24030-15-7Relevant academic research and scientific papers
Design and synthesis of quinoline-pyrimidine inspired hybrids as potential plasmodial inhibitors
Kayamba, Francis,Malimabe, Teboho,Ademola, Idowu Kehinde,Pooe, Ofentse Jacob,Kushwaha, Narva Deshwar,Mahlalela, Mavela,van Zyl, Robyn L.,Gordon, Michelle,Mudau, Pertunia T.,Zininga, Tawanda,Shonhai, Addmore,Nyamori, Vincent O.,Karpoormath, Rajshekhar
, (2021/03/22)
Presently, artemisinin-based combination therapy (ACT) is the first-line therapy of Plasmodium falciparum malaria. With the emergence of malaria parasites that are resistant to ACT, alternative antimalarial therapies are urgently needed. In line with this
PPh3/I2-catalyzed one-pot synthesis of 4,6-diarylpyrimidin-2(1H)-ones
Zhang, Yanzhi,Lei, Min,Xue, Kangsheng,Sun, Guoxiang,Zhou, Yang,Hou, Jinjun,Long, Huali,Zhang, Zijia,Chen, Xubing,Wu, Wanying
supporting information, p. 3661 - 3668 (2020/09/11)
A method using PPh3/I2-catalyzed three-component Biginelli reaction of aromatic ketone, aromatic aldehyde and urea to synthesize4,6-diarylpyrimidin-2-(1H)-ones is described. Under the experimental conditions, the main reaction produc
Biological evaluation and synthesis of new pyrimidine-2(1H)-ol/-thiol derivatives derived from chalcones using the solid phase microwave method
Fandakli, Seda,Kahriman, Nuran,Yücel, Tayyibe Beyza,Alpay Karaoglu, ?engül,Yayli, Nurettin
, p. 520 - 535 (2018/06/08)
Twenty-five new hydroxy- and methoxy-substituted 4,6-diarylpyrimidin-2(1H)-ol (20–34) and 4,6-diarylpyri-midine-2(1H)-thiol derivatives (35–44) were synthesized from the reaction of the corresponding 1,3-diaryl-2-propene-1-one compounds (1–19) with urea or thiourea using the solid-phase microwave method. All the new synthetic compounds (20–44) were evaluated with regard to their α-glucosidase activity. However, only compounds 22–25, 27, 31, 34, 35, 37, and 40 exhibited a greater inhibitory effect than standard acarbose. The IC50 values of the active compounds ranged between 2.36 and 13.34 μM. The 25 new compounds were also screened for their in vitro pancreatic lipase activity and compounds 20–27 and 35–39 were found to be active. Of these compounds 26, 27, and 39 exhibited the best antilipase activities at concentrations of 0.40 ± 0.06, 0.26 ± 0.07, and 0.29 ± 0.026 μM. All the new compounds (20–44) were evaluated for their in vitro antimicrobial activity for nine test microorganisms. Compounds 20–24 and 35–39 were determined to possess a significant broad spectrum against the gram-positive bacteria Escherichia faecalis, Staphylococcus aureus, and Bacillus cereus among the tested bacterial agents. Compounds 20–24 and 35–39 exhibit the best activity against Mycobacterium smegmatis, with minimum inhibitory concentrations of 62.5–500 μg/mL, indicating their potential use as antituberculous agents.
One-pot synthesis of 4,6-diarylpyrimidin-2(1H)-ones via multi-component reaction promoted by chlorotrimethylsilane
Wang, Lizhong,Bian, Xiaoqin,Liu, Hui,Sun, Qian,Wang, Cunde
experimental part, p. 694 - 696 (2011/04/24)
4,6-Diarylpyrimidin-2(1H)-ones were effectively synthesised by utilising chlorotrimethylsilane (TMSCI) as an efficient promoter in the cyclisation condensation of arylketones, substituted benzaldehydes and urea by a one-pot, threecomponent reaction under
Cheap and efficient protocol for the synthesis of tetrahydroquinazolinone, dihydropyrimidinone, and pyrimidinone derivatives
Mirza-Aghayan, Maryam,Moradi, Alireza,Bolourtchian, Mohammad,Boukherroub, Rabah
experimental part, p. 8 - 20 (2010/03/03)
The article reports a practical, simple, and inexpensive procedure for the synthesis of tetrahydroquinazolinone and dihydropyrimidinone derivatives from aldehydes, cyclic ketones, and urea using a catalytic amount of ammonium chloride or lithium perchlorate. The protocol provides good yields and simple workup procedure for the products. By this method, we have prepared and characterized the 4-aryl-3,4,5,6-tetrahydrobenzo[h]quinazolin-2(1H)-one (3a, c, d, f, g, j, k), 4-aryl-3,4-dihydro-1H-indeno[1,2-d]pyrimidin-2(5H)-one (3b, e, h, i), 4-aryl-5,6-dihydrobenzo[h]quinazolin-2(3H)-one (3j', k', l'), and 4-aryl-3,5-dihydro-2H-indeno[1,2-d]pyrimidin-2-one (3i', m', n', o', p') derivatives. Furthermore, we have synthesized the pyrimidinone derivatives (6a'-e') using a catalytic amount of cupric chloride from aldehydes, acyclic ketones and urea. The tautomeric interconversion of pyrimidinone derivatives 6a'-e'6a''-e'' has been observed.
