30570-19-5Relevant academic research and scientific papers
New 2-aminopyrimidine derivatives and their antitrypanosomal and antiplasmodial activities
Hoffelner, Michael,Hassan, Usama,Seebacher, Werner,Dolensky, Johanna,Hochegger, Patrick,Kaiser, Marcel,M?ser, Pascal,Saf, Robert,Weis, Robert
, p. 1375 - 1385 (2020/09/17)
Abstract: Novel 2-aminopyrimidine derivatives were prepared from acyclic starting materials, benzylidene acetones and ammonium thiocyanates, via 5 steps, including ring closure, aromatization, S-methylation, oxidation to methylsulfonyl compounds, and formation of guanidines with suitable amines. The prepared compounds differ from each other by the substitutions of their amino group and of their phenyl ring. The 2-aminopyrimidines were tested by use of microplate assays for their in vitro activities against a causative organism of sleeping sickness, Trypanosoma brucei rhodesiense, as well as against a causative organism of malaria, Plasmodium falciparum NF54. Their cytotoxic properties were determined with L-6 cells (rat skeletal myoblasts). Some of the compounds exhibited quite good antitrypanosomal activity, and others showed excellent antiplasmodial activity. The influence of the structural modifications on these activities is discussed. Graphic abstract: [Figure not available: see fulltext.].
Synthesis of new 4-phenylpyrimidine-2(1H)-thiones and their potency to inhibit COX-1 and COX-2
Seebacher, Werner,Faist, Johanna,Presser, Armin,Weis, Robert,Saf, Robert,Kaserer, Teresa,Temml, Veronika,Schuster, Daniela,Ortmann, Sabine,Otto, Nadine,Bauer, Rudolf
, p. 552 - 559 (2015/07/27)
Several new 4-phenylpyrimidine-2(1H)-thiones have been prepared and investigated for their potencies to inhibit COX-1 and COX-2 enzymes, and COX-2 expression in THP-1 cells. Structure-activity-relationships and physicochemical parameters are discussed. Pharmacophore screening and docking studies were carried out for the most active compound.
Analgesic, anticonvulsant and anti-inflammatory activities of some synthesized benzodiazipine, triazolopyrimidine and bis-imide derivatives
Said, Said A.,Amr, Abd El-Galil E.,Sabry, Nermien M.,Abdalla, Mohamed M.
body text, p. 4787 - 4792 (2010/03/03)
A series of diazipine, pyrimidine, fused triazolopyrimidine and imide derivatives were newly synthesized using 4-phenyl-but-3-en-2-one 1 as a starting material and compounds 2 and 9 are intermediates. Initially the acute toxicity of the compounds was assa
