| Autor: |
Haranahalli, Krupanandan, Tong, Simon, Kim, Saerom, Awwa, Monaf, Chen, Lei, Knudson, Susan E., Slayden, Richard A., Singleton, Eric, Russo, Riccardo, Connell, Nancy, Ojima, Iwao |
| Zdroj: |
MedChemComm; 2021, Vol. 12 Issue: 1 p78-94, 17p |
| Abstrakt: |
Filamenting temperature sensitive protein Z (FtsZ) is an essential bacterial cell division protein and a promising target for the development of new antibacterial therapeutics. As a part of our ongoing SAR studies on 2,5,6-trisubstituted benzimidazoles as antitubercular agents targeting Mtb-FtsZ, a new library of compounds with modifications at the 2 position was designed, synthesized and evaluated for their activity against Mtb-H37Rv. This new library of trisubstituted benzimidazoles exhibited MIC values in the range of 0.004–50 μg mL−1. Compounds 6b, 6c, 20fand 20gshowed excellent growth inhibitory activities ranging from 0.004–0.08 μg mL−1. This SAR study has led to the discovery of a remarkably potent compound 20g(MIC 0.0039 μg mL−1; normalized MIC 0.015 μg mL−1). Our 3DQSAR model predicted 20gas the most potent compound in the library. |
| Databáze: |
Supplemental Index |
| Externí odkaz: |
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