Design, synthesis, and biological evaluation of pyrimidine analogs as SecA inhibitors

2021 ◽  
Author(s):  
Fante Bamba ◽  
Jinshan Jin ◽  
Arpana S. Chaudhary ◽  
Phang C. Tai ◽  
Binghe Wang
Keyword(s):  
Biological Evaluation ◽  
Design Synthesis ◽  
Pyrimidine Analogs ◽  
Synthesis And Biological Evaluation

scholarly journals Design, Synthesis and Biological Evaluation of Pyrimidine Analogues as SecA Inhibitors

2021 ◽  
Author(s):  
FANTE BAMBA ◽  
Jinshan Jin ◽  
Arpana S. Chaudhary ◽  
Phang C. Tai ◽  
Binghe Wang
Keyword(s):  
Escherichia Coli ◽  
Antimicrobial Agents ◽  
Biological Evaluation ◽  
Design Synthesis ◽  
E Coli ◽  
Secretion Pathway ◽  
Antimicrobial Studies ◽  
Pyrimidine Analogues ◽  
Pyrimidine Analogs ◽  
Synthesis And Biological Evaluation

Abstract SecA, a key component of the bacterial Sec-dependent secretion pathway, is an attractive target for the development of new antimicrobial agents. We have previously reported pyrimidine analogs as SecA inhibitors. Herein, we report an extension of the earlier work in the synthesis and evaluation of a series of 15 5-cyanothiouracil derivatives as SecA inhibitors. All the compounds have been evaluated for their inhibition of SecA ATPase (EcSecAN68) and for their antimicrobial activity against Escherichia coli NR698 (a leaky mutant) and Bacillus anthracis Sterne. Twelve compounds showed IC50 of less than 6.3 µM when tested against EcSecAN68. In antimicrobial studies against E. coli NR698, six compounds showed MIC of less than 12.5 µM with three being less than 6.3 µM. Against B. anthracis Sterne, three compounds showed MIC of less than 6.3 µM.

Design, Synthesis and Biological Evaluation of Hybrid Molecules Containing Conjugated Styryl Ketone and α-Bromoacryloyl Moieties

2012 ◽  
Vol 9 (2) ◽  
pp. 140-152 ◽  
Author(s):  
Romeo Romagnoli ◽  
Pier Giovanni Baraldi ◽  
Olga Cruz-Lopez ◽  
Maria Kimatrai Salvador ◽  
Delia Preti ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
Design Synthesis ◽  
Hybrid Molecules ◽  
Synthesis And Biological Evaluation

Design, Synthesis and Biological Evaluation of Novel Aminosaccharide Derivatives of Combretastatin A-4

2013 ◽  
Vol 10 (10) ◽  
pp. 935-941
Author(s):  
Yan Tang ◽  
Zhewei Tu ◽  
Jing Sun ◽  
Xiong Zhu ◽  
Kun Liu ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
Design Synthesis ◽  
Synthesis And Biological Evaluation ◽  
Derivatives Of

Design, Synthesis and Biological Evaluation of Benzopyran Derivatives as KATP Channel Openers

2010 ◽  
Vol 7 (6) ◽  
pp. 415-420 ◽  
Author(s):  
Jinpei Zhou ◽  
Hai Qian ◽  
Huibin Zhang ◽  
Hui Gao ◽  
Wenlong Huang ◽  
...  
Keyword(s):  
Katp Channel ◽  
Biological Evaluation ◽  
Design Synthesis ◽  
Synthesis And Biological Evaluation ◽  
Katp Channel Openers
Sign in / Sign up

Export Citation Format

Share Document