摘要:
Described herein are nitroxyl progenitor compounds, and compositions including, and methods or generating, the compounds thereof, and methods of treating or preventing disease and disease symptoms using the compounds and compositions.
摘要:
The present invention relates generally to therapeutics targeting the bacterium Porphyromonas gingivalis, including its protease Lysine gingipain (Kgp), and their use for the treatment of disorders associated with P. gingivalis infection, including brain disorders such as Alzheimer's disease. In certain embodiments, the invention provides compounds according to Formula I, as described herein, and pharmaceutically acceptable salts thereof.
摘要:
The design, modeling, synthesis, biological evaluation, and photoaffinity labeling studies of a series of photoreactive potent and selective HDACs 1 and 2 benzamide based probes are disclosed herein.
摘要:
A photosensitive compound represented by formula (1) or formula (2). (Chemical formula 1) (In formula (1) and formula (2), n is an integer of 1-3; R1 is a linear or branched alkyl group having 1-6 carbon atoms or an alkylene group having 2-6 carbon atoms formed from two R1 together; R2 is —NR3R4; R3 and R4 are each independently a linear or branched alkyl group or alkenyl group having 1-6 carbon atoms, a linear or branched alkylene group having 2-6 carbon atoms formed by R3 and R4 together, or a linear or branched alkylene group or alkenylene group having 3-8 carbon atoms optionally containing an oxygen atom or nitrogen atom.)
摘要翻译:由式(1)或式(2)表示的光敏化合物。 (化学式1)(式(1)和式(2)中,n为1〜3的整数,R 1为碳原子数1〜6的直链或支链烷基或碳原子数2〜6的亚烷基 由两个R 1一起形成; R 2是-NR 3 R 4; R 3和R 4各自独立地是具有1-6个碳原子的直链或支链烷基或烯基,由R3和R4形成的具有2-6个碳原子的直链或支链亚烷基 一起或具有任选含有氧原子或氮原子的具有3-8个碳原子的直链或支链亚烷基或亚烯基)
摘要:
A process of synthesizing hyperbranched polytriazoles, linear and hyperbranched poly(aroyltriazoles) by Huisgen 1,3-dipolar cycloaddition. The polytriazoles were prepared by A2+B3 method to avoid self-polymerization during monomer preparation and storage. The polymers are light emissive and can be crosslinked to generate well-resolution photopatterns upon UV irradiation. White light emission patterns were observed with fluorescence microscopy. The high molecular weight poly(aroyltriazoles) (up to 26000 Da) are prepared in high yields (up to 92.0%) and with high regioselectivity (the ratio of 1,4- and 1,5-disubstituted 1,2,3-triazole is equal or larger than 9:1). The polycyclomerization is not moisture or oxygen sensitive and therefore, no special precautions are necessary before and during the reaction. All the polymers are processible, easily film-forming, and curable into thermosets by heat or irradiation. The hyperbranched polymers can act as fluorescent adhesive materials with large tensile strength.
摘要:
There is provided a class of crosslinking compound, said compound comprising (i) one or more fluorinated aromatic group; and (ii) one or more ionisable group, wherein the crosslinking compound is soluble in at least one polar solvent. Methods of preparing the crosslinking compounds are also disclosed. There is further provided devices obtainable from the methods of preparing the crosslinking compounds.
摘要:
Azidoaryl-substituted cyclooctene monomers and synthesized and used in the preparation of various copolymers. Among these copolymers are those prepared from ring-opening metathesis polymerization of cyclooctene, polyethylene glycol-substituted cyclooctene, and azidoaryl-substituted cyclooctene. These copolymers are useful in the formation of crosslinked films that reduce fouling of water purification membranes.
摘要:
Methods for producing perfluorocarbon monomethanols or dimethanols are disclosed. The methods of the invention can provide branched perfluorocarbon monomethanols or dimethanols with good purity and yields.
