Abstract:
:A series of 1,2,3-thiadiazole and 1,2,3-selenadiazole derivatives were synthesized by the cyclization of novel 2-(quinolin-8-yloxy) acetohydrazones. In vitro antiamoebic activity was performed against HM1: IMSS strain of Entamoeba histolytica. The results showed that all the 2-(quinolin-8-yloxy) acetohydrazones were more active than their cyclized products (1,2,3-thiadiazole and 1,2,3-selenadiazole derivatives). SAR showed that the compounds having quinoline ring and hydrazone linkage with free N-H group are responsible for higher antiamoebic activity. The cytotoxic studies of these compounds on human breast cancer MCF-7 cell line showed that all the compounds were nontoxic at the concentration range of 1.56-50 μM.
journal_name
Eur J Med Chemjournal_title
European journal of medicinal chemistryauthors
Hayat F,Salahuddin A,Zargan J,Azam Adoi
10.1016/j.ejmech.2010.09.066subject
Has Abstractpub_date
2010-12-01 00:00:00pages
6127-34issue
12eissn
0223-5234issn
1768-3254pii
S0223-5234(10)00735-Xjournal_volume
45pub_type
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