1073353-57-7Relevant articles and documents
Hydrogen Bond Directed ortho-Selective C?H Borylation of Secondary Aromatic Amides
Bai, Shao-Tao,Bheeter, Charles B.,Reek, Joost N. H.
supporting information, p. 13039 - 13043 (2019/07/31)
Reported is an iridium catalyst for ortho-selective C?H borylation of challenging secondary aromatic amide substrates, and the regioselectivity is controlled by hydrogen-bond interactions. The BAIPy-Ir catalyst forms three hydrogen bonds with the substrate during the crucial activation step, and allows ortho-C?H borylation with high selectivity. The catalyst displays unprecedented ortho selectivities for a wide variety of substrates that differ in electronic and steric properties, and the catalyst tolerates various functional groups. The regioselective C?H borylation catalyst is readily accessible and converts substrates on gram scale with high selectivity and conversion.
Arylboronic acids as dual-action FAAH and TRPV1 ligands
Morera, Enrico,Di Marzo, Vincenzo,Monti, Ludovica,Allarà, Marco,Schiano Moriello, Aniello,Nalli, Marianna,Ortar, Giorgio,De Petrocellis, Luciano
, p. 1401 - 1405 (2016/02/19)
A series of 31 arylboronic acids designed on the basis of the pharmacophore model for a variety of TRPV1 antagonists was prepared and tested on FAAH and TRPV1 channel. Four of them, that is, compounds 3c, 4a, 5a,b acted as dual FAAH/TRPV1 blockers with IC50 values between 0.56 and 8.11 μM whereas ten others (compounds 1c,f-i, 2c-f, 4b) inhibited FAAH and activated/desensitized TRPV1.
Identification of new γ-hydroxybutenolides that preferentially inhibit the activity of mPGES-1
De Simone, Rosa,Bruno, Ines,Riccio, Raffaele,Stadler, Katharina,Bauer, Julia,Schaible, Anja M.,Laufer, Stefan,Werz, Oliver
supporting information; experimental part, p. 5012 - 5016 (2012/09/22)
Microsomal prostaglandin E2 synthase-1 (mPGES-1) has been recognized as novel, promising drug target for anti-inflammatory and anticancer drugs. mPGES-1 catalyzes the synthesis of the inducible prostaglandin E 2 in response to pro-inflammatory stimuli, rendering this enzyme extremely interesting in drug discovery process owing to the drastic reduction of the severe side effects typical for traditional non-steroidal anti-inflammatory drugs. In the course of our investigations focused on this topic, we identified two interesting molecules bearing the γ- hydroxybutenolide scaffold which potently inhibit the activity of mPGES-1. Notably, the lead compound 2c that inhibited mPGES-1 with IC50 = 0.9 μM, did not affect other related enzymes within the arachidonic acid cascade.