摘要:
The present invention provides compositions and methods to facilitate the identification of compounds that are capable of interacting with a biological macromolecule of interest. In one aspect, a composition is provided that comprises an array of one or more types of chemical compounds attached to a solid support, wherein the density of the array of compounds is at least 1000 spots per cm2. In particularly preferred embodiments, these compounds are attached to the solid support through a covalent interaction. In general, these inventive arrays are generated by: (1) providing a solid support, wherein said solid support is functionalized with a selected chemical moiety capable of interacting with a desired chemical compound to form an attachment; (2) providing one or more solutions of one or more types of compounds to be attached to the solid support; and (3) delivering said one or more types of compounds to the solid support, whereby an array is formed and the array of compounds has a density of at least 1000 spots per cm2. In another aspect, the present invention provides methods for utilizing these arrays to identify small molecule partners for biological macromolecules of interest comprising: (1) providing an array of compounds, wherein the array has a density of at least 1000 spots per cm2; (2) contacting the array with one of more types of biological macromolecules of interest; and (3) determining the interaction of specific small molecule-biological macromolecule partners.
摘要翻译:本发明提供了有助于鉴定能够与感兴趣的生物大分子相互作用的化合物的组合物和方法。 在一个方面,提供了包含连接到固体支持物上的一种或多种类型化学化合物的阵列的组合物,其中化合物阵列的密度为至少1000个斑点/ cm 2。 在特别优选的实施方案中,这些化合物通过共价相互作用连接到固体支持物上。 通常,这些本发明的阵列通过以下方式产生:(1)提供固体支持物,其中所述固体支持物用能够与所需化学化合物相互作用以形成附着物的选定化学部分官能化; (2)提供待连接到固体支持物上的一种或多种类型化合物的一种或多种溶液; 和(3)将所述一种或多种类型的化合物递送到固体支持物,由此形成阵列,并且所述化合物阵列的密度至少为1000个点/ cm 2。 另一方面,本发明提供了利用这些阵列来识别感兴趣的生物大分子的小分子配偶体的方法,包括:(1)提供化合物阵列,其中阵列的密度至少为1000个点/ cm 2 ; (2)使阵列与感兴趣的多种生物大分子之一接触; 和(3)确定特定小分子 - 生物大分子伴侣的相互作用。
摘要:
Novel farnesyl derivatives which are inhibitors of the prenylated protein thyltransferase enzyme, and useful as anti-cancer drugs, have the following formula: ##STR1## wherein R.sup.1 represents farnesyl, geranyl or geranyl-geranyl; Z represents C--R.sup.6 or N; R.sup.2 represents H, CN, the groups COOR.sup.7, SO.sub.3 R.sup.7, CONR.sup.7 R.sup.8 and SO.sub.2 NR.sup.7 R.sup.7, wherein R.sup.7 and R.sup.8 are each independently hydrogen, alkyl, alkenyl, and the groups COOM and SO.sub.3 M, wherein M is a cation; R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are each independently hydrogen, carboxyl, alkyl, alkenyl, aminoalkyl, nitroalkyl, nitro, halo, amino, mono- or di-alkylamino, mercapto, mercaptoalkyl, azido, or thiocyanato; X represents O, S, SO, SO.sub.2, NH or Se; and the quaternary ammonium salts and N-oxides of the compounds of formula I wherein Z is N.
摘要翻译:作为异戊烯基化蛋白甲基转移酶的抑制剂,可用作抗癌药物的新型法呢基衍生物具有下式:其中R1代表法呢基,香叶基或香叶基 - 香叶基; Z表示C-R6或N; R 2表示H,CN,COOR 7,SO 3 R 7,CONR 7 R 8和SO 2 NR 7 R 7基团,其中R 7和R 8各自独立地为氢,烷基,烯基和基团COOM和SO 3 M,其中M为阳离子; R 3,R 4,R 5和R 6各自独立地为氢,羧基,烷基,烯基,氨基烷基,硝基烷基,硝基,卤素,氨基,单 - 或二 - 烷基氨基,巯基,巯基烷基,叠氮基或硫氰酸酯基。 X表示O,S,SO,SO 2,NH或Se; 和其中Z为N的式I化合物的季铵盐和N-氧化物。