253191-91-2Relevant academic research and scientific papers
Antibacterial quinazoline compounds
-
, (2008/06/13)
Provided are compounds of formula (I) wherein X, Y and Z are independently CH or N; n is 0 or 1; R1 is selected from OH, alkoxy, aryloxy, aralkyloxy and guanidinyl; R2 and R3 are independently selected from H, halogen, amino, hydroxyl, nitro, cyano and carboxyl; R4 is H, alkyl or acyl; R5 is selected from H, hydroxyl, halogen, nitro, alkyl, alkoxy, amino, cyclic amino, alkylamino, arylamino and aralkylamino wherein the alkyl, aryl and cyclic moieties are optionally substituted; R6 and R7 are independently selected from H, alkyl, alkoxy, halogen and amino; and R8 and R9 are independently selected from H, C1-4 alkyl, alkoxy, acyl, acyloxy, alkoxycarbonyl, hydroxyl, halogen, amino and carboxyl. The compounds have therapeutic or prophylactic use for treating bacterial infection in mammals.
Structure-activity relationships of novel 2-substituted quinazoline antibacterial agents
Kung, Pei-Pei,Casper, Martin D.,Cook, Kimberley L.,Wilson-Lingardo, Laura,Risen, Lisa M.,Vickers, Timothy A.,Ranken, Ray,Blyn, Lawrence B.,Wyatt, Jacqueline R.,Cook, P. Dan,Ecker, David J.
, p. 4705 - 4713 (2007/10/03)
High-throughput screening of in-house compound libraries led to the discovery of a novel antibacterial agent, compound 1 (MIC: 12-25 μM against S. pyogenes). In an effort to improve the activity of this active compound, a series of 2-substituted quinazolines was synthesized and evaluated in several antibacterial assays. One such compound (22) displayed improved broad- spectrum antibacterial activity against a variety of bacterial strains. This molecule also inhibited transcription/translation of bacterial RNA, suggesting a mechanism for its antibiotic effects. Structure-activity relationship studies of 22 led to the synthesis of another 24 compounds. Although some of these molecules were found to be active in bacterial growth assays, none were as potent as 22. Compound 22 was tested for its ability to cure a systemic K. pneumonia infection in the mouse and displayed moderate effects compared with a control antibiotic, gentamycin.
