A new JMedChem publication from Welab

A new JMedChem publication from Welab

Discovery of WLB-89462, a New Drug-like and Highly Selective σ2 Receptor Ligand with Neuroprotective Properties”, in the Journal of Medicinal Chemistry.

ABSTRACT: The synthesis and pharmacological activity of a new series of isoxazolylpyrimidines as sigma-2 receptor (σ2R) ligands are reported. Modification of a new hit retrieved in an HTS campaign allowed the identification of the compound WLB-89462 (20c) with good σ2R affinity (Ki = 13 nM) and high selectivity vs both the σ1R (Ki = 1777 nM) and a general panel of 180 targets. It represents one of the first σ2R ligands with drug-like properties, linked to a good physicochemical and ADMET profile (good solubility, no CYP inhibition, good metabolic stability, high permeability, brain penetration, and high oral exposure in rodents). Compound 20c shows neuroprotective activity in vitro and improves short-term memory impairment induced by hippocampal injection of amyloid β peptide in rats. Together with the promising effects in the chronic models where 20c is currently being evaluated, these results pave the way toward its clinical development as a neuroprotective agent. (link to the publication)

Dear colleagues, collaborators, and friends,

After more than 30 years of shared endeavours, in which we have grown personally and professionally, and with our emotions on the surface, we announce the closure of our company. We have travelled together through ups and downs, celebrated successes and overcome challenges as a team.

We extend our deepest gratitude to each of you for your dedication, passion, and commitment to a shared goal: discovering new treatments for the benefit and well-being of patients.

As we bid farewell, let’s cherish the memories we’ve created, the bonds we’ve formed, and the impact we’ve made together. Though our paths may diverge, the spirit of collaboration and camaraderie that defines our community will always endure.

We leave proud of the work accomplished and thank you for being an integral part of our journey, wishing you success in all your future challenges.

With heartfelt appreciation,

Welab’s team

We are proud to announce that Welab is partner of this new EU funded project.

In collaboration with 12 partners from 6 countries, Welab Barcelona is establishing the Antivirus Pandemic Preparedness EuropeAn pLatform (APPEAL), a European research initiative aimed at enhancing preparedness for future pandemics. This EU funded collaboration will establish a comprehensive program for the development of broad-spectrum antiviral drugs within a five year time frame ensuring drug affordability and accessibility to low income countries.
Link to the press release: https://lnkd.in/d-jmV2CS