Synthesis and antitrichinellosis activity of some 2-substituted-[1,3]thiazolo[3,2-a]benzimidazol-3(2H)-ones.
Some new thiazolo[3,2-a]benzimidazolone derivatives were synthesized using two methods. The structures of the synthesized compounds were proved by means of IR, (1)H NMR and mass spectral data. Ab initio computations were performed in order to determine the electronic structure and geometry of the investigated molecules and to compare it to the geometry of albendazole. Biologically, experiments in vitro and in vivo were accomplished in order to identify the efficacy of the obtained thiazolobenzimidazolones against Trichinella spiralis. The effectiveness of compounds 4a-c in the intestinal phase of trichinellosis was 100% and in the muscle phase were 88% and 80% at a concentration of 100mg/kg mw for the compounds 4a and 4c. The results of the hepatotoxicity test showed that the compounds 4a and 4b possess hepatotoxicity comparable to that of albendazole.
Mavrova
Anelia Ts
ATs
University of Chemical Technology and Metallurgy, 8 Kliment Ohridski Boulevard, 1756 Sofia, Bulgaria. anmav@abv.bg
Anichina
Kamelya K
KK
Vuchev
Dimitar I
DI
Tsenov
Jordan A
JA
Kondeva
Magdalena S
MS
Micheva
Mitka K
MK
D000818:Animals; D001562:Benzimidazoles / Q000138:chemical synthesis* / Q000494:pharmacology*; D002470:Cell Survival / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D022781:Hepatocytes / Q000187:drug effects; D015394:Molecular Structure; D021261:Parasitic Sensitivity Tests; D051381:Rats; D013844:Thiazoles / Q000138:chemical synthesis* / Q000494:pharmacology*; D017160:Trichinella spiralis / Q000187:drug effects; D014235:Trichinellosis / Q000188:drug therapy* / Q000378:metabolism / Q000517:prevention & control*
D001562:Benzimidazoles; D013844:Thiazoles