Imidazolopiperazines: Hit to Lead Optimization of New Antimalarial Agents
نویسندگان
چکیده
منابع مشابه
Imidazolopiperazines: Lead Optimization of the Second-Generation Antimalarial Agents
On the basis of the initial success of optimization of a novel series of imidazolopiperazines, a second generation of compounds involving changes in the core piperazine ring was synthesized to improve antimalarial properties. These changes were carried out to further improve the potency and metabolic stability of the compounds by leveraging the outcome of a set of in vitro metabolic identificat...
متن کاملCryptolepine and development of new antimalarial agents
Natural product-derived drugs exemplified by quinine, isolated from South American Cinchona species and artemisinin discovered in China are of immense importance for the treatment of malaria. Although malaria parasites resistant to artemisinin have not yet been found in malaria patients, the need for new antimalarial agents remains. The burden of malaria is heaviest in Africa where over a milli...
متن کاملHit To Lead Optimization, And 3D QSAR Modeling of Imidazolopiperazines Derivatives against Malaria Based On PLSR Machine Learning Technique
Malaria is a mosquito-borne lifethreatening disease. Though it is treatable but due to emerging resistance against well-known drugs like 8aminoquinolines and artemisinin analogs, it is urgent need to develop novel drugs for the treatment of malaria. In order to develop a new drug, imidazolopiperazine derivatives have been shown antimalarial efficacy against wild-type as well as drug resistant m...
متن کاملCryptolepine and development of new antimalarial agents
Natural product-derived drugs exemplified by quinine, isolated from South American Cinchona species and artemisinin discovered in China are of immense importance for the treatment of malaria. Although malaria parasites resistant to artemisinin have not yet been found in malaria patients, the need for new antimalarial agents remains. The burden of malaria is heaviest in Africa where over a milli...
متن کاملLead optimization of antimalarial propafenone analogues.
Previously reported studies identified analogues of propafenone that had potent antimalarial activity, reduced cardiac ion channel activity, and properties that suggested the potential for clinical development for malaria. Careful examination of the bioavailability, pharmacokinetics, toxicology, and efficacy of this series of compounds using rodent models revealed orally bioavailable compounds ...
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ژورنال
عنوان ژورنال: Journal of Medicinal Chemistry
سال: 2011
ISSN: 0022-2623,1520-4804
DOI: 10.1021/jm2003359