Review of Characteristics and Analytical Methods for Determination of Thiabendazole

Budetić, Mateja; Kopf, Doris; Dandić, Andrea; Samardžić, Mirela

doi:10.3390/molecules28093926

Cited by 4 publications

(1 citation statement)

References 224 publications

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“…Small molecules containing the thiazole moiety have been demonstrated to possess drug-like properties against a variety of diseases, resulting in, so far, 17 FDA-approved drugs containing the thiazole ring. The indications to which thiazole derivatives are prescribed include asthma (Cinalukast) [28], bacterial infections (Ceftizoxime) [29], diarrhea (Nitazoxanide) [30], myelogenous leukemia (Dasatinib) [31], pain (Meloxicam) [32], duodenal ulcers (famotidine) [33], anthelmintics (thiabendazole) [34], CNS neuroprotective and anticonvulsant (riluzole) [35], and vitamin (thiamine) [36].…”

Section: Introductionmentioning

confidence: 99%

Parallel Synthesis of Piperazine Tethered Thiazole Compounds with Antiplasmodial Activity

Rayala,

Chaudhari,

Bunnell

et al. 2023

IJMS

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Thiazole and piperazine are two important heterocyclic rings that play a prominent role in nature and have a broad range of applications in agricultural and medicinal chemistry. Herein, we report the parallel synthesis of a library of diverse piperazine-tethered thiazole compounds. The reaction of piperazine with newly generated 4-chloromethyl-2-amino thiazoles led to the desired piperazine thiazole compounds with high purities and good overall yields. Using a variety of commercially available carboxylic acids, the parallel synthesis of a variety of disubstituted 4-(piperazin-1-ylmethyl)thiazol-2-amine derivatives is described. the screening of the compounds led to the identification of antiplasmodial compounds that exhibited interesting antimalarial activity, primarily against the Plasmodium falciparum chloroquine-resistant Dd2 strain. The hit compound 2291-61 demonstrated an antiplasmodial EC50 of 102 nM in the chloroquine-resistant Dd2 strain and a selectivity of over 140.

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