Synthesis and evaluation of naphthyridine compounds as antimalarial agents

Zhu, Shujia; Zhang, Quan; Chandrashekar, G.; Li, Meng; Wei, Lai; Smith, Erika L.; Kong, Yuliang

doi:10.1016/j.bmcl.2007.09.044

Cited by 23 publications

(17 citation statements)

References 22 publications

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“…8-Aminoquinolines with modified aromatic ring (Fig. 11) Zhu et al synthesized a series of naphthyridine analogues of PQ [102]. The [1,5]naphthyridine ring has higher oxidation potential due to the presence of a second nitrogen atom in the aromatic system, which may prevent hydroxylation at the C-5 position, responsible for chemically reactive and potentially toxic metabolites.…”

Section: Moreira Et Al Further Described Antimalarial Activities Of mentioning

confidence: 98%

Quinolines and structurally related heterocycles as antimalarials

Kaur

Jain

Reddy

et al. 2010

European Journal of Medicinal Chemistry

662

300

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Section: Moreira Et Al Further Described Antimalarial Activities Of mentioning

confidence: 98%

Quinolines and structurally related heterocycles as antimalarials

Kaur

Jain

Reddy

et al. 2010

European Journal of Medicinal Chemistry

662

300

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“…PQ derivatives 31 were designed and synthesized by Zhu and coworkers, who found these compounds to have lower toxicity than PQ, due to a reduced tendency to produce chemically reactive toxic metabolites and metabolic intermediates [198]. Some of the compounds possessed therapeutic indices over 10 times superior to that of CQ [198].…”

Section: Modifications At the Terminal Primary Aminementioning

confidence: 99%

Primaquine revisited six decades after its discovery

Vale¹,

Moreira²,

Gomes³

2009

European Journal of Medicinal Chemistry

322

308

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“…A start point to tackle these issues is the molecular manipulation of known drugs or active classes of compound to generate new scaffolds with improved potency, safety or straightforward synthesis. Currently, analogues of existing antiparasitic drugs are under investigation for a variety of neglected diseases [28][29][30][31][32][33][34][35][36][37].…”

Section: Strategies For Drug Discovery For Tropical Diseasesmentioning

confidence: 99%

Structure-Based Drug Discovery for Tropical Diseases

Güido

Oliva

2009

CTMC

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Parasitic diseases are amongst the foremost threats to human health and welfare around the world. In tropical and subtropical regions of the world, the consequences of parasitic infections are devastating both in terms of human morbidity and mortality. The current available drugs are limited, ineffective, and require long treatment regimens. To overcome these limitations, the identification of new macromolecular targets and small-molecule modulators is of utmost importance. The advances in genomics and proteomics have prompted drug discovery to move toward more rational strategies. The increasing understanding of the fundamental principles of protein-ligand interactions combined with the availability of compound libraries has facilitated the identification of promising hits and the generation of high quality lead compounds for tropical diseases. This review presents the current progresses and applications of structure-based drug design (SBDD) for the discovery of innovative chemotherapy agents for a variety of parasitic diseases, highlighting the challenges, limitations, and future perspectives in medicinal chemistry.

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Synthesis and evaluation of naphthyridine compounds as antimalarial agents

Cited by 23 publications

References 22 publications

Quinolines and structurally related heterocycles as antimalarials

Quinolines and structurally related heterocycles as antimalarials

Primaquine revisited six decades after its discovery

Structure-Based Drug Discovery for Tropical Diseases

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