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Synthesis and in vitro Evaluation of New Benzothiazole Derivatives as Schistosomicidal Agents
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, University of Alexandria, Alexandria, Egypt
Theodor Bilharz Research Institute, Ministry of Scientific Research, Warak El Hadar, Embaba, Cairo, Egypt
Department of Pharmacology, Faculty of Pharmacy, University of Alexandria, Alexandria, Egypt
* Author to whom correspondence should be addressed.
Received: 9 November 2006; in revised form: 21 March 2007 / Accepted: 23 March 2007 / Published: 26 March 2007
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.
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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.
Mahran MA, William S, Ramzy F, Sembel AM. Synthesis and in vitro Evaluation of New Benzothiazole Derivatives as Schistosomicidal Agents. Molecules. 2007; 12(3):622-633.
Mahran, Mona A.; William, Samia; Ramzy, Fatem; Sembel, Amira M. 2007. "Synthesis and in vitro Evaluation of New Benzothiazole Derivatives as Schistosomicidal Agents." Molecules 12, no. 3: 622-633.