Synthesis and pharmacological investigation of novel 4-benzyl-1-substituted-4H-[1,2,4]triazolo[4,3-a]quinazolin-5-ones as new class of H1-antihistaminic agents

Convenient synthesis of 1-substituted-4-methyl-5-oxo [1,2,4]triazolo[4,3-a]quinazolines

“…[1][2][3] Furthermore, a series of novel 1-substituted 4-aryl [1,2,4]triazolo [4,3-a]quinazolin-5(4H)-ones II was reported as a new class of non sedative H1-antihistamines. [4][5][6] Hydrazone derivatives are reported to possess antimicrobial, [7][8][9] antitubercular, 10 anticonvulsant 11 and analgesic-anti-inflammatory 12,13 activities. Compound III which possesses a hydrazide-hydrazone structure, is used as antimicrobial.…”

Synthesis and characterization of some new 4-heteroaryl quinazoline and fused triazolo quinazoline derivatives

“…Incorporate 1,2,4-triazole moiety at 4 position of quinazoline derivatives is proven as a new class of H1-antihistaminic [26]. In this respects, a successful attempt for synthesizing 1,2,4-trizole-quinazoline derivatives was achieved via a one-pot reaction, where the hydrazinolysis of chloroquinazoline 2 and subsequent condensation with different aromatic aldehydes, namely salicylaldehyde, 4-methoxy benzaldehyde, and cinnamaldehyde furnished a series of 5-substituted trizolo-quinazolines 7a-c. Additionally, the course of such reaction is chemically investigated via generating the 4-hydrazino-quinazoline system 8 as an isolated intermediate.…”

Boric acid catalyzed one-pot synthesis of [1,2,4] triazolo quinazolinone Derivatives

“…One pot MCR provides many chemical reactions which attributes such as minimization of use of silica gel for chromatographic purification of intermediate compounds, use of solvent 5 . MCR's have been exploited as a powerful tool for the assembly of large library of biologically active molecules 6 .Nitrogen containing heterocyclic, triazolo quinazolinone ring system exhibit biological activities such as antihypertensive 7 , antihistamic 8 , analgesic, anti-inflammatory 9 , anticancer 10 and anti-HIV activities 11a . More over many naturally occurring and synthetic compounds containing triazole derivatives scaffold also posses interesting diverse pharmaceutical, agrochemical properties.…”