Phosphonamidates are the first phosphorus-based zinc binding motif to show inhibition of ?-class carbonic anhydrases from bacteria, fungi, and protozoa
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作者:
Alissa, Siham A.
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Princess Nourah Bint Abdulrahman Univ, Coll Sci, Chem Dept, POB 84428, Riyadh 11671, Saudi ArabiaPrincess Nourah Bint Abdulrahman Univ, Coll Sci, Chem Dept, POB 84428, Riyadh 11671, Saudi Arabia
Alissa, Siham A.
[1
]
Alghulikah, Hanan A.
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Princess Nourah Bint Abdulrahman Univ, Coll Sci, Chem Dept, POB 84428, Riyadh 11671, Saudi ArabiaPrincess Nourah Bint Abdulrahman Univ, Coll Sci, Chem Dept, POB 84428, Riyadh 11671, Saudi Arabia
Alghulikah, Hanan A.
[1
]
Alothman, Zeid A.
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King Saud Univ, Coll Sci, Chem Dept, Riyadh, Saudi ArabiaPrincess Nourah Bint Abdulrahman Univ, Coll Sci, Chem Dept, POB 84428, Riyadh 11671, Saudi Arabia
Alothman, Zeid A.
[2
]
Osman, Sameh M.
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King Saud Univ, Coll Sci, Chem Dept, Riyadh, Saudi ArabiaPrincess Nourah Bint Abdulrahman Univ, Coll Sci, Chem Dept, POB 84428, Riyadh 11671, Saudi Arabia
Osman, Sameh M.
[2
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Del Prete, Sonia
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CNR, Ist Biosci & Biorisorse, Naples, ItalyPrincess Nourah Bint Abdulrahman Univ, Coll Sci, Chem Dept, POB 84428, Riyadh 11671, Saudi Arabia
Del Prete, Sonia
[3
]
Capasso, Clemente
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CNR, Ist Biosci & Biorisorse, Naples, ItalyPrincess Nourah Bint Abdulrahman Univ, Coll Sci, Chem Dept, POB 84428, Riyadh 11671, Saudi Arabia
A primary strategy to combat antimicrobial resistance is the identification of novel therapeutic targets and anti-infectives with alternative mechanisms of action. The inhibition of the metalloenzymes carbonic anhydrases (CAs, EC 4.2.1.1) from pathogens (bacteria, fungi, and protozoa) was shown to produce an impairment of the microorganism growth and virulence. As phosphonamidates have been recently validated as human ?-CA inhibitors (CAIs) and no phosphorus-based zinc-binding group have been assessed to date against ?-class CAs, herein we report an inhibition study with this class of compounds against ?-CAs from pathogenic bacteria, fungi, and protozoa. Our data suggest that phosphonamidates are among the CAIs with the best selectivity for ?-class over human isozymes, making them interesting leads for the development of new anti-infectives.
机构:
Univ Fed Rio de Janeiro, Inst Microbiol Paulo de Goes, BIOINOVAR Biotechnol Labs Biocatalysis Bioprod &, Rio De Janeiro, BrazilUniv Florence, Pharmaceut & Nutraceut Sect, Dept NEUROFARBA, Via U Schiff 6, I-50019 Florence, Italy
Vermelho, Alane Beatriz
;
Cardoso, Veronica da Silva
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Fiocruz MS, Inst Oswaldo Cruz, Lab Cellular Ultrastruct, Ave Brasil 4365 Manguinhos, BR-21040900 Rio De Janeiro, RJ, BrazilUniv Florence, Pharmaceut & Nutraceut Sect, Dept NEUROFARBA, Via U Schiff 6, I-50019 Florence, Italy
Cardoso, Veronica da Silva
;
de Souza Pereira, Mirian Claudia
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Fiocruz MS, Inst Oswaldo Cruz, Lab Cellular Ultrastruct, Ave Brasil 4365 Manguinhos, BR-21040900 Rio De Janeiro, RJ, BrazilUniv Florence, Pharmaceut & Nutraceut Sect, Dept NEUROFARBA, Via U Schiff 6, I-50019 Florence, Italy
机构:
Univ Fed Rio de Janeiro, Inst Microbiol Paulo de Goes, BIOINOVAR Biotechnol Labs Biocatalysis Bioprod &, Rio De Janeiro, BrazilUniv Florence, Pharmaceut & Nutraceut Sect, Dept NEUROFARBA, Via U Schiff 6, I-50019 Florence, Italy
Vermelho, Alane Beatriz
;
Cardoso, Veronica da Silva
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h-index: 0
机构:
Fiocruz MS, Inst Oswaldo Cruz, Lab Cellular Ultrastruct, Ave Brasil 4365 Manguinhos, BR-21040900 Rio De Janeiro, RJ, BrazilUniv Florence, Pharmaceut & Nutraceut Sect, Dept NEUROFARBA, Via U Schiff 6, I-50019 Florence, Italy
Cardoso, Veronica da Silva
;
de Souza Pereira, Mirian Claudia
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h-index: 0
机构:
Fiocruz MS, Inst Oswaldo Cruz, Lab Cellular Ultrastruct, Ave Brasil 4365 Manguinhos, BR-21040900 Rio De Janeiro, RJ, BrazilUniv Florence, Pharmaceut & Nutraceut Sect, Dept NEUROFARBA, Via U Schiff 6, I-50019 Florence, Italy