128483-25-0Relevant academic research and scientific papers
Base-mediated one-pot synthesis of 3,4,5,6-tetrahydro-4-substituted benzo[h]quinazoline-2(1H)-thione derivatives and evaluation of their antioxidant activity
Sivakumar, Matam,Prabakaran, Kaliyan,Seenivasa Perumal, Muthu
supporting information, p. 197 - 207 (2018/01/01)
One-pot three-component Beginelli-like reactions of a ketone 1, an aryl aldehyde 2, and thiourea 3 in the presence of sodium hydroxide are described. In this reaction, 3,4,5,6-tertrahydro-4-substituted quinazoline-2(1H)-thione derivatives 4a–h were obtain
FeCl3·6H2O/TMSBr-catalyzed rapid synthesis of dihydropyrimidinones and dihydropyrimidinethiones under microwave irradiation
Zhao, Fei,Jia, Xiuwen,Li, Pinyi,Zhao, Jingwei,Huang, Jun,Li, Honglian,Li, Lin
, (2017/09/25)
An efficient and practical protocol has been developed to synthesize dihydropyrimidinones and dihydropyrimidinethiones through FeCl3 6H2O TMSBr-catalyzed three-component cyclocondensation under microwave irradiation. This approach features high yields, broad substrate scope, short reaction time, mild reaction conditions, operational simplicity and easy work-up, thus affording a versatile method for the synthesis of dihydropyrimidinones and dihydropyrimidinethiones.
Benzo[h]thiazolo[2,3-b]quinazolines by an efficient p-toluenesulfonic acid-catalyzed one-pot two-step tandem reaction
Sakram,Sonyanaik,Ashok,Rambabu,Johnmiya
, p. 1699 - 1705 (2016/03/16)
A highly efficient method has been developed for synthesis of 7,9-disubstituted-6,7-dihydro-5H-benzo[h]thiazolo[2,3-b]quinazolines via multicomponent one-pot two-step tandem reaction involving 1-tetralone, arylaldehydes, thiourea, and 4-chlorophenacyl bromide/(3-bromoacetyl)coumarin utilizing p-toluenesulfonic acid as catalyst in glacial acetic acid under reflux conditions. Analytically pure products are formed with excellent yield and short reaction time. All the synthesized compounds were confirmed by their spectral and elemental analyses. Graphical abstract: [Figure not available: see fulltext.]
Synthesis, characterization and biological evaluation of fused thiazolo[3,2-a]pyrimidine derivatives
Banothu, Janardhan,Khanapur, Manjulatha,Basavoju, Srinivas,Bavantula, Rajitha,Narra, Muralikrishna,Abbagani, Sadanandam
, p. 22866 - 22874 (2014/06/24)
A series of fused thiazolo[3,2-a]pyrimidines (7a-g, 8a-f, 11a-g and 12a,b) have been synthesized in good yields by reaction of fused 3,4-dihydropyrimidin- 2(1H)-thiones (4a-g) with phenacyl bromides (5,6)/3-(2-bromoacetyl)coumarins (9,10) under conventional heating in acetic acid. Analytical and spectral studies as well as single crystal X-ray diffraction data on the representative compound 8e confirmed the structure of all the reaction products. All the synthesized compounds were screened for their antibacterial, antioxidant and DNA cleavage activities. The compound 7e against Escherichia coli, 8a and 8c-e against Pseudomonas aeruginosa have shown prominent antibacterial activity compared to the standard drug Penicillin with MIC 9.375 μg mL-1, whereas the compounds 11c, 12a and 12b have shown very good antioxidant activity compared to the standard drug Trolox with IC50 values 12.36, 11.12 and 13.88 μM respectively. Compounds 11f and 12b have completely cleaved the DNA even at 50 μg mL-1 concentration and the remaining compounds have partially cleaved the DNA.
Efficient ionic liquid-catalysed synthesis and antimicrobial studies of 4,6-diaryl- and 4,5-fused pyrimidine-2-thiones
Gupta, Richa,Chaudhary, Ram Pal
, p. 718 - 721 (2013/02/23)
One-pot three-component condensation of aromatic ketones (1-tetralones, acetophenones, indane-1,3-dione), substituted aromatic aldehydes and thiourea in the presence of N-methylpyridinium tosylate under solvent free conditions at 100-110 °C for 2-4 h afforded tetrahydrobenzo[h]quinazoline-2-thiones, pyridimidine-2-thiones and indeno-pyrimidine-2-thiones in excellent yields. All synthesised thiones were screened for their antimicrobial activities.
Design, synthesis, and interaction study of quinazoline-2(1 H)-thione derivatives as novel potential Bcl-xL inhibitors
Feng, Yu,Ding, Xiao,Chen, Tao,Chen, Lili,Liu, Fang,Jia, Xu,Luo, Xiaomin,Shen, Xu,Chen, Kaixian,Jiang, Hualiang,Wang, Hui,Liu, Hong,Liu, Dongxiang
experimental part, p. 3465 - 3479 (2010/09/05)
Development of inhibitors to antagonize the activities of antiapoptotic Bcl-2 family proteins is of particular interest in cancer chemotherapy. We discovered a quinazoline-2(1H)-thione derivative (DCBL55) as a new Bcl-x L, Bcl-2, and Mcl-1 inhi
SYNTHESIS AND REACTIONS OF 2-MERCAPTO-4-ARYL 4H-1,2,3,4,5,6-HEXAHYDRO-BENZOQUINAZOLINES
Hammam, Abou El-Fotooh G.,Hussain, S. M.,Kotob, Iman R.
, p. 47 - 51 (2007/10/02)
2-Mercapto-4-aryl-4H-1,2,3,4,5,6-hexahydrobenzoquinazolines (2), have been synthesized.Compounds 2 reacted with chloroacetic acid, 2-bromopropanoic acid or 3-bromopropanoic acid in the presence of fused sodium acetate and acetic anhydride to give 5-ary
