Synthesis and collateral dilator activity of nitroxyalkylamides having direct or latent sulfhydryl moieties
摘要:
To develop an orally active, long-acting nitrate that does not induce tolerance, nitroxyalkyl compounds were prepared and their activities evaluated by the use of carotid collaterals in anesthetized dogs. A compound having a favorable pharmacological profile, that is, long-lasting collateral vasodilatation and little hypotension, and lack of nitrate tolerance, was chosen for further evaluation. (C) 2003 Elsevier Science Ltd. All rights reserved.
Total Synthesis of (+)-18-<i>epi</i>-Latrunculol A: Development of a Synthetic Route
作者:Brett D. Williams、Amos B. Smith
DOI:10.1021/jo501733m
日期:2014.10.3
The evolution of an enantioselective totalsynthesis of (+)-18-epi-latrunculol A, a congener of the marine-sponge-derived latrunculins A and B, is reported. Key steps include a late-stage Mitsunobu macrolactonization to construct the 16-membered macrolactone, a mild Carreira alkynylation to unite the northern and southern hemispheres, a diastereoselective, acid-mediated δ-hydroxy enone cyclization/equilibration
报告了 (+)-18- epi -latrunculol A(海洋海绵衍生的 latrunculins A 和 B 的同系物)的对映选择性全合成的演变。关键步骤包括后期 Mitsunobu 大环内酯化以构建 16 元大环内酯、温和的 Carreira 炔基化以统一北半球和南半球、非对映选择性、酸介导的 δ-羟基烯酮环化/平衡序列,以及功能组-耐受交叉复分解以获得烯酮环化前体。
Thiazolidone compounds and method of using the same as a vasodilator
申请人:Sankyo Company, Limited
公开号:US05298516A1
公开(公告)日:1994-03-29
Compounds of formula (I): ##STR1## wherein W represents a sulfur atom and X represents a group of formula --N(R.sup.1)--, or W represents a group of formula --N(R.sup.1)-- and X represents a sulfur atom; R.sup.1 is hydrogen, alkyl or aralkyl; R.sup.2 and R.sup.3 are each hydrogen, alkyl, aralkyl, aryl or aromatic heterocyclic; R.sup.4 is hydrogen, alkyl or aralkyl; and A is alkylene which is optionally substituted by carboxy; and pharmaceutically acceptable salts and esters thereof, have a valuable vasodilatory activity.
Oxazolidinone compounds and method of using the same as a vasodilator
申请人:Sankyo Company, Ltd.
公开号:US05356918A1
公开(公告)日:1994-10-18
Compounds of formula (I): ##STR1## wherein W represents an oxygen atom and X represents a group of formula --N(R.sup.1)--; R.sup.1 is hydrogen, alkyl or aralkyl; R.sub.2 and R.sup.3 are each hydrogen, alkyl, aralkyl, aryl or aromatic heterocyclic; R.sup.4 is hydrogen, alkyl or aralkyl; and A is alkylene which is optionally substituted by carboxy; and pharmaceutically acceptable salts and esters thereof, have a valuable vasodilatory activity.
The present invention provides hepatoprotectant acetaminophen mutual prodrugs, which have an acetaminophen moiety covalently linked to a second moiety that may act as a hepatoprotectant against acetaminophen hepatotoxicity. Additionally, acetaminophen mutual prodrugs may have improved water solubility which may provide better suitability for parenteral and other dosage forms relative to administration of acetaminophen. Also provided are methods of treating a disease or condition that is responsive to acetaminophen (such as fever, pain and ischemic injury) using hepatoprotectant acetaminophen mutual prodrugs, as well as kits and unit dosages.