53278-67-4Relevant academic research and scientific papers
Synthesis, XRD, EXAFS and XANES study of Cu(II) complexes of aniline dithiocarbamate
Geete, Anurag,Shrivastava,Mishra, Ashutosh
, p. 627 - 633 (2020)
In present investigation, seven copper(II) complexes were synthesized using various aniline dithiocarbamate. The synthesized Cu(II) complexes were studied for different structural and chemical parameters using XRD, EXAFS and XANES. The output obtained fro
Amine-carbon disulfide promoted synthesis of novel benzo[e][1,3]thiazepin-5(1H)-one derivatives
Asgari, Mohammad Sadegh,Bahadorikhalili, Saeed,Asadi, Mehdi,Rashidi Ranjbar, Parviz,Larijani, Bagher,Rahimi, Rahmatollah,Mahdavi, Mohammad
, p. 413 - 418 (2019/12/24)
In this paper, a simple method is introduced for the synthesis of novel 4-substituted-3-thioxo-3,4-dihydrobenzo[e][1,3]thiazepin-5(1H)-one derivatives. The synthesis is based on a two-step reaction of 2-methylbenzoic acid, an amine, and carbon disulfide. In the first step, 2-methylbenzoic acid reacts with sulfuric acid in ethanol, followed by the reaction with N-bromosuccinimide to produce ethyl 2-(bromomethyl)benzoate. Amine and carbon disulfide react in a separate flask in basic medium to give carbamodithioate salt. Carbamodithioate and ethyl 2-(bromomethyl)benzoate react together in dimethylformamide to produce the desired 4-substituted-3-thioxo-3,4-dihydrobenzo[e][1,3]thiazepin-5(1H)-one derivatives. The method is simple and fast and is applicable to a wide variety of substrates and gives the desired products in high isolated yields.
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.
Syntheses and antimicrobial activities of 1-(3-benzyl-4-oxo-3,4-dihydroquinazolin-2-yl)-4-(substituted) thiosemicarbazide derivatives
Alagarsamy, Veerachamy,Solomon, Viswas Raja,Krishnamoorthy,Sulthana,Narendar
, p. 1471 - 1479 (2016/02/18)
A series of 1-(3-benzyl-4-oxo-3,4-dihydroquinazolin-2-yl)-4- (substituted) thiosemicarbazides (AS1-AS10) were obtained by the reaction of 3-benzyl-2-hydrazino-3H-quinazolin-4-one (6) with different dithiocarbamic acid methyl ester derivatives. The key intermediate, 3-benzyl-2-thioxo-2,3- dihydro-1H-quinazolin-4-one (4), was obtained by the reaction of benzyl amine (1) with carbon disulphide and sodium hydroxide in dimethyl sulphoxide to give sodium dithiocarbamate, which was methylated with dimethyl sulphate to yield the dithiocarbamic acid methyl ester 2 and condensation with methyl anthranilate (3) in ethanol yielded the desired compound (4) via the thiourea intermediate. The SH group of compound (4) was methylated in the favourable nucleophilic displacement reaction with hydrazine hydrate, which afforded 3-benzyl-2-hydrazino-3H-quinazolin-4-one (6). The IR, and 1H- and 13C-NMR spectra of these compounds showed the presence of peaks due to thiosemicarbazides, carbonyl (C=O), NH and aryl groups. The molecular ion peaks of the quinazolin-4-one moiety (m/z 144) were observed in all the mass spectra of the compounds AS1-AS10. Elemental (C, H, N) analysis satisfactorily confirmed purity and elemental composition of the synthesized compounds. All the synthesized compounds were screened for their antimicrobial activity against selective gram positive and gram negative bacteria by agar dilution method. In the present study, compounds AS8 and AS9 emerged as the most active compounds of the series.
