312607-68-4Relevant academic research and scientific papers
Synthesis method of 2-aminopyrimidine antiplatelet compound
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Paragraph 0027-0030; 0049-0052, (2019/11/21)
The invention discloses a synthesis method of a 2-aminopyrimidine antiplatelet compound, and the synthesis method comprises the following steps: selecting o-hydroxybenzaldehyde A and 2-bromoacetophenone B containing different substituent groups as raw materials, taking nitrogen heterocyclic carbene as a reaction catalyst, synthesizing an intermediate 1,3-diketone compound C of a novel antiplateletdrug under an alkaline condition, then synthesizing a flavonoid compound D under an acidic condition by the 1,3-diketone compound C, and finally generating the end product 2-aminopyrimidine antiplatelet compound E by the flavonoid compound D and guanidine hydrochloride under an alkaline condition. The synthesis method simplifies the original synthesis method from four steps to three steps, greatly simplifies the original synthesis method, thereby effectively reducing the production cost and the price of medicines, and improving the possibility for industrial production.
Design, synthesis and structure-activity relationships of 3,5-diaryl-1H-pyrazoles as inhibitors of arylamine N-acetyltransferase
Fullam, Elizabeth,Talbot, James,Abuhammed, Areej,Westwood, Isaac,Davies, Stephen G.,Russell, Angela J.,Sim, Edith
supporting information, p. 2759 - 2764 (2013/06/27)
The synthesis and inhibitory potencies of a novel series of 3,5-diaryl-1H-pyrazoles as specific inhibitors of prokaryotic arylamine N-acetyltransferase enzymes is described. The series is based on hit compound 1 3,5-diaryl-1H-pyrazole identified from a high-throughout screen that has been carried out previously and found to inhibit the growth of Mycobacterium tuberculosis.
Convenient one-pot synthesis of chromone derivatives and their antifungal and antibacterial evaluation
Ghani, Sherif B. Abdel,Mugisha, Patrick J.,Wilcox, Juliet C.,Gado, Emad A. M.,Medu, Erere O.,Lamb, Andrew J.,Brown, Richard C. D.
supporting information, p. 1549 - 1556 (2013/05/22)
A one-pot method for the synthesis of chromone derivatives from the reaction of 2-hydroxyacetophenones with aliphatic or aromatic acid chlorides is reported. Esterification and Baker-Venkataraman rearrangement were promoted by t-BuOK, which was followed directly by acid-catalyzed cyclization in one pot. Some of 2-cyclohexyl- and 2-cyclohexylmethyl-substituted chromones displayed activity against plant pathogenic fungal strains. Supplemental materials are available for this article. Go to the publisher's online edition of Synthetic Communications1 to view the free supplemental file. Copyright Taylor & Francis Group, LLC.
Synthesis of novel 4,6-diaryl-2-aminopyrimidines as potential antiplasmodial agents
Giridhar, Rajani,Tamboli, Riyaj S.,Prajapati, Dhaval G.,Soni, Sanket,Gupta, Sarita,Yadav
, p. 3309 - 3315 (2013/07/27)
A novel series of 4,6-diaryl-2-aminopyrimidines 8a-o has been synthesized and evaluated for in vitro antiplasmodial activity against Plasmodium falciparum. Out of the 15 compounds synthesized and tested, 6 compounds have shown IC50 values in the range of 1.61-9.53 μg/mL. These compounds are several times more potent than chloroquine and quinine, the two standard drugs used for the purpose of comparison.
Assessment of antiplatelet activity of 2-aminopyrimidines
Giridhar, Rajani,Tamboli, Riyaj S.,Ramajayam,Prajapati, Dhaval G.,Yadav
, p. 428 - 432 (2012/07/03)
A series of 4,6-diaryl-2-aminopyrimidines was developed as antiplatelet agents and their potency was evaluated by in vitro assay. Compound 14k was found to be two times more potent than aspirin. These encouraging results could be helpful for the development of new antiplatelet compounds.
