938524-81-3Relevant academic research and scientific papers
Synthesis and structure-activity relationship of: N 4-benzylamine- N 2-isopropyl-quinazoline-2,4-diamines derivatives as potential antibacterial agents
Jiang, Zhengyun,Hong, W. David,Cui, Xiping,Gao, Hongcan,Wu, Panpan,Chen, Yingshan,Shen, Ding,Yang, Yang,Zhang, Bingjie,Taylor, Mark J.,Ward, Stephen A.,O'Neill, Paul M.,Zhao, Suqing,Zhang, Kun
, p. 52227 - 52237 (2017)
A series of N4-benzylamine-N2-isopropyl-quinazoline-2,4-diamine derivatives has been synthesized and tested for antibacterial activity against five bacterial strains. Twelve different substituents on the N4-benzylamine group have been investigated along with replacement of the quinazoline core (with either a benzothiophene or regioisomeric pyridopyrimidine ring systems). In order to develop structure activity relationships, all derivatives were tested for their antibacterial activities against Escherichia coli and Staphylococcus aureus via Kirby-Bauer assays and minimum inhibitory concentration assays. Eight of the most potent compounds against S. aureus and E. coli were also screened against one strain of methicillin-resistant S. aureus (MRSA), Staphylococcus epidermidis and Salmonella typhimurium to further examine their antibacterial activities. Lead compound A5 showed good activities with MICs of 3.9 μg mL-1 against E. coli, S. aureus and S. epidermidis and 7.8 μg mL-1 against MRSA. Selected front runners were also screened for their DMPK properties in vitro to assess their potential for further development.
USE OF COMPOUNDS FOR PREPARING ANTI-TUBERCULOSIS AGENTS
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Page/Page column 13; 15, (2010/12/29)
Compounds of a compound of compound of general formula (I) wherein X1, X2, A, R1R2, R3 and R4 are as defined herein; are useful as anti-mycobacterial agents, especially agents for the treatment of tuberculosis.
