A quantitative structure-activity study of anticonvulsant phenylacetanilides.
摘要:
通过最大电击癫痫发作试验,对一系列邻、间、对取代的苯乙酸苯胺类化合物在小鼠体内的抗惊厥活性进行了测试,并通过汉斯赫分析法对结构-活性关系进行了定量研究。结果表明,元衍生物的药效(-log ED50)与对数 P(P 为 1-辛醇-H2O 分配系数)呈抛物线关系,与 Hammett σ 值呈线性关系。根据推导出的相关性预测,当对数 P 约为 2.3 且引入了一个电子捐赠取代基时,将获得最大活性。这一结论与最近报告的 m 和 p 取代的 N,N-二甲基氨基甲酸苄酯的结构要求一致。大多数 o 和 p 取代的化合物的活性低于 m 衍生物。本文讨论了正对和对位取代的影响。
Meta-bifunctional benzenes and herbicidal compositions
申请人:Monsanto Company
公开号:US03979202A1
公开(公告)日:1976-09-07
Meta-bifunctional of the general formula ##EQU1## wherein A is selected from the groups ##EQU2## These compounds possess herbicidal activity.
通式##EQU1##中的元双功能化合物,其中A选自##EQU2##这些化合物具有除草活性。
Nonpeptide Inhibitors of Measles Virus Entry
作者:Aiming Sun、Andrew Prussia、Weiqiang Zhan、Ernest E. Murray、Joshua Doyle、Li-Ting Cheng、Jeong-Joong Yoon、Eugene V. Radchenko、Vladimir A. Palyulin、Richard W. Compans、Dennis C. Liotta、Richard K. Plemper、James P. Snyder
DOI:10.1021/jm0602559
日期:2006.8.1
Measles virus (MV) is one of the most infectious pathogens known. Despite the existence of a vaccine, over 500 000 deaths/year result from MV or associated complications. Anti-measles compounds could conceivably reverse these statistics. Previously, we described a homology model of the MV fusion protein trimer and a putative binding site near the head-neck region. The resulting model permitted the identification of two nonpeptidic entry inhibitors. Here, we present the design, synthesis, and bioevaluation of several series of fusion inhibitors and describe their structure-activity relationships (SAR). Five simply substituted anilides show low-mu M blockade of the MV, one of which (AS-48) exhibits IC50 0.6-3.0 mu M across a panel of wild-type MV strains found in the field. Molecular field topology analysis (MFTA), a 2D QSAR approach based on local molecular properties (atomic charges, hydrogen-bonding capacity and local lipophilicity), applied to the anilide series suggests structural modifications to improve potency.
Photosensitive Resin Composition and Photosensitive Film
申请人:Miyazaki Kuon
公开号:US20090191385A1
公开(公告)日:2009-07-30
Disclosed is a photosensitive resin composition comprising an alkali-soluble resin, wherein the dissolution rate of the alkali-soluble resin in an aqueous sodium carbonate solution is not less than 0.04 μm/sec. When a photosensitive layer having a thickness of 30 μm is formed by applying the photosensitive resin composition onto a base and removing the solvent by heating, and thus-obtained photosensitive layer is irradiated with an active ray of 1000 mJ/cm
2
or less, the dissolution rate of the portion irradiated with the active ray in the photosensitive layer made of the photosensitive resin composition is not less than 0.22 μm/sec and the film residual rate of the portion not irradiated with the active ray is not less than 90%.