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

• Main Authors: Mona A Mahran, Samia William, Fatem Ramzy, Amira M Sembel
• Format: Article
• Language: English
• Published: MDPI AG 2007-03-01
• Series: Molecules
• Subjects: Benzothiazole; dithiocarbamate; thiadiazole; thiosemicarbazones; schistosomicidal agents.
• Online Access: http://www.mdpi.com/1420-3049/12/3/622/

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.