Synthesis and evaluation of anti-Toxoplasma gondii and antimicrobial activities of thiosemicarbazides, 4-thiazolidinones and 1,3,4-thiadiazoles.
In this work we reported the synthesis and evaluation of anti-Toxoplasma gondii and antimicrobial activities in vitro of three new compound series obtained from ethyl(5-methyl-1-H-imidazole-4-carboxylate): acylthiosemicarbazide analogues 3a-d, 4-thiazolidinone analogues 4a-d and 1,3,4-thiadiazole analogues 5a-d. All synthesized compounds were characterized by IR, (1)H, (13)C NMR and HRMS. The majority of the tested compounds show excellent anti-T. gondii activity when compared to hydroxyurea and sulfadiazine. In addition it was also shown that most of the compounds in this study have a better performance against intracellular tachyzoites. The results for antimicrobial activity evaluation showed weak antibacterial and antifungal activities for all the tested molecules, when compared with the standard drugs (chloramphenicol and rifampicin for antibacterial activity; nistatin and ketoconazole for antifungal activity).
Liesen
André P
AP
Departamento de Antibióticos, Universidade Federal de Pernambuco, Recife 50670-901, Brazil.
de Aquino
Thiago M
TM
Carvalho
Cristiane S
CS
Lima
Vânia T
VT
de Araújo
Janete M
JM
de Lima
José G
JG
de Faria
Antônio R
AR
de Melo
Edésio J T
EJ
Alves
Antonio J
AJ
Alves
Elias W
EW
Alves
Anselmo Q
AQ
Góes
Alexandre J S
AJ
D000818:Animals; D000890:Anti-Infective Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D000981:Antiprotozoal Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D001419:Bacteria / Q000187:drug effects; D002522:Chlorocebus aethiops; D004351:Drug Resistance; D005658:Fungi / Q000187:drug effects; D042541:Intracellular Space / Q000187:drug effects / Q000469:parasitology; D008826:Microbial Sensitivity Tests; D012663:Semicarbazides / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D053778:Thiazolidines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D014122:Toxoplasma / Q000187:drug effects* / Q000502:physiology; D014709:Vero Cells
D000890:Anti-Infective Agents; D000981:Antiprotozoal Agents; D012663:Semicarbazides; D053778:Thiazolidines; C005151:thiosemicarbazide