Synthesis, in silico Study and Antimicrobial Evaluation of New Diesters Derived from Phthaloylglycine

• Autor(a) principal: Oliveira,Rafael F. de
• Data de Publicação: 2020
• Outros Autores: Souza,Helivaldo D. S., Alves,Francinara S., Sousa,Abraão P. de, Lima,Priscila S. V. de, Huang,Min-Fu N., Cordeiro,Laísa V., Diniz Neto,Hermes, Lima,Edeltrudes O., Trindade,Emmely O., Barbosa-Filho,José M., Athayde-Filho,Petrônio F. de
• Tipo de documento: Artigo
• Idioma: eng
• Título da fonte: Journal of the Brazilian Chemical Society (Online)
• Texto Completo: http://old.scielo.br/scielo.php?script=sci_arttext&pid=S0103-50532020000500953
• topic: phthalimide; phthaloylglycine; antibacterial activity; antifungal activity

New diesters derived from phthaloylglycine (7a-7i) were synthesized and their structures characterized by infrared, 1H and 13C nuclear magnetic resonance (NMR) spectroscopy. The compounds were evaluated in an in silico study, which demonstrated positive features indicating a possible drug candidate. The diesters showed antifungal activity ranging from moderate to strong against strains of Candida. Compounds 7a, 7b, 7c, 7e and 7i had a moderate minimum inhibitory concentration (MIC) of 1024 µg mL−1 against all fungal strains, while 7h showed a very good MIC of 256 µg mL−1 against Candida albicans, Candida parapsilosis and Candida krusei and 64 µg mL−1 against Candida tropicalis. However, only 7h and 7i were able to inhibit bacterial growth of strains of Staphylococcus aureus, Staphylococcus epidermidis, Pseudomonas aeruginosa and Escherichia coli with an MIC of 1024 µg mL−1.