Ester is a chemical compound derived from an oxoacid (organic or inorganic) in which at least one –OH hydroxyl group is replaced by an –O– alkyl (alkoxy) group, 87-13-8, formula is C10H16O5, Name is Diethyl 2-(ethoxymethylene)malonate. as in the substitution reaction of a carboxylic acid and an alcohol. Electric Literature of 87-13-8.
Messore, Antonella;Corona, Angela;Madia, Valentina Noemi;Saccoliti, Francesco;Tudino, Valeria;De Leo, Alessandro;Ialongo, Davide;Scipione, Luigi;De Vita, Daniela;Amendola, Giorgio;Novellino, Ettore;Cosconati, Sandro;Metifiot, Mathieu;Andreola, Marie-Line;Esposito, Francesca;Grandi, Nicole;Tramontano, Enzo;Costi, Roberta;Di Santo, Roberto research published 《 Quinolinonyl Non-Diketo Acid Derivatives as Inhibitors of HIV-1 Ribonuclease H and Polymerase Functions of Reverse Transcriptase》, the research content is summarized as follows. Novel anti-HIV agents are still needed to overcome resistance issues, in particular inhibitors acting against novel viral targets. The RNase H function of the reverse transcriptase (RT) represents a validated and promising target, and no inhibitor has reached the clin. pipeline yet. Here, we present rationally designed non-diketo acid selective RNase H inhibitors (RHIs) based on the quinolinone scaffold starting from former dual integrase (IN)/RNase H quinolinonyl diketo acids. Several derivatives were synthesized and tested against RNase H and viral replication and found active at micromolar concentrations Docking studies within the RNase H catalytic site, coupled with site-directed mutagenesis, and Mg2+ titration experiments demonstrated that our compounds coordinate the Mg2+ cofactor and interact with amino acids of the RNase H domain that are highly conserved among naive and treatment-experienced patients. In general, the new inhibitors influenced also the polymerase activity of RT but were selective against RNase H vs. the IN enzyme.
87-13-8, Diethyl ethoxymethylenemalonate is a useful research compound. Its molecular formula is C10H16O5 and its molecular weight is 216.23 g/mol. The purity is usually 95%.
Diethyl ethoxymethylidenemalonate is a matrix effect reagent used in analytical chemistry. It is often used as a substrate for the cycloaddition process, which produces malondialdehyde and hydrochloric acid. The UV-absorption of the malondialdehyde can be measured to determine the concentration of the sample. Diethyl ethoxymethylidenemalonate is also used as a dna template in binding constants, where it binds with amines to form complexes that are then analyzed by light emission. It has been shown to have an inhibitory effect on gyrase and trifluoroacetic acid, both enzymes involved in DNA replication., Electric Literature of 87-13-8
Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics