当前位置： SCI文献检索 > BIOORGANIC & MEDICINAL CHEMISTRY期刊下所有文献 > Synthesis and antitrichinellosis activity of some 2-substituted-[1,3]thiazolo[3,2-a]benzimidazol-3(2H)-ones.

Synthesis and antitrichinellosis activity of some 2-substituted-[1,3]thiazolo[3,2-a]benzimidazol-3(2H)-ones.

Abstract：

: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.

journal_name

Bioorg Med Chem

journal_title

Bioorganic & medicinal chemistry

authors

Mavrova ATs,Anichina KK,Vuchev DI,Tsenov JA,Kondeva MS,Micheva MK

doi

10.1016/j.bmc.2005.06.046

subject

Has Abstract

pub_date

2005-10-01 00:00:00

pages

5550-9

issue

19

eissn

0968-0896

issn

1464-3391

pii

S0968-0896(05)00574-2

journal_volume

13

pub_type

杂志文章

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