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Isatin analogs as novel inhibitors of Candida spp. β-carbonic anhydrase enzymes
被引:26
作者:
Akdemir, Atilla
[1
]
Guzel-Akdemir, Ozlen
[2
]
Karali, Nilgun
[2
]
Supuran, Claudiu T.
[3
]
机构:
[1] Bezmialem Vakif Univ, Dept Pharmacol, Fac Pharm, Vatan Caddesi, TR-34093 Istanbul, Turkey
[2] Istanbul Univ, Fac Pharm, Dept Pharmaceut Chem, TR-34116 Istanbul, Turkey
[3] Univ Firenze, NEUROFARBA Dept, Sez Sci Farmaceut, Via Ugo Schiff 6, I-5001 Florence, Italy
关键词:
Carbonic anhydrase;
Carbonic anhydrase inhibitors;
Candida;
Isatins;
Sulfonamides;
CRYPTOCOCCUS-NEOFORMANS;
CO2;
IX;
SULFONAMIDES;
GLABRATA;
PATENT;
XII;
VIRULENCE;
D O I:
10.1016/j.bmc.2016.02.036
中图分类号:
Q5 [生物化学];
Q7 [分子生物学];
学科分类号:
071010 ;
081704 ;
摘要:
Enzyme inhibition data of structurally novel isatin-containing sulfonamides were determined for two carbonic anhydrases (CAs, EC 4.2.1.1) from pathogenic Candida species (CaNce103 from C. albicans and CgNce103 from C. glabrata). The compounds show K-I values in the low nanomolar range for the fungal CAs, while they have significantly higher K-I values for the human CAs. Homology models were constructed for the CaNce103 and CgNce103 and subsequently the ligands were docked into these models to rationalize their enzyme inhibitory properties. (C) 2016 Elsevier Ltd. All rights reserved.
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页码:1648 / 1652
页数:5
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