33489-69-9Relevant academic research and scientific papers
Synthesis and in Vitro and in Vivo anticoagulant and antiplatelet activities of amidino- and non-amidinobenzamides
Lee, Soo Hyun,Lee, Wonhwa,Bae, Jong-Sup,Ma, Eunsook
, (2016/07/06)
Three amidino- and ten non-amidinobenzamides were synthesized as 3-aminobenzoic acid scaffold-based anticoagulant and antiplatelet compounds. The anticoagulant activities of thirteen synthesized compounds 1-13, and 2b and 3b as prodrugs were preliminary evaluated by screening the prolongation of activated partial thromboplastin time (aPTT) and prothrombin time (PT) in vitro. From the aPTT results obtained, two amidinobenzamides, N-(3′-amidinophenyl)-3-(thiophen-2″-ylcarbonylamino) benzamide (1, 33.2 ± 0.7 s) and N-(4′-amidinophenyl)-3-(thiophen-2″-ylcarbonylamino) benzamide (2, 43.5 ± 0.6 s) were selected to investigate the further anticoagulant and antiplatelet activities. The aPTT results of 1 (33.2± 0.7 s) and 2 (43.5 ± 0.6 s) were compared with heparin (62.5 ± 0.8 s) in vitro at 30 μM. We investigated the effect of 1 and 2 on blood anticoagulant activity (ex vivo) and on tail bleeding time (in vivo) on mice. A tail cutting/bleeding time assay revealed that both 1 and 2 prolonged bleeding time in mice at a dose of 24.1 g/mouse and above. Compounds 1 and 2 dose-dependently inhibited thrombin-catalyzed fibrin polymerization and platelet aggregation. In addition, 1 and 2 were evaluated on the inhibitory activities of thrombin and FXa as well as the generation of thrombin and FXa in human umbilical vein endothelial cells (HUVECs). Collectively, 1 and 2 possess some antiplatelet and anticoagulant activities and offer a basis for development of a novel antithrombotic product.
FUNCTIONALISED AND SUBSTITUTED INDOLES AS ANTI-CANCER AGENTS
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Page/Page column 81, (2015/06/08)
The present invention relates to anti-tropomyosin compounds, processes for their preparation, and methods for treating or preventing a proliferative disease, preferably cancer, using compounds of the invention.
3-(2′-Bromopropionylamino)-benzamides as novel S-phase arrest agents
Hu, Laixing,Li, Zhuo-rong,Li, Jian-Nong,Qu, Jinrong,Jiang, Jian-Dong,Boykin, David W.
, p. 6847 - 6852 (2008/09/16)
We report the synthesis, antiproliferative activity, and SAR of novel 3-(2′-bromopropionylamino)-benzamides. Many of the benzamide compounds showed potent cytotoxicities against Molt-3 leukemia cells. Several compounds exihibited cytotoxicities (under 6.5
Substituted cyclic amine compound, production process thereof and pharmaceutical composition for circulatory organ use containing the same
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, (2008/06/13)
A substituted cyclic amine compound represented by the following general formula (1) STR1 wherein each of R1 to R5 represents a hydrogen atom, a halogen atom, a lower alkyl group, a lower alkoxy group or the like, A represents a carbonyl group or a sulfonyl group, B represents a methine moiety or a nitrogen atom, D represents a methine moiety, a nitrogen atom or =N(→O)-- and n is an integer of 2 to 3; and synthetic methods thereof. The inventive compound is useful in preventing and treating circulatory organ-related diseases such as hypertension, ischemic heart disease, cerebrovascular disease, peripheral circulatory disease and the like.
