title: [Study on derivatives of 5-amino-4-acylamino-1H-pyrazole as inhibitors of furin].
abstract: A series of 5-amino-1H-pyrazoles was synthesized and studied as inhibitors of furin. The most potent compound, 5-amino-4-acetylamino-3-(4-methylphenylamino)1H-pyrazole, was found to retard the activity of furin by mixed-type inhibition with K = 288 microM. These findings permit to plan new ways for chemical modifications of the 5-amino-1H-pyrazole structure and design more potent furin inhibitors of non-peptide nature.
authors.forename: V K
authors.initials: VK
authors.lastname: Kibirev
authors.forename: T V
authors.initials: TV
authors.lastname: Osadchuk
authors.forename: O B
authors.initials: OB
authors.lastname: Vadziuk
authors.forename: O V
authors.initials: OV
authors.lastname: Shablykin
authors.forename: A P
authors.initials: AP
authors.lastname: Kozachenko
authors.forename: S A
authors.initials: SA
authors.lastname: Chumachenko
authors.forename: S V
authors.initials: SV
authors.lastname: Popil'nichenko
authors.forename: V S
authors.initials: VS
authors.lastname: Brovarets
mesh_terms: D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D045683:Furin / Q000037:antagonists & inhibitors* / Q000737:chemistry; D015394:Molecular Structure; D011720:Pyrazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D013329:Structure-Activity Relationship
chemical_list: C561133:5-amino-4-acetylamino-3-(4-methylphenylamino)1H-pyrazole; D004791:Enzyme Inhibitors; D011720:Pyrazoles; D045683:Furin