Mayoka, Godfrey published the artcileStructure-Activity Relationship and in Vitro Absorption, Distribution, Metabolism, Excretion, and Toxicity (ADMET) Studies of N-aryl 3-Trifluoromethyl Pyrido[1,2-a]benzimidazoles That Are Efficacious in a Mouse Model of Schistosomiasis, Computed Properties of 5961-59-1, the main research area is Schistosoma mansoni newly transformed schistosomula antschistosomal lead; Schistosoma mansoni; antischistosomal lead; newly transformed schistosomula; pyrido[1,2-a]benzimidazole.
We have previously reported on the antischistosomal activity of pyrido[1,2-a]benzimidazole (PBI) derivatives As a follow-up, we designed and prosecuted further structure-activity relationship (SAR) studies that incorporate N-aryl substitutions on the PBI scaffold. Investigations into the in vitro antischistosomal activity against newly transformed schistosomula (NTS) and adult worms revealed several leads with promising potency. Active compounds with a good cytotoxicity profile were tested in vivo whereby 6 and 44 induced noteworthy reduction (62-69%) in the worm load in the Schistosoma mansoni mouse model. Pharmacokinetic anal. on 44 (8-Dichloro-1-((2-fluorobenzyl)amino)-3(trifluoromethyl)benzo[4,5]imidazo[1,2-a]pyridine-4-carbonitrile) pointed to slow absorption, low volume of distribution, and low plasma clearance indicating the potential of these compounds to achieve a long duration of action. Overall, our work demonstrates that PBI chemotype is a promising scaffold in the discovery of new antischistosomal leads.
ACS Infectious Diseases published new progress about Pharmacokinetics. 5961-59-1 belongs to class isoquinoline, name is 4-Methoxy-N-methylaniline, and the molecular formula is C8H11NO, Computed Properties of 5961-59-1.
Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem