Add to ORKG*S Supporting Information ABSTRACT: On the basis of the initial success of optimi-zation of a novel series of imidazolopiperazines, a second genera-tion 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 out-come of a set of in vitro metabolic identification studies. The optimized 8,8-dimethyl imidazolopiperazine analogues exhib-ited improved potency, in vitro metabolic stability profile and, as a result, enhanced oral exposure in vivo in mice. The optimized compounds were found to be more efficacious than the current antimalarials in a malaria mouse model. They ...
Toward improving pharmacokinetics, in vivo efficacy, and selectivity over hERG, structure-activity r...
Novel antimalarial therapeutics that target multiple stages of the parasite lifecycle are urgently r...
Optimization of a chemical series originating from whole-cell phenotypic screening against the human...
On the basis of the initial success of optimization of a novel series of imidazolopiperazines, a sec...
On the basis of our recent results on a novel series of imidazopyridazine-based antimalarials, we fo...
A previous publication from our laboratory reported the identification of a new class of 2-(1H-imida...
Imidazopyridine <b>1</b> was identified from a phenotypic screen against <i>P. falciparum</i> (Pf) b...
On the basis of our recent results on a novel series of imidazopyridazine-based antimalarials, we fo...
A lead-optimization program around a 2,6-imidazopyridine scaffold was initiated based on the two ear...
A novel class of imidazopyridazines identified from whole cell screening of a SoftFocus kinase libra...
Malaria deaths have been decreasing over the last 10–15 years, with global mortality rates having fa...
Most malaria drug development focuses on parasite stages detected in red blood cells, even though, t...
Introduction of water-solubilizing groups on the 5-phenyl ring of a 2-aminopyrazine series led to th...
Despite recent progress in the fight against malaria, the emergence and spread of drug-resistant par...
Malaria deaths have been decreasing over the last 10–15 years, with global mortality rates having fa...
Toward improving pharmacokinetics, in vivo efficacy, and selectivity over hERG, structure-activity r...
Novel antimalarial therapeutics that target multiple stages of the parasite lifecycle are urgently r...
Optimization of a chemical series originating from whole-cell phenotypic screening against the human...
On the basis of the initial success of optimization of a novel series of imidazolopiperazines, a sec...
On the basis of our recent results on a novel series of imidazopyridazine-based antimalarials, we fo...
A previous publication from our laboratory reported the identification of a new class of 2-(1H-imida...
Imidazopyridine <b>1</b> was identified from a phenotypic screen against <i>P. falciparum</i> (Pf) b...
On the basis of our recent results on a novel series of imidazopyridazine-based antimalarials, we fo...
A lead-optimization program around a 2,6-imidazopyridine scaffold was initiated based on the two ear...
A novel class of imidazopyridazines identified from whole cell screening of a SoftFocus kinase libra...
Malaria deaths have been decreasing over the last 10–15 years, with global mortality rates having fa...
Most malaria drug development focuses on parasite stages detected in red blood cells, even though, t...
Introduction of water-solubilizing groups on the 5-phenyl ring of a 2-aminopyrazine series led to th...
Despite recent progress in the fight against malaria, the emergence and spread of drug-resistant par...
Malaria deaths have been decreasing over the last 10–15 years, with global mortality rates having fa...
Toward improving pharmacokinetics, in vivo efficacy, and selectivity over hERG, structure-activity r...
Novel antimalarial therapeutics that target multiple stages of the parasite lifecycle are urgently r...
Optimization of a chemical series originating from whole-cell phenotypic screening against the human...