Design, facile synthesis and anthelmintic activity of new O-substituted 6-methoxybenzothiazole-2-carbamates

Omar, A.-Mohsen M.E.; Aboulwafa, Omaima M.; Issa, Doaa A. E.; El-Shokrofy, May M. S.; Amr, May E.; El-Ashmawy, Ibrahim M.

doi:10.1039/c4md00557k

Cited by 6 publications

(1 citation statement)

References 21 publications

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“…Anticonvulsant 5 , Anti-diabetic 6 , Antimicrobia l7 , Antifungal [8][9] , CNS depressant 10 , Antimalarial 11 , Anthelmintic 12 , Anticancer 13 Antiurease 14 , Hypoglycemic agent 15 , Anti-oxidant 16 , Antihelmenthic 17 , Anti-histaminic 18 , Insecticidal 19, Anti-HIV 20 , Antiprotozoal 21 , Antitubercular 22 .…”

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confidence: 99%

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2021

IJPSR

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Benzthiazole, Chalcones, and their analogs have a wide variety of biological activities like antihelminthic, antifungal, antibacterial, anti-diabetic, anti-tubercular, anti-inflammatory, anticonvulsant, diuretic etc., In the present research work, an effort has been made to synthesize some new series of novel benzothiazole linked chalcones from 3-aminoacetophenone and potassium thiocyanate which were dissolved in glacial acetic acid at room temperature. Liquid bromine in glacial acetic acid was then added drop-wise, and finally, the reaction mass is quenched and basified with ammonia to obtain the desired Benzthiazole linked chalcone. The progress of the reaction is monitored through TLC. The purity of the compounds was identified by TLC and purified by recrystallization and column chromatography. The structures were determined by IR, 1H NMR, and Mass spectral data. The synthesized benthiazole linked chalcone analogues were screened for anti-tubercular activity by the use of MABA (Microplate Alamar Blue assay) analytical method on H37Rv strain of Mycobacterium tuberculosis. Based on the results of anti-tubercular activity, it can be seen that the compounds containing electron-withdrawing groups like chlorine, fluorine, nitrogen showed better activity than that of the other compounds in the series. The mechanism of action of the compounds can assassinate for their cell wall disruption by inhibiting the peptidoglycan synthesis as a potential antimicrobial agent or inhibiting the synthesis of mycolic acid as a potential anti-tubercular agent.INTRODUCTION: Synthesis of hybrid drug technology paved the way for the development of innovative medicines, which are a sign of relief from several complex abnormalities / diseases, which include tuberculosis, cancer, and many other microbial infections.

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