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

Molecules

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.