https://pubmed.ncbi.nlm.nih.gov/38116446
Researchers from Pfizer discovered a new class of potent and orally bioavailable SHP2 inhibitors, 5-azaquinoxaline derivatives, as promising candidates for oncology drug discovery.
https://pubmed.ncbi.nlm.nih.gov/38116445
Researchers at Novartis have developed a chiral synthesis route for muscarinic M4 agonists using biocatalytic synthesis of spirocyclic diamine building blocks, leading to the identification of selective M1/M4 agonists.
https://pubmed.ncbi.nlm.nih.gov/38116444
A new series of benzodiazepine compounds have been discovered that inhibit Cbl-b, a protein responsible for suppressing immune cell activation, and show potential for enhancing antitumor immunity.
https://pubmed.ncbi.nlm.nih.gov/38116443
This abstract describes the discovery of new fused pyrazole amide analogs that inhibit glucosylceramide synthase, with potential therapeutic applications in various diseases including lysosomal storage diseases, neurodegenerative diseases, cystic diseases, and cancer.
https://pubmed.ncbi.nlm.nih.gov/38116442
The study identified specific 5-arylethynyl aminothiophene derivatives that act as positive allosteric modulators of the A1 adenosine receptor, with one compound also exhibiting agonist activity, offering potential as drug candidates for engaging protective A1ARs.
https://pubmed.ncbi.nlm.nih.gov/38116441
Researchers have developed conformationally restricted analogues of α-galactosylceramide that enhance the immune response to a COVID-19 subunit vaccine in mice, and omitting certain adjuvants in the booster vaccine has minimal impact on antibody and cellular responses.
https://pubmed.ncbi.nlm.nih.gov/38116438
Researchers have developed new NBTIs (Novel Bacterial Topoisomerase Inhibitors) with a indane DNA intercalating moiety that exhibit potent activity against Gram-negative bacteria and minimal hERG inhibition, although their unusual pharmacokinetic profile limits their development as potential new antibiotics.
https://pubmed.ncbi.nlm.nih.gov/38116437
Enniatin A analogues have been identified as novel Hsp90 inhibitors with immunogenic activity, and preliminary SAR studies reveal that branching moieties are necessary for their activity.