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Molecules 2007, 12(3), 622-633; doi:10.3390/12030622

Synthesis and in vitro Evaluation of New Benzothiazole Derivatives as Schistosomicidal Agents

1
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, University of Alexandria, Alexandria, Egypt
2
Theodor Bilharz Research Institute, Ministry of Scientific Research, Warak El Hadar, Embaba, Cairo, Egypt
3
Department of Pharmacology, Faculty of Pharmacy, University of Alexandria, Alexandria, Egypt
*
Author to whom correspondence should be addressed.
Received: 9 November 2006 / Revised: 21 March 2007 / Accepted: 23 March 2007 / Published: 26 March 2007
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Abstract

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.
Keywords: Benzothiazole; dithiocarbamate; thiadiazole; thiosemicarbazones; schistosomicidal agents. Benzothiazole; dithiocarbamate; thiadiazole; thiosemicarbazones; schistosomicidal agents.
This is an open access article distributed under the Creative Commons Attribution License (CC BY 3.0).

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MDPI and ACS Style

Mahran, M.A.; William, S.; Ramzy, F.; Sembel, A.M. Synthesis and in vitro Evaluation of New Benzothiazole Derivatives as Schistosomicidal Agents. Molecules 2007, 12, 622-633.

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