Synthesis of 1-Substituted-4-(Pyridin-4-yl) [1,2,4] Triazolo [4,3-a] Quinazolin-5(4H)-ones as a New Class of H1- Antihistaminic Agents

Abstract

Purpose: To synthesize a new series of 1-substituted-4-(pyridin-4-yl) [1,2,4] triazolo [4,3-a]

The synthesis, computer prediction of the biological activity and the acute toxicity of 1-Ar-4-R-[1,2,4]triazolo[4,3-a] quinazolin-5(4H)-ones

“…The data of computer prediction of the biological activity obtained are fully consistent with the fact that [1,2,4]triazolo[4,3-a]quinazolin-5(4H)-one derivatives are similar in their chemical structure to the chemical structures described as promising nonsedative H1-antihistaminic drugs [1][2][3][4][5][6][7][8][9][10][11].…”

“…Derivatives of [1,2,4] triazolo [4,3-a]quinazolin-5(4H)-one, which are representatives of the important class of condensed heterocycles possessing a wide range of the biological activity, attract particular interest in this direction. Among their potential pharmacologically significant properties the H1-antihistaminic [1][2][3][4][5][6][7][8][9][10][11], anticonvulsant [12], antibacterial [13][14][15], antitubercular [13,15], antifungal [13,14], anticancer [15], anti-asthmatic [10,16], antiHIV [13], anti-allergic [16], anti-inflammatory [16,17] bioactivities should be mentioned. It determines the prospects for developing synthetic approaches to fundamentally new compounds of the specified class.…”

Synthesis of New Rhodanine, Thiazole, Quinazolin-4-One, Imidazolone and Pyranothiazole Derivatives Incorporating Antipyrine Moiety as Antimicrobial Agents

“…The 1 H NMR spectra of 26 revealed the characteristic methylene proton at δ 4.34 (CH 2 ). Also, the literature indicated that methyl dithiocarbamate group in compound 3 reacts with anthranilic acid or methyl anthrnilate, leading to the formation of quinazoline and its derivatives [19][20][21][22][23]. Thus, interaction of 3 with anthranilic acid in refluxing ethanol in the presence of TEA as catalyst to yield the thiourea intermediate 27 which underwent cyclization via loss of water molecule yielding quinazoline derivative 28, Figure 4 .…”

Pd(II)-Catalyzed Cascade Annulation of o-Aminobenzoic Acids with CO, Amines, and Aldehydes to N3-/N1,N3-Substituted 2,3-Dihydroquinazolin-4(1H)-ones

“…As important and useful fused heterocycles, N 3-substituted and N 1, N 3-disubstituted 2,3-dihydroquinazolin-4­(1 H )-ones have drawn much attention due to their broad range of pharmacological and biological properties, such as anticancer, antidiabetic, antihypertensive, anti-inflammatory, , antibacterial, antihistaminic, antiviral, antitumor, diuretic, , vasodilatory, , antiobesity, , antimalarial, anthelmintic, anti-Shiga toxin, antiricin, antimicrobial, , and anticonvulsant activities. In addition, N 3-substituted 2,3-dihydroquinazolin-4­(1 H )-ones can also be readily oxidized to the corresponding quinazolin-4­(3 H )-one derivatives, which are important building blocks in natural products and synthetic drugs .…”