Mu, Ruixu published the artcileDiscovery of novel triazole compounds as selective IL-1β releasement inhibitors, HPLC of Formula: 15029-36-4, the publication is Bioorganic & Medicinal Chemistry Letters (2021), 128415, database is CAplus and MEDLINE.
Inflammation and immunity are closely related to the occurrence and development of a variety of immune diseases. Although IL-1β has been identified as a key cytokine in many immune diseases, safe and specific small mol. IL-1β releasement inhibitors are still scarce and urgently required in clinic. The investigation prospect of triazoleis limited by its complicated pharmacol. effect which exhibited inferior effects on IL-1β and TNF-α. Herein, 36 novel derivatives were designed and synthesized, and nearly half of the derivatives exhibited much better selectivity on IL-1β releasement inhibition as well as keep similar inhibitory activities to lead compound In 20 μM, compound 19 exhibited IL-1β releasement inhibitory activity (IC50 = 5.489 μM) which closed to the original compound, and 4.5-fold superior selectivity (SI = 4.71) to the lead compound (SI = 0.82). A probable SAR model of triazole derivatives for IL-1β releasement inhibition and selectivity was also proposed, which might promote the discovery of more effective and specific IL-1β releasement inhibitors in the future.
Bioorganic & Medicinal Chemistry Letters published new progress about 15029-36-4. 15029-36-4 belongs to amides-buliding-blocks, auxiliary class Nitrile,Amine,Aliphatic hydrocarbon chain,Amide, name is 2-Cyano-N-ethylacetamide, and the molecular formula is C5H8N2O, HPLC of Formula: 15029-36-4.
Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics