Taurultams incorporating arylsulfonamide: First in vitro inhibition studies of ?-, ?- and ?-class Carbonic Anhydrases from Vibrio cholerae and Burkholderia pseudomallei
Küçük Resim Yok
Tarih
2021
Dergi Başlığı
Dergi ISSN
Cilt Başlığı
Yayıncı
Elsevier Masson s.r.l.
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-?, VchCA-? and VchCA-?) and Burkholderia pseudomallei (BpsCA-? and BpsCA-?). Among the compounds tested, derivatives 4, 5, 7, 10, 12, and 16 resulted in highly effective VchCA? inhibitors (KI values spanning within the 6.1–9.6 nM range) and endowed with excellent Selectivity Indexes (SIs; KI VchCA-?/KI hCA II) all comprised between 0.04 and 0.09. Potent in vitro inhibitors for the BpsCA-? were also identified (KIs 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. © 2021 Elsevier Masson SAS
Açıklama
Anahtar Kelimeler
Benzensulfonamide, Burkholderia pseudomallei, Carbonic anhydrase inhibitors (CAIs), Taurine, Taurultam, Vibrio cholerae
Kaynak
European Journal of Medicinal Chemistry
WoS Q Değeri
Scopus Q Değeri
Q1
Cilt
219
