,2)和前胡素b(=pd-Ii,11),在各种促聚剂中,对血小板活化因子(Paf)诱导的血小板聚集具有特异性的拮抗作用,代表了一类新的paf拮抗剂.我们研究了20种化合物对paf诱导的血小板聚集以及对离体豚鼠回肠中组胺和白三烯d4(Ltd4)诱导的收缩的影响.化合物2,(+/-)-顺式-3',4'-二乙酰基khellactone(3),(+/-)-顺式-4'-乙酰基-3'-丁烯酰基khellactone(5),(+/-)-顺式-4'-乙酰基-3'-四羟基苯甲酰基khellactone(6),(+/-)-顺式-4'-乙酰基-3'-惕各酰基khellactone(7),(+/-)-顺式-4'-乙酰基-3'-(2"-甲基丁酰基)Khellactone(8),(+/-)-顺式-3',4'-二惕各酰基khellactone(10)和11均强烈抑制paf诱导的血小板聚集.(+/-)-顺式-4'-乙酰基-3'-(2"-甲基-2"-十二碳烯酰基)Khellactone(9),(+/-)-顺式-4'-乙基-3'-惕各酰基khellactone(13),(+/-)-顺式-4'-乙基-3'-[N-(2"-三乙基铵)乙基氨基甲酰基]Khellactone碘化物(16),(+/-)-反式-3',4'-二乙酰基khellactone(18),(+/-)-反式-4'-乙酰基-3'-丁烯酰基khellactone(19),(+/-)-反式-4'-乙酰基-3'-戊酰基khellactone(20),(+/-)-反式-4'-乙酰基-3'-异戊酰基khellactone(21)和(+/-)-反式-4'-乙酰基-3'-惕各酰基khellactone(22)的抑制作用较弱.大多数化合物对组胺和ltd4诱导的收缩表现出非竞争性拮抗作用.对组胺作用的拮抗效能顺序为7=22>=2=8=10>6=11=13>=5>19=9,对ltd4作用的拮抗效能顺序为6=22=2>10=8>7=9=11>=13.因此,具有强paf拮抗活性的化合物具有以下特点:C-3'和c-4'位置的顺式异构体比反式异构体更有利,Khellactone的c-3'位置的酰基部分必须具有适当的分子大小.对于组胺和ltd4的拮抗活性,两种异构体显示出类似的效果,C-3'和c-4'位置需要适当大小的酰基部分.这些结果对于作为草药药用的peucedanum属植物的医疗用途具有重要意义.
Doi:10.1248/Cpb.43.859

专利信息

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-11739112-B2
优先权日:2017-02-02
标 题:Low temperature process for the synthesis of MOF carboxylate nanoparticles
发明人：PANCHAL MONIK; NOUAR FARID; SERRE CHRISTIAN; BENZAQUI MARVIN; SENE SAAD; STEUNOU NATHALIE; GIMÉNEZ MARQUÉS MONICA
权利人:CENTRE NAT RECH SCIENT; UNIV DE VERSAILLES—SAINT QUENTIN EN YVELINES
摘要:The present invention relates to low temperature process for preparing nanoparticles of porous crystalline Fe-, Al- or Ti-based MOF carboxylate materials with low polydispersity index, and uses thereof, particularly as catalyst support for carrying out heterogeneously catalyzed chemical reactions, or as gas storage/separation/purification material, or as matrix for encapsulating active principles (medicine, cosmetics).

专利号:US-2023288116-A1
优先权日:2022-03-14
标 题:Large scale synthesis of pharmaceutical and biologic formulations using thin film freezing
发明人：OWENS III DONALD E; KOLENG JR JOHN J
权利人:TFF PHARMACEUTICALS INC
摘要:The invention encompasses methods for the large-scale (preferably under cGMP or cGLP standards) preparation of micron-sized or submicron-sized particles including pharmaceutical or biologic active agents. The systems and methods include a cryogenic cooling system including a novel shroud that enhances the cooling effects thereby reducing product loss and increasing product yields.

专利号:WO-2006097348-A1
优先权日:2005-03-15
标 题:Use of agents such as nonpolymeric nitric oxide donors for making the lips full again and/or colouring the lips
发明人：CALS-GRIERSON MARIE-MADELEINE
权利人:OREAL; CALS-GRIERSON MARIE-MADELEINE
摘要:The invention relates in particular to the cosmetic use (i) of at least one agent for promoting the production of NO in and/or on the lips, chosen from nitric oxide NO donors or precursors; nonpolymeric NO releasers; and NO synthase synthesis and/or activity stimulators; or (ii) of other agents for promoting microcirculation in the skin, chosen from potassium channel openers; calcium channel blockers; phosphodiesterase inhibitors; flavonoids; vasodilator peptides that are not NO donors; temperature modulators; agents for promoting the stimulation and/or maintenance of angiogenesis; agents for promoting the stimulation of endothelial cell proliferation; agents for promoting endothelial cell migration; and mixtures thereof, in a makeup and/or care composition for the lips, as an agent for naturally making the lips full again and/or naturally coloring the lips. It also relates to specific care and/or makeup compositions for the lips containing said agent, and also to a cosmetic process aimed at making the lips naturally full and/or colored, using said compositions .

专利号:US-10814013-B2
优先权日:2006-10-05
标 题 :Efficient synthesis of chelators for nuclear imaging and radiotherapy: compositions and applications

专利号:US-2020102337-A1
优先权日:2017-02-02
标题 :Low temperature process for the synthesis of mof carboxylate nanoparticles