"LIPOPHILIC AND STRUCTURE ACTIVITY RELATIONSHIPS STUDY OF THIOSEMICARBAZONES AND DERIVATIVES;"

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AuteurGLINMA, BIENVENU
AuteurFAGLA MEDEGAN GOUSSANOU, SEDAMI R
AuteurYAYI LADEKAN, ELEONORE
AuteurAGNIMONHAN, FINAGNON HYACINTHE
AuteurKPOVIESSI DOSSOU, SIKA SALOME
AuteurQUETIN LECLERCQ, JOELLE
AuteurACCROMBESSI, COFFI GEORGES
AuteurKOTCHONI, O SIMEON
AuteurPOUPAERT, HENRI JACQUES
AuteurGBAGUIDI, AHOKANNOU FERNAND
Date d'ajout2026-06-02T16:06:57Z
Date de disponibilite2026-06-02T16:06:57Z
Date de publication2019
ResumeTraditionally, small molecules have been a reliable source for discovering novel biologically active compounds because these molecules are easily synthesized and their smooth structural optimization would usually lead to a feasible candidate compound. Here, some thiosemicarbazones, N(4)-methyl and N(4)-phenyl-3- thiosemicarbazones were synthesized in good yield (52-84%), characterized and then their anti-parasitic activity were evaluated. The structure and lipophilic-activity relationships of compounds were particularly studied. Among them, some products exhibited trypanocidal activity with their half inhibitory concentration (IC50 ≤ 10 micromolar “μM”) especially compounds L1-3, D2, B3, C3, D1 (from 2 to 8.73 μM). Other showed moderate antitrypanosomal activity with their IC50 between 12 to 87 μM (L4, C2, C1, B2) while certain showed little activity (IC50 ≥ 100μM). Some active products turned out quick selective on the parasite with their selectivity index greater than to unit (SI ≥ 1). Several factors including lipophilicity, steric and electronic effects of the substituents have played a vital role in this activity. The elongation of the carbon chain of the carbonyl, the substitution on a phenyl radical, the fixing of a methyl or phenyl on the N(4) nitrogen atom induced significantly the increased trypanocidal activity of compounds. This is the case specifically of N(4)-methyl and especially of N(4)-phenylsubstituted thiosemicarbazones. Such compounds could be able to have applications in the treatment of parasitic diseases.
DOI10.21474/IJAR01/9971
Autre identifiantBECDB-11476
URIhttps://dspace.uac.bj/handle/123456789/10090
Languefr
Fait partie deInternational Journal of Advanced Research
SujetSynthesize
Sujetthiosemicarbazones
Sujettrypanocidal
Sujetlipophilicity
Sujetselectivity
Titre"LIPOPHILIC AND STRUCTURE ACTIVITY RELATIONSHIPS STUDY OF THIOSEMICARBAZONES AND DERIVATIVES;"
TypeArticle

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