86364-65-0Relevant articles and documents
Design, synthesis and biological evaluation of anthranilamide derivatives as potential factor Xa (fXa) inhibitors
Xing, Junhao,Yang, Lingyun,Zhou, Jinpei,Zhang, Huibin
, p. 5987 - 5999 (2018/11/23)
Factor Xa (fXa) is a crucial player in various thromboembolic disorders. Inhibition of fXa can provide safe and effective antithrombotic effects. In this study, a series of anthranilamide compounds were designed by utilizing structure-based design strategies. Optimization at P1 and P4 groups led to the discovery of compound 16g: a highly potent, selective fXa inhibitor with pronounced in vitro anticoagulant activity. Moreover, 16g also displayed excellent in vivo antithrombotic activity in the rat venous thrombosis (VT) and arteriovenous shunt (AV-SHUNT) models. The bleeding risk evaluation showed that 16g had a safer profile than that of betrixaban at 1 mg/kg and 5 mg/kg dose. Additionally, 16g also exhibited satisfactory PK profiles. Eventually, 16g was selected to investigate its effect on hypoxia-reoxygenation- induced H9C2 cell viability. MTT results showed that H9C2 cell viability can be remarkably alleviated by 16g.
3,4-dibenzamido benzamide derivative, preparation method and application thereof
-
Paragraph 0161; 0164; 0165, (2016/12/22)
The invention discloses a 3,4-dibenzamido benzamide derivative (I), wherein R1, R2 and R3 are respectively and individually hydrogen, fluorine, chlorine, bromine, hydroxyl groups, alkoxy groups, amino groups or substituted amino groups. The alkoxy groups
PROCESS FOR PRODUCING 3-ACYLAMINOBENZOFURAN-2-CARBOXYLIC ACID DERIVATIVE
-
Page/Page column 22, (2008/06/13)
The present invention provides a process of preparing a compound of the formula [I]: wherein X is a group of the formula: -N="or" -CH=; R1 is a hydrogen atom, a halogen atom, a lower alkyl group, a lower alkoxy group, a cyano group or an amino group optionally substituted by a lower alkyl group; Ring A is a nitrogen-containing heterocyclic group; Ring B is an optionally substituted benzene ring or an optionally substituted pyridine ring; and R3 is a hydrogen atom or a lower alkyl group, or a pharmaceutically acceptable salt thereof , which is useful as an inhibitor of activated blood coagulation factor X.
Synthesis and biological activity of open-chain analogues of 5,6,7,8- tetrahydrofolic acid-potential antitumor agents
Bigham,Hodson,Mallory,Wilson,Duch,Smith,Ferone
, p. 1399 - 1410 (2007/10/02)
This study describes the synthesis and in vitro antitumor activity of inhibitors of purine de novo biosynthesis that are analogues of N-[4-[[3- (2,4-diamino-1,6-dihydro-6-oxo-5-pyrimidinyl)propyl]amino]benzoyl-L-glutamic acid (5-DACTHF). Benzene ring subs
Potential Antiatherosclerotic Agents. 4. benzoic Acid Analogues of Cetaben
DeVries, Vern G.,Largis, Elwood E.,Miner, Thomas G.,Shepherd, Robert G.,Upeslacis, Janis
, p. 1411 - 1421 (2007/10/02)
The synthesis of a series of analogues in which the alkyl group of cetaben is substituted with various functional groups or replaced entirely by a functionalized alkanoyl moiety is described.Also reported are the syntheses of branched-chain (alkylamino)be