Kumar Kewal, Pradines Bruno, Madamet Marilyn, Amalvict Rémy, Benoit Nicolas, Kumar Vipan
Department of Chemistry, Guru Nanak Dev University, Amritsar 143005, India.
Unité de Parasitologie et d'Entomologie, Département des Maladies Infectieuses, Institut de Recherche Biomédicale des Armées, Brétigny sur Orge, France; Aix Marseille Université, Unité de Recherche sur les Maladies Infectieuses et Tropicales Emergentes, UM 63, CNRS 7278, IRD 198, Inserm 1095, Marseille, France; Centre National de Référence du Paludisme, Marseille, France.
Eur J Med Chem. 2014 Nov 24;87:801-4. doi: 10.1016/j.ejmech.2014.10.024. Epub 2014 Oct 13.
1H-1,2,3-triazole tethered isatin-ferrocene conjugates were synthesized and evaluated for their antiplasmodial activities against chloroquine-susceptible (3D7) and chloroquine-resistant (W2) strains of Plasmodium falciparum. The conjugates 5f and 5h with an optimum combination of electron-withdrawing halogen substituent at C-5 position of isatin ring and a propyl chain, introduced as linker, proved to be most potent and non-cytotoxic among the series with IC50 values of 3.76 and 4.58 μM against 3D7 and W2 strains, respectively.
合成了1H-1,2,3-三唑连接的异吲哚酮-二茂铁共轭物，并评估了它们对恶性疟原虫氯喹敏感株（3D7）和氯喹耐药株（W2）的抗疟活性。异吲哚酮环C-5位具有吸电子卤素取代基和作为连接基引入的丙基链的共轭物5f和5h，在该系列中被证明是最有效的且无细胞毒性，对3D7和W2菌株的IC50值分别为3.76和4.58 μM。
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