Spermicidal, anti-HIV, and micellar properties of di- and trihydroxylated cationic surfactants
作者:Yue-Ling Wong、Christopher L Curfman、Gustavo F Doncel、M Patricia Hubieki、Travis C Dudding、Prashant S Savle、Richard D Gandour
DOI:10.1016/s0040-4020(01)01114-0
日期:2002.1
effective at 0.1 mg mL−1 in the cell-free assay and 0.5 mg mL−1 in the cell-associated assay. Compound 1(16) shows the best combination of dual activity against sperm and HIV. In summary, hydroxylated cationic surfactants, 1 and 2, show promise as inexpensive topical, contraceptive microbicides.
2-羟基-N-(2-羟乙基)-N,N-二甲基-1-烷胺1(p)和2-羟基-N,N-双(2-羟乙基)-N-甲基-1- alkanaminium 2(p为同源系列中描述)溴化物,tetradecanaminium(p = 14)通过octadecaminium(p= 18)。该系列偶数成员的临界胶束浓度(cmc's)在25和37°C下通过电导率测量,显示了预期的线性依赖于链长。所有化合物均显示杀精和杀虫活性。在Sander–Cramer杀虫剂测定法1和2中,最小有效浓度(MEC)与链长的关系图分别显示了截止效应和抛物线关系。最好的化合物1(17)和1(18)的MEC(〜0.12 mg mL -1)略低于市售杀精子剂壬氧化酚9(N-9)。化合物1(16)和2(17)在体外,无细胞和细胞相关的病毒灭活试验中显示出最佳的抗HIV活性。两者在无细胞测定中均为0.1 mg mL -1,在细胞相关测定中均为0
Cobalt-Mediated Mizoroki-Heck-Type Reaction of Epoxide with Styrene
Treatment of a mixture of epoxide and styrene with trimethylsilylmethylmagnesium bromide in the presence of a cobalt-phosphine complex afforded homocinnamyl alcohol in good yield. The reaction should begin with ring opening of the epoxide by the action of magnesium bromide which leads to the formation of a magnesium 2-bromoethoxide derivative and not with a direct single electron transfer from a cobalt
Detergents are the most frequently applied reagents in membraneprotein (MP) studies. The limited diversity of one-head-one-tailed traditional detergents, however, is far from sufficient for structurally distinct MPs. Expansion of detergent repertoire has a continuous momentum. In line with the speculation that detergent pre-assembly exerts superiority, herein we report for the first time cross-conjugation
去污剂是膜蛋白 (MP) 研究中最常用的试剂。然而,一头一尾传统洗涤剂的有限多样性对于结构不同的 MP 来说还远远不够。洗涤剂品种的扩张势头不断。与去污剂预组装发挥优势的推测一致,本文首次报道了两个系列单体去污剂的交叉共轭,用于构建二聚去污剂的二维库。最佳去污剂在个体 MP 的系统评估中具有独特的偏好。此外,前所未有的混合去污剂 14M8G 和 14M9G 分别实现了转运蛋白 MsbA 的高质量 EM 研究和 G 蛋白偶联受体 A2A AR 的 NMR 研究。鉴于交叉偶联化学物质的丰富性,
SANTANIELLO, E.;FERRABOSCHI, P.;SOZZANI, P., J. ORG. CHEM., 1981, 46, N 22, 4584-4585