{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,9,26]],"date-time":"2026-09-26T04:05:48Z","timestamp":1790395548382,"version":"4.1.0"},"reference-count":23,"publisher":"Wiley","issue":"7","license":[{"start":{"date-parts":[[2025,1,12]],"date-time":"2025-01-12T00:00:00Z","timestamp":1736640000000},"content-version":"vor","delay-in-days":0,"URL":"http:\/\/onlinelibrary.wiley.com\/termsAndConditions#vor"}],"content-domain":{"domain":["chemistry-europe.onlinelibrary.wiley.com"],"crossmark-restriction":true},"short-container-title":["ChemMedChem"],"published-print":{"date-parts":[[2025,4]]},"abstract":"<jats:title>Abstract<\/jats:title>\n                  <jats:p>\n                    The pro\u2010inflammatory cytokine interleukin\u201017A (IL\u201017) plays an important role in the body's defense against bacterial and fungal infections. However, overexpression of IL\u201017 has been associated with several diseases, including rheumatoid arthritis, asthma, psoriasis, and even cancer. The role of IL\u201017 in psoriasis has been confirmed by clinical use of IL\u201017 antibodies, e.\u2009g. secukinumab (Cosentyx\n                    <jats:sup>\u00ae<\/jats:sup>\n                    ). Ongoing research is focused on discovering low molecular weight IL\u201017 inhibitors. In this publication, we present thiazole\u2010based IL\u201017 inhibitors discovered through a scaffold\u2010morphing strategy. This strategy involved ring\u2010opening of a known scaffold and utilization of a chalcogen interaction between thiazole\u2010sulfur and central amide\u2010oxygen to maintain the coplanar conformation found in the parent compound. The new scaffold enabled the generation of highly potent compounds with good overall profile. The optimized compounds\n                    <jats:bold>11<\/jats:bold>\n                    and\n                    <jats:bold>15<\/jats:bold>\n                    demonstrated good exposure in rats after oral dosing. Importantly, compound\n                    <jats:bold>11<\/jats:bold>\n                    exhibited no adverse effects in a rat tolerability study after a four\u2010day administration of up to 300\u2005mg\/kg\/day.\n                  <\/jats:p>","DOI":"10.1002\/cmdc.202400851","type":"journal-article","created":{"date-parts":[[2024,12,23]],"date-time":"2024-12-23T12:39:02Z","timestamp":1734957542000},"update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":14,"title":["Thiazole\u2010Based IL\u201017 Inhibitors Discovered by Scaffold Morphing"],"prefix":"10.1002","volume":"20","author":[{"ORCID":"https:\/\/orcid.org\/0000-0001-6564-1448","authenticated-orcid":false,"given":"Juraj","family":"Velcicky","sequence":"first","affiliation":[{"name":"Novartis Biomedical Research Novartis Campus  4056 Basel 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