2012
DOI: 10.1021/ml300217f
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Novel 2-Aminobenzamides as Potential Orally Active Antithrombotic Agents

Abstract: ABSTRACT:In an effort to develop potent antithrombotic agents, a series of novel 2-aminobenzamide derivatives were synthesized and screened for their in vivo antithrombotic activity. Among the 23 compounds tested, compound (8g) showed the most promising antithrombotic activity, which was comparable with clinically used aspirin or warfarin, but at variance with these standard drugs, 8g did not exhibit the increased bleeding time, suggesting its potential as a novel antithrombotic agent.

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Cited by 3 publications
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“…4 Specically 2aminobenzamide and its derivatives are used in the blood coagulation cascade. 5 They may serve as lead candidates in the development of novel anticancer agents 6 (Fig. 1a) and also can act as bioinspired molecular electrodes (Fig.…”
Section: Introductionmentioning
confidence: 99%
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“…4 Specically 2aminobenzamide and its derivatives are used in the blood coagulation cascade. 5 They may serve as lead candidates in the development of novel anticancer agents 6 (Fig. 1a) and also can act as bioinspired molecular electrodes (Fig.…”
Section: Introductionmentioning
confidence: 99%
“…6 (a) Solvatochromic study of compound 3i; (b) normalized fluorescence spectra of compound 3i in various solvents. Solvents: from left to right, 1, DCM; 2, DMF; 3, acetonitrile; 4, THF;5, chloroform; 6, acetone;7, ethyl acetate;8, dioxane;9, DMSO; and 10, ethanol.…”
mentioning
confidence: 99%
“…O -Aminobenzamides and their derivatives have attracted special research interest due to their remarkable applications as important reactive intermediates in organic synthesis . In addition, they also find utilization in medicinal chemistry due to their biological activities such as antimicrobial activity, antithrombotic activity, glycogen phosphorylase inhibition, and thyroid-stimulating hormone receptor (TSHR) antagonistic activity . The main methods for the synthesis of these compounds involve the ring opening of isatoic anhydride, , coupling of anthranilic acid with amines, , N -arylation between 2-bromobenzenamine and benzonitrile, the amidation of alcohols with 2-aminobenzonitrile, or N -Fries rearrangement of N -carbamoyldiarylamines .…”
mentioning
confidence: 99%