66679-64-9Relevant academic research and scientific papers
Antimicrobial activities of some synthesized 1-(3-(2-methylphenyl)-4-Oxo-3H-quinazolin-2-yl-4-(substituted)thiosemicarbazide derivatives
Alagarsamy,Anjana,Sulthana,Parthiban,Solomon, V. Raja
, p. 332 - 339 (2016/07/06)
The substituted thiosemicarbazide moiety was placed at the C-2 position and 2-methylphenyl group at N-3 position of quinazoline ring and obtained compounds were tested for their antitubercular activities and antibacterial activities against selected gram-positive and gram-negative bacteria. The target compounds 1-(3-(2-methylphenyl)-4-oxo-3H-quinazolin-2-yl)-4-(substituted) thiosemicarbazides were obtained by the reaction of 2-hydrazino-3-(2-methylphenyl) quinazolin-4(3H)-one with different dithiocarbamic acid methyl ester derivatives. All synthesized compounds were also screened for their antimicrobial activity against selective gram-positive and gram-negative bacteria by agar dilution method. Among the series, 1-[3-(2-methylphenyl)-4-oxo-3H-quinazolin-2-yl]-4-[4-chlorophenyl]-thiosemicarbazide exhibited the most potent activity against S. typhi, E. coli, and B. subtilis, while 1-[3-(2-methylphenyl)-4-oxo-3H-quinazolin-2-yl]-4-[4-nitrophenyl]-thiosemicarbazide was the most potent against E. coli, B. subtilis, P. aeruginosa, S. typhi, and S. flexneri. These two compounds exhibited the antitubercular activity at the minimum concentration (3 μg/mL) that offered potential for further optimization and development of new antitubercular agents. The obtained results demonstrated promising antimicrobial and antitubercular activities of the synthesized quinazoline compounds which could be used as new scaffolds for improving their antimicrobial activity.
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.
Cynogen bromide and ethylacetoacetate in heterocyclization: Novel synthesis of tetracyclic derivative of 3-aryl quinazolinones
Deshmukh,Patil, Suresh S.,Patil, Sanjeevani S.,Jadhav, Swati D.
experimental part, p. 1144 - 1147 (2010/11/03)
(Chemical Equation Presented) In this work, tricyclic 1-amino-4- (substituted phenyl)[1,2,4]triazolo[4,3-a]quinazolin-5(4H)-one 3 was synthesized by treatment of 2-hydrazinyl-3-(substituted phenyl)quinazolin-4(3H)-one 2 with cyanogen bromide, which on cyc
Synthesis and pharmacological investigation of novel 4-(2-methylphenyl)-1-substituted-4H-[1,2,4]triazolo[4,3-a]quinazolin-5-o nes as new class of H1-antihistaminic agents
Alagarsamy,Rupeshkumar,Kavitha,Meena,Shankar,Siddiqui,Rajesh
, p. 2331 - 2337 (2008/12/23)
A series of novel 1-substituted-4-(2-methylphenyl)-4H-[1,2,4]triazolo[4,3-a]quinazolin-5-o nes were synthesized by the cyclization of 2-hydrazino-3-(2-methylphenyl)-3H-quinazolin-4-one with various one carbon donors. The starting material 2-hydrazino-3-(2
Synthesis and pharmacological evaluation of some 3-(2-methylphenyl)-2- substituted amino-quinazolin-4(3H)-ones as analgesic and anti-inflammatory agents
Alagarsamy, Veerachamy,Solomon, Viswas Raja,Murugesan, Sankaranarayanan
, p. 174 - 181 (2008/09/19)
A variety of novel 3-(2-methylphenyl)-2-substituted amino-quinazolin-4(3H)- ones were synthesized by reacting the amino group of 2-hydrazino-3-(2- methylphenyl)-quinazolin-4(3H)-one with a variety of aldehydes and ketones. The starting material 2-hydrazino-3-(2-methylphenyl)-quinazolin-4(3H)-one was synthesized from 2-methyl aniline. The title compounds were investigated for analgesic, anti-inflammatory and ulcerogenic index activities. Among these, the compound 2-(1-ethylpropylidene)-hydrazino-3-(2-methylphenyl)-quinazolin-4(3H)- one emerged as the most active compound for analgesic activity, while the compound 2-(1-methylbutylidene)-hydrazino-3-(2-methylphenyl)-quinazolin-4(3H)- one showed most potent anti-inflammatory activity of the series and was moderately more potent in its anti-inflammatory activity when compared to the reference standard diclofenac sodium (CAS 15307-86-5). Interestingly, the test compounds showed only mild ulcerogenic potential when compared to acetylsalicylic acid (CAS No: 50-78-2). ECV - Editio Cantor Verlag.
