3 documents found, page 1 of 1
Synthesis, activity, toxicity, and in silico studies of new antimycobacterial N...
Pais, João P.; Antoniuk, Olha; Pires, David; Delgado, Tiago; Fortuna, Andreia; Costa, Paulo J.; Anes, Elsa; Constantino, LuisTuberculosis (TB) is a disease that plagues the frailest members of society. We have developed a family of N-alkyl nitrobenzamides that exhibit promising antitubercular activities and can be considered a structural simplification of known inhibitors of decaprenylphosphoryl-β-D-ribofuranose 2′-oxidase (DprE1), an essential Mycobacterium tuberculosis (Mtb) enzyme and an emergent antitubercular target. Hereby, we ...
Nitrobenzoates and nitrothiobenzoates with activity against M. tuberculosis
Pais, João P.; Antoniuk, Olha; Freire, Raquel; Pires, David; Valente, Emília; Anes, Elsa; Constantino, LuisEsters of weak acids have shown improved antimycobacterial activity over the corresponding free acids and nitro benzoates in particular have previously shown to have a very intriguing activity. To expand the potential of nitro-derivatives of benzoic acid as antimycobacterial drugs and explore the effects of various structural features on the activity of these compounds, we have obtained a library of 64 derivati...
Sugar-based bactericides targeting phosphatidylethanolamine-enriched membranes
Dias, Catarina; Pais, João P.; Nunes, Rafael; Blázquez-Sánchez, Maria-Teresa; Marquês, Joaquim T.; Almeida, Andreia F.; Serra, Patrícia; Xavier, Nuno M.Anthrax is an infectious disease caused by Bacillus anthracis, a bioterrorism agent that develops resistance to clinically used antibiotics. Therefore, alternative mechanisms of action remain a challenge. Herein, we disclose deoxy glycosides responsible for specific carbohydrate-phospholipid interactions, causing phosphatidylethanolamine lamellar-to-inverted hexagonal phase transition and acting over B. anthrac...