Design and synthesis of triazolopyrimidine acylsulfonamides as novel anti-mycobacterial leads acting through inhibition of acetohydroxyacid synthase
| Autor: | Kale Manoj Ganpat, Dwarakanath Prahlad, P. Shahul Hameed, B. Bhaskar, Santosh Nandan, Vikas Patil, Anandkumar Raichurkar, Meenakshi Balganesh |
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| Rok vydání: | 2013 |
| Předmět: |
Models
Molecular Antimycobacterial Agents Stereochemistry medicine.drug_class Clinical Biochemistry Pharmaceutical Science Antimycobacterial Biochemistry Anti mycobacterial Drug Discovery medicine Humans Tuberculosis Molecular Biology health care economics and organizations Sulfonyl chemistry.chemical_classification Sulfonamides Chemistry Acetohydroxyacid synthase Organic Chemistry Mycobacterium tuberculosis Combinatorial chemistry Anti-Bacterial Agents Acetolactate Synthase Enzyme Pyrimidines Mechanism of action Drug Design Molecular Medicine medicine.symptom Whole cell |
| Zdroj: | Bioorganicmedicinal chemistry letters. 24(9) |
| ISSN: | 1464-3405 |
| Popis: | Novel triazolopyrimidine acylsulfonamides class of antimycobacterial agents, which are mycobacterial acetohydroxyacid synthase (AHAS) inhibitors were designed by hybridization of known AHAS inhibitors such as sulfonyl urea and triazolopyrimidine sulfonamides. This Letter describes the synthesis and SAR studies of this class of molecules by variation of two parts of the molecule, the phenyl and triazolopyrimidine rings. SAR study describes optimisation of enzyme potency, whole cell potency and evidence of mechanism of action. |
| Databáze: | OpenAIRE |
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