摘要:
The current invention relates to the design, synthesis, and biochemical evaluation of chromogenic substrate compounds for sialidases of bacterial, viral, protozoa, and vertebrate (including human) origin. In particular, this invention provides a novel class of effective compounds as chromogenic substrates of these sialidases which yield chromogenic products after reactions catalyzed by sialidase take place. Also provided are methods of making these substrate compounds, methods of diagnosis and prognosis of sialidase related diseases using these substrate compounds.
摘要:
The invention discloses the compounds of formula (I): R1 = H, OH, alkyl, alkenyl or alkynyl optionally substituted or alkoxy; R2 = H, Hal; R3 = H, alkyl, Hal, R4 = (a) where Rg and Rh are H, alkyl, an aryl heterocycle; R5 = H or O-alkyl; R6 = alkyl or CH2-O-alkyl; R7 = H or alkyl. The compounds of formula (I) have antibiotic properties.
摘要:
The invention concerns compounds of formula (I), in which Y is oxygen, N-Nalc1 or NOalc2; X represents hydrogen, hydroxyl, alkyl, alkenyl, alkynyl, alkoxy, CONOR or NRcRd, Rc and Rd being hydrogen or alkyl; Z represents hydrogen, halogen or free, etherified or esterified OH; R2 hydrogen or halogen; R3 hydrogen, alkyl or halogen; R hydrogen or alkyl; R1 hydrogen, alkyl, alkenyl or alkynyl; R5 hydrogen or O-alkyl; R6 alkyl or CH2-O-alkyl and R7 hydrogen or alkyl; or R6 and R7 form with the carbon atom which bears them a cyclic radical containing up to 8 carbon atoms. The compounds of formula (I) have antibiotic properties.
摘要:
L'invention a pour objet les composés de formule (I) : dans lesquels :
R 1 : H ou Hal, R 2 : H ou alc, R 3 : alc ou halogène, R 4 : H, halogène, alc, alkényle ou alkynyle, R 5 : H, OH ou O-alkyle, R a et R b : un atome d'hydrogène, un radical alkyle renfermant jusqu'à 4 atomes de carbone, ou bien R a et R b forment avec l'atome d'azote auquel ils sont liés un hétérocycle mono ou polycyclique, ou bien R a et/ou R b représentent un radical : dans lequel n est un nombre entier variant de O à 6, alc 1 et alc 2 représentent un radical alkyle renfermant jusqu'à 8 atomes de carbone et leurs sels sous toutes leurs formes stéréoisomères possibles ainsi que leurs mélanges. Les composés de formule (I) présentent des propriétés antibiotiques.
摘要翻译:式(I)的核糖取代的芳族衍生物及其盐以所有立体异构形式及其混合物是新的:R1 = H或卤素; R2 = H或1-4C烷基; R3 =卤素或1-4C烷基; R4 = H,卤素或烷基,烯基或炔基,最高达12 C(任选环状); Ra,Rb = H或1-4C烷基; 或NR a R b =可以含有另外的杂原子(O,N或S)的单环或多环杂环,或者R a和/或R b可以形成式-CO-(CH 2)n -N(Alc 1)(Alc 2)的基团。 n = 0-6; 和alc1,alc2 = 1-8C烷基。
摘要:
The derivatives of glycoside bioflavonoids having general formula: wherein P represents the flavonic residue containing phenolic hydroxyls and R′ represents H, (CO-R-CO-O-N) n , in which X is selected among H, the cation of a pharmaceutically acceptable base and the radicals of polyoxyethylenglycols, polyoxypropylenglycols and their monomethylethers and R is an alkyl or aryl radical of a dicarboxylic acid, are water soluble and biodecomposable, maintaining at least the same therapeutical activity of the starting bioflavonoids. For their preparation the starting glycoside is reacted with the anhydride of the dicarboxylic acid , the resulting ether carboxylic derivative is reacted with a pharmaceutically acceptable base, for instance an alkali methal hydroxyde, carbonate or bicarbonate, or with polyoxyethylenglycol, polyoxypropylenglycol or their monomethylethers.
摘要翻译:具有通式糖苷生物类黄酮的衍生物: worin P darstellt的flavonic残余物含酚羟基和R分钟darstellt H,(CO-R-CO-ON)N,其中X是选自H,a的阳离子 药学上可接受的碱和聚氧乙烯二醇,聚氧丙烯二醇及其单甲基和R的自由基是自由基的二羧酸的烷基或芳基,是水溶性的并且biodecomposable,保持至少起始生物类黄酮的相同治疗活性。 对于它们的制备起始糖苷进行反应与二羧酸的酐氢氧化物,将得到的醚羧酸衍生物进行反应与药学上可接受的碱,对碱methal,碳酸盐或碳酸氢盐,或者与聚氧乙烯二醇,聚氧丙烯二醇或它们的单甲基醚的实例。