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

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.

Synthesis of some thiazolyl aminobenzothiazole derivatives as potential antibacterial, antifungal and anthelmintic agents

“…The compounds 6-substituted-1,3-benzothiazol-2-amines 1-4 were synthesised with an excellent yield following the methodology as described by Jimonet et al [25] from aryl amines. The compounds 1-4 on reaction with chloracetyl chloride afforded 2-chloro-N-(6-substituted-1,3-benzothiazol-2-yl)acetamide 5-8 on refluxing the reaction mixture at 120°C for 5h [26]. The MIC (μg/mL) of tested compounds are shown in Table 1.…”

Synthesis and Characterization of Novel N-(Benzo[d]Thiazol-2-yl)-2-(2-(6-Chloroquinolin-4-yl)Hydrazinyl)Acetamide Derivatives Containing Quinoline Linkage as Potent Antibacterial Agents

“…Benzothiazole are an important class of bioactive and industrially important organic compounds. From the recent literature, these derivatives are also known to possess anti-tubercular, [3] local anesthetic, [4] antidiabetic, [5] antiulcer, [6] antipsychotic, [7] anti-tumor, [8] anti-oxidant, [9] analgesic, [10] schistosomicidal, [11] antileishmanial, [12] anti-convulsant, [13] anti-parasitic, [14] diuretic, [15] plant growth regulator [16] activities, anthelmintic, [17] Acaricidal. [18] Quinoline or 1-aza-naphthalene is one of the most important N-based heterocyclic aromatic compounds.…”

Insilico Design, Synthesis and Characterization of Some Novel Benzothiazole Derivatives as Anti-Cancer Agents

“…They are widely found in bio-organic and medicinal chemistry with application in drug discovery [1]. Benzothiazole moieties are part of compounds showing numerous biological activities such as antifungal [2], antiepileptic [3] anticancer [4], anti-inflammatory (COX-inhibitors) [5], antidiabetic [6], anticonvulsant [7], antimicrobial [8] , diuretic [9], antitubercular [10], schictosomicidal [11], and anthelmintic [12] activities. Benzothiazole is used in research as a starting material for the synthesis of various bioactive structures.…”