Bioorganic & medicinal chemistry letters

Bioorg Med Chem Lett · ISSN (e) 1464-3405 · 5 papers in corpus
other 2025
Design of a peripherally biased NPSR1 antagonist for neuropeptide S induced inflammation
doi:10.1016/j.bmcl.2025.130353 ·PMID:40752839

Neuropeptide S (NPS) is a potent agonist for the GPCR receptor NPSR1, implicated in various physiological and pathological processes, including inflammation. NPSR1 gene polymorphisms have been linked to asthma, inflammatory bowel disease, a…

article 2019
Discovery and optimization of pyridyl-cycloalkyl-carboxylic acids as inhibitors of microsomal prostaglandin E synthase-1 for the treatment of endometriosis
doi:10.1016/j.bmcl.2019.07.007 ·PMID:31362919
other 2012
New aromatase inhibitors from the 3-pyridyl arylether and 1-aryl pyrrolo[2,3-c]pyridine series
doi:10.1016/j.bmcl.2012.01.076 ·PMID:22335894

Aromatase inhibition is the new standard of care for estrogen receptor positive breast cancer and has also potential for treatment of other diseases such as endometriosis. Simple and readily available 3-pyridyl arylethers and 1-aryl pyrrolo…

other 2010
Improving the developability profile of pyrrolidine progesterone receptor partial agonists
doi:10.1016/j.bmcl.2009.10.092 ·PMID:19926282

The previously reported pyrrolidine class of progesterone receptor partial agonists demonstrated excellent potency but suffered from serious liabilities including hERG blockade and high volume of distribution in the rat. The basic pyrrolidi…

other 2010
Synthesis and biological evaluation of piperazinyl heterocyclic antagonists of the gonadotropin releasing hormone (GnRH) receptor
doi:10.1016/j.bmcl.2010.02.099 ·PMID:20236823

Antagonism of the gonadotropin releasing hormone (GnRH) receptor has resulted in positive clinical results in reproductive tissue disorders such as endometriosis and prostate cancer. Following the recent discovery of orally active GnRH anta…