ChemInform Abstract: 2(1H)‐Quinolinone Derivatives as Novel Antiarteriostenotic Agents Showing Antithrombotic and Antihyperplastic Activities.

Abstract

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Asymmetric Amination of meso-Epoxide with Vegetable Powder as a Low-Toxicity Catalyst

“…Chiral β-aminoalcohol units are found in many bioactive compounds used for the therapeutic treatment of various diseases [1][2][3]. Chiral trans-β-aminocyclohexanol derivatives are particularly useful substrates as key intermediates for the synthesis of 1-cyclopropyl-1-((1R,2R)-2-hydroxycyclohexyl)-3-(3-((2-oxo-1,2-dihydroquinolin-6-yl)oxy)propyl)urea, which is a phosphodiesterase III inhibitor with vascular hypertrophy effects, and (R)-1-((1R,2R)-2-(3,4dimethoxyphenethoxy)cyclohexyl)-pyrrolidin-3-ol, which is an antiarrhythmic agent ( Figure 1) [4][5][6]. The most effective method to synthesize chiral trans-β-aminocycloalkanols is the catalytic asymmetric amination of the corresponding 1,2-epoxycycloalkanes.…”

Design, synthesis and pharmacological evaluation of 6-hydroxy-4-methylquinolin-2(1H)-one derivatives as inotropic agents

“…Indeed, cilostazol (OPC-13013) has been available clinically for a long time as a vasodilator and anti-platelet drug ( Figure 1) [13][14][15]. Cilostamide (potent and selective PDE3 inhibitors: IC 50 = 70 nM [16,17]; IC 50 (PDE3A) = 27 nM and IC 50 (PDE3B) = 50 nM [18]) possesses both antithrombotic and antiintimal hyperplastic actions [7,11,19]. In summary, cilostamide is a highly functionalized compound which shows potent activity of PDE3 inhibitory [3,16,20,21] lead to cardiotonic effects [22], inhibition of platelet aggregation [7,18,23] and increase in the secretion of Insulin-stimulated glucose [24].…”

“…In summary, cilostamide is a highly functionalized compound which shows potent activity of PDE3 inhibitory [3,16,20,21] lead to cardiotonic effects [22], inhibition of platelet aggregation [7,18,23] and increase in the secretion of Insulin-stimulated glucose [24]. Unfortunately, this compound shows the side effect of tachycardia [19]. Since last three decades, too many related analogs of cilostamide have been synthesized and biologically evaluated [19,21,25,26].…”

“…Unfortunately, this compound shows the side effect of tachycardia [19]. Since last three decades, too many related analogs of cilostamide have been synthesized and biologically evaluated [19,21,25,26].…”