71834-49-6Relevant academic research and scientific papers
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.
, p. 2995 - 3000 (2019)
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
Novel potent and selective DPP-4 inhibitors: Design, synthesis and molecular docking study of dihydropyrimidine phthalimide hybrids
Mourad, Ahmed A. E.,Khodir, Ahmed E.,Saber, Sameh,Mourad, Mai A. E.
, p. 1 - 24 (2021/02/26)
Background: Dipeptidyl peptidase-4 (DPP-4) inhibitors have emerged as antihyperglycemic agents that improve glycemic control in type 2 diabetic patients, either as monotherapy or in combination with other antidiabetic drugs. Methods: A novel series of dihydropyrimidine phthalimide hybrids was synthesized and evaluated for their in vitro and in vivo DPP-4 inhibition activity and selectivity using alogliptin as reference. Oral glucose tolerance test was assessed in type 2 diabetic rats after chronic treatment with the synthesized hybrids ± metformin. Cytotoxicity and antioxidant assays were performed. Additionally, molecular docking study with DPP-4 and structure activity relationship of the novel hybrids were also studied. Results: Among the synthesized hybrids, 10g, 10i, 10e, 10d and 10b had stronger in vitro DPP-4 inhibitory activity than alogliptin. Moreover, an in vivo DPP-4 inhibition assay revealed that 10g and 10i have the strongest and the most extended blood DPP-4 inhibitory activity compared to alogliptin. In type 2 diabetic rats, hybrids 10g, 10i and 10e exhibited better glycemic control than alogliptin, an effect that further supported by metformin combination. Finally, 10j, 10e, 10h and 10d had the highest radical scavenging activity in DPPH assay. Conclusions: Hybrids 10g, 10i and 10e are potent DPP-4 inhibitors which may be beneficial for T2DM treatment.
3 - benzoyl - 5, 7 - diphenyl - 5H - thiazolo [3, 2 - a] pyrimidine derivatives and application thereof
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Paragraph 0018-0020, (2017/08/25)
The invention discloses application of 3-benzoyl-5, 7-diphenyl-5H-thiazole [3, 2-a] pyrimidine derivatives shown in a general formula to antibacterial drugs, wherein R1, R2 and R3 are hydrogen, methyl, halogen, hydroxyl, methoxyl, nitryl, ethanoyl, propionyl or alkoxyl which are separated from each other respectively. The compound has an obvious inhibiting effect in the plurality of bacteria such as meticillin-resistant staphylococcus aureus, escherichia colim, pseudomonas aeruginosa and the like, and can be used for preparing the antibacterial drugs.
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.
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)
