Epoxy compounds usually have stronger nucleophilic ability, because the alkyl group on the oxygen atom makes the bond angle smaller, which makes the lone pair of electrons react more dissimilarly with the electron-deficient system. Compound: 2-Amino-5-chlorobenzaldehyde, is researched, Molecular C7H6ClNO, CAS is 20028-53-9, about Synthesis and Pharmacological Evaluation of Tetrahydro-γ-carboline Derivatives as Potent Anti-inflammatory Agents Targeting Cyclic GMP-AMP Synthase.Reference of 2-Amino-5-chlorobenzaldehyde.
The activation of cyclic GMP-AMP synthase (cGAS) by double-stranded DNA is implicated in the pathogenesis of many hyper inflammatory and autoimmune diseases, and the cGAS-targeting small mol. has emerged as a novel therapeutic strategy for treating these diseases. However, the currently reported cGAS inhibitors are far beyond maturity, barely demonstrating in vivo efficacy. Inspired by the structural novelty of compound I (G140), a structural optimization on both its side chain and the central tricyclic core, leads to several subseries of compounds, including those unexpectedly cyclized complex ones. Compound II (R = aminomethyl) bearing an N-glycylglycinoyl side chain was identified as the most potent one with cellular IC50 values of 1.38 and 11.4μM for h- and m-cGAS, resp. Mechanistic studies confirmed its direct targeting of cGAS. Further, compound II (R = aminomethyl) showed superior in vivo anti-inflammatory effects in the lipopolysaccharide-induced mouse model. The encouraging result of compound II (R = aminomethyl) provides solid evidence for further pursuit of cGAS-targeting inhibitors as a new anti-inflammatory treatment.
This literature about this compound(20028-53-9)Reference of 2-Amino-5-chlorobenzaldehydehas given us a lot of inspiration, and I hope that the research on this compound(2-Amino-5-chlorobenzaldehyde) can be further advanced. Maybe we can get more compounds in a similar way.
Reference:
Tetrahydrofuran – Wikipedia,
Tetrahydrofuran | (CH2)3CH2O – PubChem