Design, synthesis, and biological evaluation of pyrimidine analogs as SecA inhibitors
| Autor: | Fante Bamba, Jinshan Jin, Arpana S. Chaudhary, Binghe Wang, Phang C. Tai |
|---|---|
| Rok vydání: | 2021 |
| Předmět: |
biology
010405 organic chemistry Chemistry ATPase Organic Chemistry Mutant biology.organism_classification medicine.disease_cause Antimicrobial 01 natural sciences 0104 chemical sciences Bacillus anthracis 010404 medicinal & biomolecular chemistry Pyrimidine analogue Biochemistry biology.protein medicine bacteria Bioorganic chemistry General Pharmacology Toxicology and Pharmaceutics IC50 Escherichia coli |
| Zdroj: | Medicinal Chemistry Research. 30:1334-1340 |
| ISSN: | 1554-8120 1054-2523 |
| DOI: | 10.1007/s00044-021-02717-6 |
| Popis: | 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 |
| Databáze: | OpenAIRE |
| Externí odkaz: |
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