Structural insight into the optimization of ethyl 5-hydroxybenzo[g]indol-3-carboxylates and their bioisosteric analogues as 5-LO/m-PGES-1 dual inhibitors able to suppress inflammation was written by Bruno, Ferdinando;Errico, Suann;Pace, Simona;Nawrozkij, Maxim B.;Mkrtchyan, Arthur S.;Guida, Francesca;Maisto, Rosa;Olgac, Abdurrahman;D’Amico, Michele;Maione, Sabatino;De Rosa, Mario;Banoglu, Erden;Werz, Oliver;Fiorentino, Antonio;Filosa, Rosanna. And the article was included in European Journal of Medicinal Chemistry in 2018.Application In Synthesis of Ethyl 3-oxo-3-(m-tolyl)propanoate This article mentions the following:
The release of pro-inflammatory mediators, such as prostaglandines (PGs) and leukotrienes (LTs), arising from the arachidonic acid (AA) cascade, play a crucial role in initiating, maintaining, and regulating inflammatory processes. New dual inhibitors of 5-lipoxygenase (5-LO) and microsomal prostaglandin E2 synthase-1 (mPGES-1), that block, at the same time, the formation of PGE2 and LTs, are currently emerged as a highly interesting drug candidates for better pharmacotherapie of inflammation-related disorders. Following our previous studies, we here performed a detailed structure-based design of benzo[g]indol-3-carboxylate derivatives, disclosing several new key factors that affect both enzyme activity. Et 2-(3,4-dichlorobenzyl)-5-hydroxy-1H-benzo[g]indole-3-carboxylate (4b, RAF-01) and Et 2-(3,4-dichlorophenyl)-5-hydroxy-1H-benzo[g]indole-3-carboxylate (7h, RAF-02) emerged as the most active compounds of the series. Addnl., together with selected structure based analogs, both derivatives displayed significant in vivo anti-inflammatory properties. In conclusion, modeling and exptl. studies lead to the discovery of new candidate compounds prone to further developments as multi-target inhibitors of the inflammatory pathway. In the experiment, the researchers used many compounds, for example, Ethyl 3-oxo-3-(m-tolyl)propanoate (cas: 33166-79-9Application In Synthesis of Ethyl 3-oxo-3-(m-tolyl)propanoate).
Ethyl 3-oxo-3-(m-tolyl)propanoate (cas: 33166-79-9) belongs to esters. Esters are also usually derived from carboxylic acids. It may also be obtained by reaction of acid anhydride or acid halides with alcohols or by the reaction of salts of carboxylic acids with alkyl halides. Esterification is the general name for a chemical reaction in which two reactants (typically an alcohol and an acid) form an ester as the reaction product. Esters are common in organic chemistry and biological materials.Application In Synthesis of Ethyl 3-oxo-3-(m-tolyl)propanoate
Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics