Synthesis and in vitro evaluation of new benzothiazole derivatives as schistosomicidal agents. 2007

Mona A Mahran, and Samia William, and Fatem Ramzy, and Amira M Sembel
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, University of Alexandria, Alexandria, Egypt. monamahran@yahoo.com

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 microg/mL). Three of these products, 4a-c, showed schistosomicidal activity similar to praziquantel, with 100% worm mortality at 10 microg/mL. These compounds would constitute a new class of potent schistosomicidal agents.

UI MeSH Term Description Entries
D011223 Praziquantel An anthelmintic used in most schistosome and many cestode infestations. Biltricide,Cesol,Cisticid,Cysticide,Droncit,Drontsit,EMBAY 8440,Prasiquantel,Praziquantel, (+-)-Isomer,Praziquantel, (R)-Isomer,Praziquantel, (S)-Isomer,Pyquiton,Traziquantel
D000818 Animals Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA. Animal,Metazoa,Animalia
D000981 Antiprotozoal Agents Substances that are destructive to protozoans. Schizonticides,Agents, Antiprotozoal
D012550 Schistosoma mansoni A species of trematode blood flukes of the family Schistosomatidae. It is common in the Nile delta. The intermediate host is the planorbid snail. This parasite causes schistosomiasis mansoni and intestinal bilharziasis. Schistosoma mansonus,mansonus, Schistosoma
D052160 Benzothiazoles Compounds with a benzene ring fused to a thiazole ring.
D023382 Toxicity Tests, Acute Experiments designed to determine the potential toxic effects of one-time, short-term exposure to a chemical or chemicals. Acute Toxicity Tests,Acute Toxicity Test,Test, Acute Toxicity,Tests, Acute Toxicity,Toxicity Test, Acute

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