Chemistry can be defined as the study of matter and the changes it undergoes. You’ll sometimes hear it called the central science because it is the connection between physics and all the other sciences, starting with biology. 4727-72-4, Name is 1-Benzylpiperidin-4-ol, molecular formula is , belongs to piperidines compound. In a document, author is Ngemenya, Moses N., Application In Synthesis of 1-Benzylpiperidin-4-ol.
Background: Emergence of resistance to artemisinins and some of their combinations in chemotherapy of clinical malaria has intensified the search for novel safe efficacious antimalarial molecules. Fourteen synthetic 1,4-disubstituted piperidines with simple molecular structures were evaluated in this study. Methods: Antiplasmodial activity were determined against cultured chloroquine-sensitive 3D7 and resistant Dd2 strains of P. falciparum by in vitro parasite growth inhibition. A primary screen was done to identify active compounds by fluorescence microscopy followed by a secondary screen to determine IC50 and IC90 values of active compounds by the parasite lactate dehydrogenase assay. Cytotoxicity of active compounds was assessed using the MTT/formazan assay and selectivity indices (SIs) determined. Optical densities were analysed to obtain experimental results. Results: The compounds produced 56 to 93% inhibition of parasite growth at 40 mu g/mL. Eight compounds (2 ketone, 5 alcohol and one amine analogues) showed high activity (IC(50)s between 1 and 5 mu g/mL). Nine compounds were highly selective for the parasite (SIs = 15 to 182). Three promising (alcohol) analogues were identified: [1-(4-fluorobenzyl) piperidin- 4-yl] [4-fluorophenyl] methanol, (7), [1-(3, 4-dichlorobenzyl) piperidin-4-yl] [4- fluorophenyl] methanol (8) and [1-(4-bromobenzyl) piperidin-4-yl] [4- fluorophenyl] methanol (11) which were more active on the resistant strain (IC50 values between 1.03 to 2.52 mu g/mL), than the sensitive strain (IC50 values between 2.51 to 4. 43 mu g/mL). Conclusions: The alcohol analogues were the most active and most selective for the parasite with three promising hit molecules identified among them, suggesting the hydroxyl group at C-7′ in these alcohol analogues is contributing greatly to their antiplasmodial activity. Further exploration of the core structure using chemistry approaches and biological screening including in vivo studies in an animal model of malaria may yield important antimalarial leads.
Sometimes chemists are able to propose two or more mechanisms that are consistent with the available data. If a proposed mechanism predicts the wrong experimental rate law, however, the mechanism must be incorrect.Welcome to check out more blogs about 4727-72-4, in my other articles. Application In Synthesis of 1-Benzylpiperidin-4-ol.
Reference:
Piperidine – Wikipedia,
,Piperidine | C5H11N – PubChem