Synthesis, anticholinesterase, and calcium-antagonist activity of phenyl esters of n-substituted carbamic acid
作者:Yu. Ya. Ivanov、N. M. Smirnova
DOI:10.1007/bf02464676
日期:1997.1
anticholinesterase compounds renders them capable of producing calcium-antagonist action in addition to the anticholinesterase effect [1-4] . For example, Ca 2§ antagonism was observed in reversible cholinesterase inhibitors such as the esters of N-substituted carbamic acid with aliphatic structure of the alcohol part of the molecule [4]. The purpose of this work was to answer the question as to whether
先前我们已经证明,抗胆碱酯酶化合物的化学结构的某些修饰使它们能够产生除抗胆碱酯酶作用之外的钙拮抗剂作用 [1-4] 。例如,在可逆胆碱酯酶抑制剂中观察到 Ca 2§ 拮抗作用,例如 N-取代氨基甲酸的酯类,其分子的醇部分具有脂肪族结构 [4]。这项工作的目的是回答关于钙拮抗剂活性是否也是通过不同机制与胆碱酯酶相互作用的抗胆碱酯酶物质所固有的问题。初步研究表明,N-取代氨基甲酸的苯基酯通过组合机制(同时具有可逆和不可逆特征)抑制这些酶。在这方面,我们合成了一系列通式为RtNHC(O)OR 2 的化合物,其中R 1 = Me (I, II), Ph (IV, V), n-Bu (III);R 2 = Ph (I, III, IV), CrI-I4Me-4 (II, V)。
BRYOSTATIN ANALOGUES AND METHODS OF MAKING AND USING THEREOF
申请人:Keck Gary E.
公开号:US20110269713A1
公开(公告)日:2011-11-03
Described herein are tricyclic macrolactones. The macrolactones have a high binding affinity for PKC. The compounds described herein can be used in a number of therapeutic applications including cancer and Alzheimer's prevention and treatment. The compounds described herein can also treat memory loss. Also described herein are methods for producing macrolactones. The methods permit the high-yield synthesis of macrolactones in fewer steps and with a higher degree of substitution and specificity.
Concomitant Desulfurization and Transesterification of Alkyl Thionocarbamates
作者:Uday M. Joshi、Laxmikant N. Patkar、Srinivasachari Rajappa
DOI:10.1081/scc-120027235
日期:2004.12.31
Abstract Alkyl carbamate (such as 1) reacts with triphosgene at the nitrogen atom, whereas the analogous thionocarbamates (5) react at the sulfur. Subsequent treatment with various phenols or alcohols leads to the corresponding aryl carbamates or alkyl carbamates (6) respectively. The process thus involves both desulfurization and transesterification.
The present invention relates to aminocyclohexanol derivatives useful for the treatment and/or prophylaxis of diseases which are associated with 2,3-oxidosqualene-lanosterol cyclase such as hypercholesterolemia, hyperlipemia, arteriosclerosis, vascular diseases, mycoses, gallstones, tumors and/or hyperproliferative disorders, and treatment and/or prophylaxis of impaired glucose tolerance and diabetes.
Conjugates of a GLP-I moiety may be covalently attached to one or more water-soluble polymers. For instance, a GLP-I polymer conjugate may include a GLP-I moiety releasably attached at its N-terminus to a water-soluble polymer. The GLP-I polymer conjugate may include a GLP-I moiety covalently attached to a water-soluble polymer, wherein the GLP-I moiety possesses an N-methyl substituent. The GLP-I polymer conjugate may include a GLP-I moiety covalently attached at a polymer attachment site to a water-soluble polymer, wherein the GLP-I moiety is glycosylated at a site separate from the polymer attachment site.