131555-40-3Relevant academic research and scientific papers
Ring closure reactions of chalcones using microwave technology
Kidwai, Mazaahir,Misra, Preeti
, p. 3237 - 3250 (1999)
The synthesis of heterocyclic compounds containing pyrimidine, pyrazoline, isoxazoline and cyclohexenone ring from chalcone derivatives containing anisole and 3'4'-methylenedioxy phenyl ring under 'dry conditions' using microwaves and by conventional meth
Pyrimidine-2-thione derivatives as corrosion inhibitors for mild steel in acidic environments
Soltani,Behpour,Oguzie,Mahluji,Ghasemzadeh
, p. 11145 - 11162 (2015)
The inhibition of mild steel corrosion in 1.0 M sulphuric acid by pyrimidine-2-thione derivatives (4,6-diphenyl-3,4-dihydropyrimidine-2(1H)-thione (PTH); 4-(4-methylphenyl)-6-phenyl-3,4-dihydropyrimidine-2(1H)-thione (PTM) and 4-(4-methoxyphenyl)-6-phenyl
Synthesis, evaluation of biological activity, docking and molecular dynamic studies of pyrimidine derivatives
Amanlou, Massoud,Amini, Mohsen,Boumi, Shahin,Moghimirad, Jafar,Ostad, Seyed Nasser,Tavajohi, Shohreh
, p. 212 - 225 (2021/03/19)
The microtubule is composed of αβ-tubulin heterodimers and is an attractive target for the design of anticancer drugs. Over the years, various compounds have been developed and their effect on tubulin polymerization has been studied. Despite great efforts to make an effective drug, no drug has been introduced which inhibit colchicine binding site. In the current work, a series of pyrimidine derivatives were designed and synthesized. Furthermore, their cytotoxic activities were evaluated and molecular docking studies were performed. Twenty compounds of pyrimidine were synthesized in 2 different groups. In the first group, 4,6-diaryl pyrimidine was connected to the third aryl group via thio-methylene spacer. In the second group, this linker was substituted by S-CH2-triazole moiety. The cyto-toxic activity of these compounds was evaluated against 4 different cell lines (HT-29, MCF-7, T47D, NIH3T3). Compounds 6d, 6m, 6p showed potent cytotoxic activity against MCF7 cancerous cell lines. Between these compounds, compound 6p did not show cytotoxic activity against NIH-3T3 (normal cell) cell line. Docking studies show that these compounds occupy colchicine binding site in tubulin protein and probably their anticancer mechanism is inhibition of tubulin polymerization. Altogether, with respect to obtained results, it is attractive and beneficial to further investigation on pyrimidine scaffold as antimitotic agents. Attention to the selectivity index of 6p on MCF7 cell line could be valu-able in design new chemical agents for the treatment of breast cancer.
Facile one-pot three-component synthesis of 4,6-diaryl-3,4-dihydropyrimidine-2(1H)-thiones under ultrasonic irradiation
Abbass, Shymaa A.,Moustafa, Gamal A. I.,Hassan, Heba A.,Abuo-Rahma, Gamal El-Din A.
supporting information, p. 2995 - 3000 (2019/08/22)
We developed a facile one-pot procedure for the synthesis of 4,6-diaryl-3,4-dihydropyrimidine-2(1H)-thione under ultrasonic irradiation. The method is based on a three components reaction of aldehydes, ketones, and thiourea under basic conditions affordin
Biological evaluation of halogenated thiazolo[3,2-a]pyrimidin-3-one carboxylic acid derivatives targeting the YycG histidine kinase
Zhao, Dan,Chen, Chen,Liu, Huayong,Zheng, Likang,Tong, Yao,Qu, Di,Han, Shiqing
supporting information, p. 500 - 507 (2015/01/09)
With an intention to potent inhibitors of YycG histidine kinase, a series of halogenated thiazolo[3,2-a]pyrimidin-3-one carboxylic acid derivatives were synthesized and evaluated for their antibacterial, antibiofilm and hemolytic activities. The majority of the compounds showed good activity against Staphylococcus epidermidis and Staphylococcus aureus, with MIC values of 1.56-6.25 μM, simultaneously presented promising antiobifilm activity against S. epidermidis ATCC35984 at 50 μM. The test of inhibitory activity on YycG kinase suggested the antibacterial activities of these derivatives are based on inhibiting the enzyme activity of the YycG HK domain. The hemolytic activity test suggested these compounds exhibited in vitro antibacterial activity at non-hemolytic concentrations.
Synthesis, antimicrobial and DFT studies of novel fused thiazolopyrimidine derivatives
Gupta, Richa,Chaudhary, Ram Pal
, p. 207 - 214 (2013/09/02)
The reaction of dihydropyrimidine-2(1H)-thione 4, obtained by the condensation of chalcone 3 with thiourea, with chloroacetic acid and 1,2-dibromoethane furnished compounds 5 and 6 and not their respective isomers 8 and 9. The regiochemistry of the cycliz
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.
Facile Biginelli-type reactions catalysed by super acidic ionic liquid under solvent-free conditions
Wang, Liang,Zhou, Min,Chen, Qun,He, Ming-Yang
, p. 712 - 714 (2013/02/23)
[MeC(OH)2]+ClO4-?as a super acidic ionic liquid is an extremely active catalyst for Biginelli-type reactions. The present method is especially effective for the inactive aliphatic aldehydes. The solvent-free conditions, high catalytic activity, wide substrates tolerance and convenient product isolation make the protocol more advantageous.
Ultrasound-assisted synthesis of dihydropyrimidine-2-thiones
Safaei-Ghomi, Javad,Ghasemzadeh, Mohammad Ali
experimental part, p. 679 - 684 (2012/01/16)
Chalcone derivatives were prepared by the condensation of various substituted aryl aldehydes and acetophenone in alkaline ethanol, while pyrimidine- 2-thione derivatives were prepared by the combination of chalcones and thiourea under conventional and ult
Synthesis of 3,4-dihydropyrimidin-2(1H)ones and 3,4,5,6,7,8- hexahydroquinazolin-2(1H)-ones via three component cyclocondensation
Phucho,Nongpiur,Nongrum,Nongkhlaw
experimental part, p. 346 - 350 (2010/10/03)
3,4 Dihydropyrimidin-2(1H)-ones and 3,4,5,6,7,8-hexahydroquinazolin-2(1H)- ones have been synthesized from the condensation of ketones, aldehydes and urea/thiourea in the presence of sodium tertiary butoxide by the solventless microwave irradiation (MWI)
