Novel 2-indolinones containing a sulfonamide moiety as selective inhibitors of candida beta-carbonic anhydrase enzyme
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY, cilt.34, sa.1, ss.528-531, 2019 (SCI-Expanded, Scopus)
- Yayın Türü: Makale / Tam Makale
- Cilt numarası: 34 Sayı: 1
- Basım Tarihi: 2019
- Doi Numarası: 10.1080/14756366.2018.1564045
- Dergi Adı: JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
- Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus
- Sayfa Sayıları: ss.528-531
- Anahtar Kelimeler: Sulfonamides, Candida glabrata, carbonic anhydrase, docking, VIBRIO-CHOLERAE, BACTERIAL, ISATIN, ALPHA, RESISTANCE, GLABRATA, ALBICANS, BINDING, POTENT, LIGHT
- İstanbul Üniversitesi Adresli: Evet
Özet
Inhibition of the beta-carbonic anhydrase (CA, EC 4.2.1.1) from pathogenic Candida glabrata (CgNce103) by 1H-indole-2,3-dione 3-[N-(4-sulfamoylphenyl)thiosemicarbazones] 4a-m was investigated. All the compounds were found to be potent inhibitors of CgNce103, with inhibition constants in the range of 6.4-63.9 nM. The 5,7-dichloro substituted derivative 4l showed the most effective inhibition (K-I of 6.4 nM) as well as the highest selectivity for inhibiting CgNce103 over the cytosolic human (h) isoforms hCA I and II. A possible binding interaction of compound 4l within the active site of CgNce103 has been proposed based on docking studies.