Hypocholesterolemic activity of 1,3-bis(substituted phenoxy)-2-propanones
作者:Claude Piantadosi、Iris H. Hall、Steven D. Wyrick、Khalid S. Ishaq
DOI:10.1021/jm00224a006
日期:1976.2
phenoxy)-2-propanones was found to be active hypocholesterolemicagents at 10 mg/kg/day. The p-chloro- and p-methyl-substituted phenoxy compounds possess the highest activity. These compounds did not possess the estrogenic and antifertility activities of the related previously reported derivatives of the bis(beta-phenylethyl) ketone series. The 1,3-bis(p-methylphenoxy)-2-propanone (7) also lowered serum triglycerides
发现一系列的1,3-双(取代的苯氧基)-2-丙烷是有效的降胆固醇药,剂量为10 mg / kg / day。对氯-和对甲基取代的苯氧基化合物具有最高的活性。这些化合物不具有以前报道过的双(β-苯乙基)酮系列相关衍生物的雌激素和抗生育活性。1,3-双(对甲基苯氧基)-2-丙酮(7)也会降低血清甘油三酸酯和甘油,这似乎是由于血清脂肪酶水平升高和肝脂肪酶活性降低所致。肝脏减少了游离脂肪酸向复杂脂质中的掺入。胆固醇在治疗的动物中排泄更快。
Synthesis and antileishmanial activity of 1,3-bis(aryloxy)propan-2-amines
作者:Stefânia N. Lavorato、Mariana C. Duarte、Daniela P. Lage、Carlos A. P. Tavares、Eduardo A. F. Coelho、Ricardo J. Alves
DOI:10.1007/s00044-017-1805-1
日期:2017.5
We describe herein the antileishmanial activity of 1,3-bis(aryloxy)propan-2-amines, prepared in four simple steps from epichlorohydrin. Among the evaluated compounds, three (4o, 4q, and 4r) displayed considerable activity against Leishmania amazonensis promastigote forms, with IC50 values below 10 µM. We also analyzed the effects of the nature and the position of ring substituent on activity. Two amines
1,3-Bis(aryloxy)propan-2-ols as potential antileishmanial agents
作者:Stefânia N. Lavorato、Mariana C. Duarte、Daniela P. Lage、Carlos A. P. Tavares、Eduardo A. F. Coelho、Ricardo J. Alves
DOI:10.1111/cbdd.13024
日期:2017.11
We describe herein the synthesis and antileishmanial activity of 1,3-bis(aryloxy)propan-2-ols. Five compounds (2, 3, 13, 17, and 18) exhibited an effective antileishmanial activity against stationary promastigote forms of Leishmania amazonensis (IC50 < 15.0 μm), and an influence of compound lipophilicity on activity was suggested. Most of the compounds were poorly selective, as they showed toxicity
[EN] MONOMER, POLYMER, PREPARATION METHOD THEREFOR AND USE THEREOF<br/>[FR] MONOMÈRE, POLYMÈRE, PROCÉDÉ DE PRÉPARATION ET APPLICATION ASSOCIÉS<br/>[ZH] 单体、聚合物、制备方法及其用途
申请人:SUNSHINE LAKE PHARMA CO LTD
公开号:WO2018041132A1
公开(公告)日:2018-03-08
提出了单体、聚合物、制备方法及其用途。单体的结构如式(I)所示:
Levas, Annales de Chimie (Cachan, France), 1948, vol. <12> 3, p. 145,191