Assessing different thiazolidine and thiazole based compounds as antileishmanial scaffolds

Schadich, Ermin; Kryshchyshyn‐Dylevych, Anna; Holota, Serhii; Polishchuk, Pavel; Džubák, Petr; Gurská, Soňa; Hajdúch, Marián; Lesyk, Roman

doi:10.1016/j.bmcl.2020.127616

Cited by 24 publications

(13 citation statements)

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“…Schadich et al [198], encouraged by the data from the literature regarding the antitrypanosomal activity of some thiazole-based compounds against Trypanosoma brucei and Trypanosoma gambiense [199], decided to test previously synthesized thiazolidinone and thiazole-based compounds [200,201] for their antileishmanial activity against Leishmania major.…”

Section: Neglected Diseasesmentioning

confidence: 99%

Thiazole Ring—A Biologically Active Scaffold

2021

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Background: Thiazole is a good pharmacophore nucleus due to its various pharmaceutical applications. Its derivatives have a wide range of biological activities such as antioxidant, analgesic, and antimicrobial including antibacterial, antifungal, antimalarial, anticancer, antiallergic, antihypertensive, anti-inflammatory, and antipsychotic. Indeed, the thiazole scaffold is contained in more than 18 FDA-approved drugs as well as in numerous experimental drugs. Objective: To summarize recent literature on the biological activities of thiazole ring-containing compounds Methods: A literature survey regarding the topics from the year 2015 up to now was carried out. Older publications were not included, since they were previously analyzed in available peer reviews. Results: Nearly 124 research articles were found, critically analyzed, and arranged regarding the synthesis and biological activities of thiazoles derivatives in the last 5 years.

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Section: Neglected Diseasesmentioning

confidence: 99%

Thiazole Ring—A Biologically Active Scaffold

2021

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“…In the aforementioned context, the darbufelone-NSAID, a dual inhibitor targeting COX-2 and 5-lipoxygenase (5-LOX), presents interest for study as a possible potential anticonvulsant. Darbufelone belongs to 4-thiazolidinone derivatives, and among this class of heterocycles, the thiazole-4-thiazolidinone hybrid molecules are known as an important source of drug-like molecules with various kinds of biological activities as well as polypharmacological agents [24][25][26][27][28][29]. The thiazole-4-thiazolidinone-bearing hybrids with promising anticonvulsant properties were identified and reported [26,30].…”

Section: Introductionmentioning

confidence: 99%

Evaluation of Anticonvulsant Activity of Dual COX-2/5-LOX Inhibitor Darbufelon and Its Novel Analogues

et al. 2021

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Neuroinflammation is an integral part of epilepsy pathogenesis and other convulsive conditions, and non-steroidal anti-inflammatory drugs (NSAIDs) present a potent tool for the contemporary search and design of novel anticonvulsants. In the present paper, evaluation of the anticonvulsant activity of the potential NSAID dual COX-2/5-LOX inhibitor darbufelone methanesulfonate using an scPTZ model in mice in dose 100 mg/kg is reported. Darbufelone possesses anticonvulsant properties in the scPTZ model and presents interest for in-depth studies as a possible anticonvulsant multi-target agent with anti-inflammatory activity. The series of 4-thiazolidinone derivatives have been synthesized following the analogue-based drug design and hybrid-pharmacophore approach using a darbufelone matrix. The synthesized derivatives showed a significant protection level for animals in the scPTZ model and are promising compounds for the design of potential anticonvulsants with satisfactory drug-like parameters.

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“…The oxidative stress [19][20][21] and redox [22,23] processes play important role under inflammation condition. The ability of neutralization of the impacts of reactive element species (Oxygen, Nitrogen, free radicals) is a desirable feature for modern NSAIDs [24,25]. That is why an of the chemical groups with anti-scavenging/anti-oxidant or redox properties into the molecular structure of potential NSAIDs seems an attractive strategy for design.…”

Section: Introductionmentioning

confidence: 99%