1,3-DISUPSTITUISAN BENZIMIDAZOL-2-ON DERIVAT KAO INHIBITOR DIPEPTIDIL PEPTIDAZE-4
Sažetak
Benzimidazol je vredan sintetski povoljan drug-like skelet. Derivata benzimidazola ima i među inhibitorima multifunkcionalne aminopeptidaze dipeptidil peptidaze-4 (DPP-4), ciljane proteaze u terapiji dijabetesa tipa 2. Nakon proučavanja serije DPP-4 inhibitora sa 1,3-disupstituisanim benzimidazol-2-iminom kao osnovom, u ovom radu je ispitivan inhibitorni potencijal 1,3-disupstituisanih benzimidazol-2-on derivata na ovoj proteazi. 5-Metil-1,3-bis(2-okso-2-feniletil)-1,3-dihidro-2H-benzimidazol-2-on (jedinjenje 5) inhibirao je aktivnost DPP-4 sa IC50 vrednošću koja je iznosila oko 200 μM. Iako nije tako potentan inhibitor, jedinjenje 5 može doprineti dizajnu i optimizaciji inhibitora DPP-4 sa benzimidazolom kao osnovom.
Reference
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