94644-47-0Relevant articles and documents
Search for the pharmacophore in prazosin for Transport-P
Zunszain, Patricia A.,Federico, Cesare,Sechi, Mario,Al-Damluji, Saad,Ganellin, C. Robin
, p. 3681 - 3689 (2007/10/03)
Partial structures of prazosin have been synthesised and tested for inhibition of Transport-P in order to identify the structural features of prazosin, which appear to be involved in binding to the putative transporter. It is shown that the pyrimidinyl 4-amino group is critically important for binding but that the 6,7-dimethoxy and 2-furoyl groups are not essential.
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.