title: Synthesis and antibacterial properties of pyrimidine derivatives.
abstract: The paper presents the synthesis of 1,2,3,7-tetraaryl-1,2,3,4-tetrahydropyrimido[4,5-d]pyrimidines. The structures of the obtained compounds were confirmed by crystallographic and spectroscopic analyses, and their antibacterial activity was tested on 9 selected strains, comparing chemical structure changes with increased microbiological activity. It was confirmed that aromatic residues in the hydrogenated pyrimidine ring constitute a significant element influencing antibacterial activity. Electronegative radicals increase microbiological activity, but decrease solubility of the compounds. Therefore, substituents should be selected in a manner ensuring a balanced effect. The presented crystal structure of 6f includes two stereoisomers, which we decided to isolate and compare the microbiological properties in further studies.
authors.affiliation: Department of Organic Chemistry, Wrocław Medical University, Grodzka St. 9, 50-137 Wrocław, Poland. jerzycieplik@o2.pl
authors.forename: Jerzy
authors.initials: J
authors.lastname: Cieplik
authors.forename: Marcin
authors.initials: M
authors.lastname: Stolarczyk
authors.forename: Janusz
authors.initials: J
authors.lastname: Pluta
authors.forename: Olaf
authors.initials: O
authors.lastname: Gubrynowicz
authors.forename: Iwona
authors.initials: I
authors.lastname: Bryndal
authors.forename: Tadeusz
authors.initials: T
authors.lastname: Lis
authors.forename: Marcin
authors.initials: M
authors.lastname: Mikulewicz
mesh_terms: D000704:Analysis of Variance; D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D001419:Bacteria / Q000187:drug effects / Q000254:growth & development; D018360:Crystallography, X-Ray; D009682:Magnetic Resonance Spectroscopy; D008826:Microbial Sensitivity Tests; D003904:Mitosporic Fungi / Q000187:drug effects / Q000254:growth & development; D015394:Molecular Structure; D011743:Pyrimidines / Q000138:chemical synthesis* / Q000494:pharmacology*; D013055:Spectrophotometry, Infrared; D013329:Structure-Activity Relationship
chemical_list: D000900:Anti-Bacterial Agents; D011743:Pyrimidines