Literature DB >> 24625106

Antibacterial activity of a series of N2,N4-disubstituted quinazoline-2,4-diamines.

Kurt S Van Horn1, Whittney N Burda, Renee Fleeman, Lindsey N Shaw, Roman Manetsch.   

Abstract

A series of N(2),N(4)-disubstituted quinazoline-2,4-diamines has been synthesized and tested against multidrug resistant Staphylococcus aureus. A structure-activity and structure-property relationship study was conducted to identify new hit compounds. This study led to the identification of N(2),N(4)-disubstituted quinazoline-2,4-diamines with minimum inhibitory concentrations (MICs) in the low micromolar range in addition to favorable physicochemical properties. Testing of biological activity revealed limited potential for resistance to these agents, low toxicity, and highly effective in vivo activity, even with low dosing regimens. Collectively, these characteristics make this compound series a suitable platform for future development of antibacterial agents.

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Year:  2014        PMID： 24625106     DOI： 10.1021/jm500039e

Source DB:  PubMed          Journal:  J Med Chem        ISSN： 0022-2623            Impact factor:   7.446


  19 in total

1.  Synthesis, crystal structure and antimicrobial activity of 2-((2-(4-(1H-1,2,4-triazol-1-yl)phenyl)quinazolin-4-yl)oxy)-N-phenylacetamide derivatives against phytopathogens.

Authors:  Zhijiang Fan; Jun Shi; Na Luo; Xiaoping Bao
Journal:  Mol Divers       Date:  2018-12-03       Impact factor: 2.943

2.  Late-Stage Functionalization of Platensimycin Leading to Multiple Analogues with Improved Antibacterial Activity in Vitro and in Vivo.

Authors:  Youchao Deng; Xiang Weng; Yuling Li; Meng Su; Zhongqing Wen; Xinxin Ji; Nan Ren; Ben Shen; Yanwen Duan; Yong Huang
Journal:  J Med Chem       Date:  2019-07-02       Impact factor: 7.446

3.  SAR refinement of antileishmanial N(2),N(4)-disubstituted quinazoline-2,4-diamines.

Authors:  Xiaohua Zhu; Kurt S Van Horn; Megan M Barber; Sihyung Yang; Michael Zhuo Wang; Roman Manetsch; Karl A Werbovetz
Journal:  Bioorg Med Chem       Date:  2015-02-18       Impact factor: 3.641

4.  Synthesis and antimicrobial evaluation of novel 1,2,4-triazole thioether derivatives bearing a quinazoline moiety.

Authors:  Zhijiang Fan; Jun Shi; Xiaoping Bao
Journal:  Mol Divers       Date:  2018-03-24       Impact factor: 2.943

5.  Semisynthesis of Platensimycin Derivatives with Antibiotic Activities in Mice via Suzuki-Miyaura Cross-Coupling Reactions.

Authors:  Youchao Deng; Meng Su; Dingding Kang; Xingyun Liu; Zhongqing Wen; Yuling Li; Lin Qiu; Ben Shen; Yanwen Duan; Yong Huang
Journal:  J Med Chem       Date:  2018-12-05       Impact factor: 7.446

6.  Design, Synthesis, and Antitumor Evaluation of 4-Amino-(1H)-pyrazole Derivatives as JAKs Inhibitors.

Authors:  Xuewu Liang; Jie Zang; Mengyuan Zhu; Qianwen Gao; Binghe Wang; Wenfang Xu; Yingjie Zhang
Journal:  ACS Med Chem Lett       Date:  2016-08-23       Impact factor: 4.345

7.  Design and Synthesis of Orally Bioavailable Piperazine Substituted 4(1H)-Quinolones with Potent Antimalarial Activity: Structure-Activity and Structure-Property Relationship Studies.

Authors:  Raghupathi Neelarapu; Jordany R Maignan; Cynthia L Lichorowic; Andrii Monastyrskyi; Tina S Mutka; Alexis N LaCrue; Lynn D Blake; Debora Casandra; Sherwin Mashkouri; Jeremy N Burrows; Paul A Willis; Dennis E Kyle; Roman Manetsch
Journal:  J Med Chem       Date:  2018-02-09       Impact factor: 7.446

8.  Discovery, Synthesis, and Evaluation of 2,4-Diaminoquinazolines as a Novel Class of Pancreatic β-Cell-Protective Agents against Endoplasmic Reticulum (ER) Stress.

Authors:  Hongliang Duan; Jae Wook Lee; Sung Won Moon; Daleep Arora; Yu Li; Hui-Ying Lim; Weidong Wang
Journal:  J Med Chem       Date:  2016-08-23       Impact factor: 7.446

9.  Characterizing the Antimicrobial Activity of N2,N4-Disubstituted Quinazoline-2,4-Diamines toward Multidrug-Resistant Acinetobacter baumannii.

Authors:  Renee Fleeman; Kurt S Van Horn; Megan M Barber; Whittney N Burda; David L Flanigan; Roman Manetsch; Lindsey N Shaw
Journal:  Antimicrob Agents Chemother       Date:  2017-05-24       Impact factor: 5.191

10.  Synthesis and biofilm inhibition studies of 2-(2-amino-6-arylpyrimidin-4-yl)quinazolin-4(3H)-ones.

Authors:  Sivappa Rasapalli; Zachary F Murphy; Vamshikrishna Reddy Sammeta; James A Golen; Alexander W Weig; Roberta J Melander; Christian Melander; Prathyushakrishna Macha; Milana C Vasudev
Journal:  Bioorg Med Chem Lett       Date:  2020-09-12       Impact factor: 2.823
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