Molecules, Vol. 25, Pages 138: Substituted N-(Pyrazin-2-yl)benzenesulfonamides; Synthesis, Anti-Infective Evaluation, Cytotoxicity, and In Silico Studies
Molecules, Vol. 25, Pages 138: Substituted N-(Pyrazin-2-yl)benzenesulfonamides; Synthesis, Anti-Infective Evaluation, Cytotoxicity, and In Silico Studies
Molecules doi: 10.3390/molecules25010138
Authors:
Ghada Bouz
Martin Juhás
Lluis Pausas Otero
Cristina Paredes de la Red
Ondřej Janďourek
Klára Konečná
Pavla Paterová
Vladimír Kubíček
Jiří Janoušek
Martin Doležal
Jan Zitko
We prepared a series of substituted N-(pyrazin-2-yl)benzenesulfonamides as an attempt to investigate the effect of different linkers connecting pyrazine to benzene cores on antimicrobial activity when compared to our previous compounds of amide or retro-amide linker type. Only two compounds, 4-amino-N-(pyrazin-2-yl)benzenesulfonamide (MIC = 6.25 μg/mL, 25 μM) and 4-amino-N-(6-chloropyrazin-2-yl)benzenesulfonamide (MIC = 6.25 μg/mL, 22 μM) exerted good antitubercular activity against M. tuberculosis H37Rv. However, they were excluded from the comparison as they—unlike the other compounds—possessed the pharmacophore for the inhibition of folate pathway, which was proven by docking studies. We performed target fishing, where we identified matrix metalloproteinase-8 as a promising target for our title compounds that is worth future exploration.
Source: Molecules - Category: Chemistry Authors: Ghada Bouz Martin Juh ás Lluis Pausas Otero Cristina Paredes de la Red Ond řej Janďourek Kl ára Konečná Pavla Paterov á Vladim ír Kubíček Ji ří Janoušek Martin Dole žal Jan Zitko Tags: Article Source Type: research