Taurultams incorporating arylsulfonamide: First in vitro inhibition studies of alpha-, beta- and gamma-class Carbonic Anhydrases from Vibrio cholerae and Burkholderia pseudomallei
Küçük Resim Yok
Tarih
2021
Dergi Başlığı
Dergi ISSN
Cilt Başlığı
Yayıncı
Elsevier France-Editions Scientifiques Medicales Elsevier
Erişim Hakkı
info:eu-repo/semantics/closedAccess
Özet
A new series of taurultambenzenesulfonamides 1-17 were prepared and considered for their inhibitory activity in vitro against the Carbonic Anhydrases from Vibrio cholerae (VchCA-alpha, VchCA-beta and VchCA-gamma) and Burkholderia pseudomallei (BpsCA-beta and BpsCA-gamma). Among the compounds tested, derivatives 4, 5, 7, 10, 12, and 16 resulted in highly effective VchCA alpha inhibitors (K-I values spanning within the 6.1-9.6 nM range) and endowed with excellent Selectivity Indexes (SIs; K-I VchCA-alpha/K-I hCA II) all comprised between 0.04 and 0.09. Potent in vitro inhibitors for the BpsCA-gamma were also identified (K(I)s of 18.9-19.5 nM). The results here reported may represent the blueprint for the future development of a new generation of CA-based antibiotics integrated with free of resistance mechanisms of action adopted from known drugs. (C) 2021 Elsevier Masson SAS. All rights reserved.
Açıklama
Anahtar Kelimeler
Carbonic anhydrase inhibitors (CAIs), Benzensulfonamide, Taurultam, Taurine, Vibrio cholerae, Burkholderia pseudomallei
Kaynak
European Journal of Medicinal Chemistry
WoS Q Değeri
Q1
Scopus Q Değeri
Cilt
219
