Molecules | |
Synthesis and in vitro Evaluation of New Benzothiazole Derivatives as Schistosomicidal Agents | |
Mona A Mahran1  Samia William1  Fatem Ramzy1  | |
[1] 1Department of Pharmaceutical Chemistry, Faculty of Pharmacy, University of Alexandria, Alexandria, Egypt 2Theodor Bilharz Research Institute, Ministry of Scientific Research, Warak El Hadar, Embaba, Cairo, Egypt 3Department of Pharmacology, Faculty of Pharmacy, University of Alexandria, Alexandria, Egypt | |
关键词: Benzothiazole; dithiocarbamate; thiadiazole; thiosemicarbazones; schistosomicidal agents.; | |
DOI : 10.3390/12030622 | |
来源: mdpi | |
【 摘 要 】
A series of benzothiazol-2-yl-dithiocarbamates 3a-d along with their copper complexes 4a-c were synthesized via the reaction of suitable alkyl, aralkyl or heteroaryl halides with the sodium salt of benzothiazol-2-yl-dithiocarbamic acid, followed by complexation with copper sulphate. N-(4-Acetyl-5-aryl-4,5-dihydro-1,3,4-thiadiazol-2-yl)-N-benzothiazol-2-yl-acetamides 7a-c were synthesized by cyclization of the appropriate thiosemicarbazones 6a-c in acetic anhydride. Selected compounds were screened for in vitro schistosomicidal activity against Schistosoma mansoni at three different dosage levels (10, 50 and 100 μg/ mL). Three of these products, 4a-c, showed schistosomicidal activity similar to praziquantel, with 100% worm mortality at 10 μg/mL. These compounds would constitute a new class of potent schistosomicidal agents.
【 授权许可】
CC BY
This is an open access article distributed under the Creative Commons Attribution License (CC BY) which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.
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