Recent Developments in Antimalarial Drug Discovery

Joshi, Anupama; Viswanathan, C. L.

doi:10.2174/187152106774755626

Cited by 41 publications

(24 citation statements)

References 0 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…This is particularly important in light of a recent study that highlights the paucity of new antimalarial compound development around novel classes of compounds (5). Identification of new targets and pathways are a vital aspect of antimalarial discovery in which academia must play a key role (6).…”

mentioning

confidence: 99%

Searching for New Antimalarial Therapeutics amongst Known Drugs

et al. 2006

View full text Add to dashboard Cite

The need to discover and develop new antimalarial therapeutics is severe. The annual mortality attributed to malaria, currently approximately 2.5 million, is increasing due primarily to widespread resistance to currently used drugs. One strategy to identify new treatment alternatives for malaria is to examine libraries of diverse compounds for the possible identification of novel scaffolds. Beginning with libraries of drug or drug-like compounds is an ideal starting point because, in the case of approved drugs, substantial pharmacokinetic and toxicologic data should be available for each compound series. We have employed a high throughput screen of the MicroSource Spectrum and Killer collections, a library of known drugs, bioactive compounds, and natural products. Our screening assay identifies compounds that inhibit growth of Plasmodium falciparum cultured in human erythrocytes. We have identified 36 novel inhibitors of P. falciparum, of which 19 are therapeutics, and five of these drugs exhibit effective 50% inhibitory concentrations within similar ranges to therapeutic serum concentrations for their currently indicated uses: propafenone, thioridazine, chlorprothixene, perhexiline and azlocillin. The findings we report here indicate that this is an effective strategy to identify novel scaffolds and therefore aid in antimalarial drug discovery efforts.

show abstract

mentioning

confidence: 99%

Searching for New Antimalarial Therapeutics amongst Known Drugs

et al. 2006

View full text Add to dashboard Cite

show abstract

“…Quinolines 19.7 (Me), 24.5 (CH 2 ), 24.7 (2CH 2 ), 32.5 (CH 2 ), 32.7 (CH 2 ), 49.0 (CHNH), 57.3 (CH of cyclohexyl), 110. 9,115.2,125.6,126.8,127.5,127.7,128.1,130.1,130.3,131.1,136.7,137.7,143.9,146.5,149.2, (10), 203 (7). Anal.…”

Section: Entrymentioning

confidence: 99%

Synthesis of Novel Tetrazole Containing Quinoline and 2,3,4,9‐Tetrahydro‐1H‐β‐Carboline Derivatives

Ghandi

Rahimi

Zarezadeh

2015

Journal of Heterocyclic Chem

View full text Add to dashboard Cite

show abstract

“…Therefore, it is not surprising that research on the synthesis of polyfunctionalized heterocyclic compounds has received significant attention. Pyrimidoquinolines have been an object of great interest to organic, medicinal and materials scientists over many years, as they are present in a number of biologically active organic compounds which exhibit antimalarial [2,3], anticancer [4], antitumor [5] antimicrobial [6], antiviral [7], analgesic [8], anti-oxidant [8], and anti-inflammatory activities [8,9]. Furthermore, multi-component reactions (MCRs) play an increasingly important role in organic and medicinal chemistry for their convergence, productivity, ease of execution, excellent yield, and broad application in combinational chemistry [10 -18].…”

Section: Introductionmentioning

confidence: 99%