2 documents found, page 1 of 1
Lipophilic pyrazinoic acid amide and ester prodrugs Stability, activation and a...
Simoes, Marta Filipa; Valente, Emilia; Rodriguez Gomez, M. Jose; Anes, Elsa; Constantino, LuisPyrazinamide (PZA) is active against M. tuberculosis and is a first line agent for the treatment of human tuberculosis. PZA is itself a prodrug that requires activation by a pyrazinamidase to form its active metabolite pyrazinoic acid (POA). Since the specificity of cleavage is dependent on a single bacterial enzyme, resistance to PZA is often found in tuberculosis patients. Esters of POA have been proposed in ...
Structure-activity relationships for dipeptide prodrugs of acyclovir
Santos, Cledir R.; Capela, Rita; Pereira, Claudia S. G. P.; Valente, Emilia; Gouveia, Luis; Pannecouque, Christophe; De Clercq, Erik; Moreira, RuiA series of water-soluble dipeptide ester prodrugs of the antiviral acyclovir (ACV) were evaluated for their chemical stability, cytotoxicity, and antiviral activity against several strains of Herpes Simplex-1 and -2, vaccinia, vesicular stomatitis, cytomegalovirus and varicella zoster viruses. ACV dipeptide esters were very active against herpetic viruses, independently of the rate at which they liberate the p...