Synthesis and evaluation of the antiplasmodial activity of novel indeno[2,1-c]quinoline derivatives |
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| Institution: | 1. Dipartimento di Scienze Farmaceutiche, Università degli Studi di Milano, Via Mangiagalli 25, 20133 Milano, Italy;2. Dipartimento di Scienze Farmacologiche e Biomolecolari, Università degli Studi di Milano, Via C. Pascal 36, 20133 Milano, Italy;3. Dipartimento di Scienze Biomediche Chirurgiche e Odontoiatriche, Università degli Studi di Milano, Via C. Pascal 36, 20133 Milano, Italy;1. Division of Infectious Diseases, Department of Medicine, Johns Hopkins University School of Medicine, 725 North Wolfe Street, Room 226, Baltimore, MD 21205, USA;2. Department of Specialty Services, Southwest CARE Center, 649 Harkle Road, Suite E, Sante Fe, NM 87505, USA;1. Ural Federal University, 620002 Ekaterinburg, Russian Federation;2. I. Ya. Postovsky Institute of Organic Synthesis, Ural Branch of the Russian Academy of Sciences, 620990 Ekaterinburg, Russian Federation;1. Departamento de Química, Centro de Investigación y de Estudios Avanzados del Instituto Politécnico Nacional, Apartado 14-740, Mexico City, 07000, Mexico;2. Programa de Posgrado en Farmacología, Centro de Investigación y de Estudios Avanzados del Instituto Politécnico Nacional, Apartado 14-740, Mexico City, 07000, Mexico;3. Área Académica de Química, Universidad Autónoma del Estado de Hidalgo, Mineral de la Reforma, Hidalgo, 42184, Mexico;1. Key Laboratory of Pesticide & Chemical Biology of Ministry of Education, Central China Normal University, Wuhan 430079, PR China;2. Institute of Medicinal Chemistry, Hubei University of Medicine, Shiyan 442000, PR China;1. Laboratory of Structure-Function Biochemistry, Department of Chemistry, Faculty and Graduate School of Sciences, Risk Science Research Center, Kyushu University, Fukuoka 812-8581, Japan;2. Laboratorio di Farmacologia, Istituto Superiore di Sanità, Viale Regina Elena 299, Roma, Italy |
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| Abstract: | With the aim to explore the potentiality of new chemical scaffolds for the design of new antimalarials, a set of new indeno2,1-c]quinolines bearing different basic heads has been synthesized and tested in vitro against chloroquine sensitive (CQ-S) and chloroquine resistant (CQ-R) strains of Plasmodium falciparum. Most of the synthesized compounds exhibited a moderate antiplasmodial activity, inhibiting the growth of both CQ-S and CQ-R strains of P. falciparum with IC50 ranging from 0.24 to 6.9 μM and with a very low resistance index. The most potent compounds (1.2–1.3-fold the CQ on the W-2 strain) can be considered as promising ‘lead compounds’ to be further optimized to improve efficacy and selectivity against Plasmodia. |
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| Keywords: | Antimalarial activity Antiplasmodial activity |
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