68357-48-2Relevant academic research and scientific papers
Synthesis and pharmacological investigation of novel 1-substituted-4- phenyl-1,2,4-triazolo[4,3-a]quinazolin-5(4H)-ones as a new class of H 1-antihistaminic agents
Alagarsamy, Veerachamy,Giridhar, Rajani,Yadav, Mangai Ram
, p. 1877 - 1880 (2005)
A series of novel 1-substituted-4-phenyl-1,2,4-triazolo[4,3-a]quinazolin- 5(4H)-ones 7 were synthesized by the cyclization of 2-hydrazino-3- phenylquinazolin-4(3H)-one 6 with various one carbon donors. The starting material 2-hydrazino-3-phenylquinazolin-4(3H)-one 6, was synthesized from aniline 1 by a novel innovative route. When tested for their in vivo H 1-antihistaminic activity on conscious guinea pigs all the test compounds protected the animals from histamine induced bronchospasm significantly, whereas the compound 1-methyl-4-phenyl-1,2,4-triazolo[4,3-a] quinazolin-5(4H)-one 7b (percentage protection 70.7%) was found to be equipotent with the reference standard chlorpheniramine maleate (percentage protection 71%). These compounds show negligible sedation (～5%) when compared to the reference standard (26%). Hence they could serve as prototype molecules for future development.
Synthesis and Anticonvulsant Activity Evaluation of 4-Phenyl-[1,2,4]triazolo[4,3-a]quinazolin-5(4H)-one and Its Derivatives
Zhang, Hong-Jian,Jin, Peng,Wang, Shi-Ben,Li, Fu-Nan,Guan, Li-Ping,Quan, Zhe-Shan
, p. 564 - 574 (2015/08/06)
A series of 4-(substituted-phenyl)-[1,2,4]triazolo[4,3-a]quinazolin-5(4H)-ones (6a-x) with triazole and other heterocyclic substituents (7-14) were synthesized and the compounds were evaluated for their anticonvulsant activity and neurotoxicity by maximal electroshock (MES) and rotarod neurotoxicity tests. Among the compounds studied, 6o and 6q showed wide margins of safety with protective indices (PIs) that were much higher than those of currently used drugs (PI6o > 25.5, PI6q > 26.0). Compounds 6o and 6q showed significant oral activity against MES-induced seizures in mice, with ED50 values of 88.02 and 94.6 mg/kg, respectively. The two compounds were also found to have potent activity against seizures that were induced by pentylenetetrazole and bicuculline. A series of 4-(substituted-phenyl)-[1,2,4]triazolo[4,3-a]quinazolin-5(4H)-ones with triazole and other heterocyclic substituents were synthesized and the compounds were evaluated for their anticonvulsant activity and neurotoxicity using maximal electroshock and rotarod neurotoxicity tests.
Synthesis of the 1,2,4-Triazoloquinazolin-5-ones and Related Compounds
El-Sherief, H. A.,Abdel-Rahman, A. E.,El-Naggar, G. M.,Mahmoud, A. M.
, p. 1227 - 1230 (2007/10/02)
2-Hydrazino-3-phenyl-4(3H)-quinazolinone (1) underwent ring closure with aliphatic acid, aldehydes, and carbon disulfide to 1-alkyl-, 1-aryl-, and 1-mercapto-4-phenyl-1,2,4-triazoloquinazolin-5(4H)-ones (7) for instance.The 1-alkylthio-3-phenyl-1,2
