Category: 332026-86-5

Li, Qi published the artcileDiscovery and Biological Evaluation of a Novel Highly Potent Selective Butyrylcholinsterase Inhibitor, Recommanded Product: 4-(1H-Benzo[d]imidazol-2-yl)-1,2,5-oxadiazol-3-amine, the publication is Journal of Medicinal Chemistry (2020), 63(17), 10030-10044, database is CAplus and MEDLINE.

To discover novel BChE inhibitors, a hierarchical virtual screening protocol followed by biochem. evaluation was applied. The most potent compound 8012-9656(I) (eqBChE IC₅₀ = 0.18 ± 0.03 μM, hBChE IC₅₀ = 0.32 ± 0.07 μM) was purchased and synthesized. It inhibited BChE in a noncompetitive manner and could occupy the binding pocket forming diverse interactions with the target. 8012-9656 was proven to be safe in vivo and in vitro and showed comparable performance in ameliorating the scopolamine-induced cognition impairment to tacrine. Addnl., treatment with 8012-9656 could almost entirely recover the Aβ_1-42 (icv)-impaired cognitive function to the normal level and showed better behavioral performance than donepezil. The evaluation of the Aβ_1-42 total amount confirmed its anti-amyloidogenic profile. Moreover, 8012-9656 possessed blood-brain barrier (BBB) penetrating ability, a long T_1/2, and low intrinsic clearance. Hence, the novel potential BChE inhibitor 8012-9656 can be considered as a promising lead compound for further investigation of anti-AD agents.

Journal of Medicinal Chemistry published new progress about 332026-86-5. 332026-86-5 belongs to imidazoles-derivatives, auxiliary class Oxadiazole,Amine,Benzimidazole, name is 4-(1H-Benzo[d]imidazol-2-yl)-1,2,5-oxadiazol-3-amine, and the molecular formula is C9H7N5O, Recommanded Product: 4-(1H-Benzo[d]imidazol-2-yl)-1,2,5-oxadiazol-3-amine.

Referemce:
https://en.wikipedia.org/wiki/Imidazole,
Imidazole | C3H4N2 – PubChem

Moore, Terry W. published the artcileSynthesis and Metabolic Studies of Host-Directed Inhibitors for Antiviral Therapy, Recommanded Product: 4-(1H-Benzo[d]imidazol-2-yl)-1,2,5-oxadiazol-3-amine, the publication is ACS Medicinal Chemistry Letters (2013), 4(8), 762-767, database is CAplus and MEDLINE.

Targeting host cell factors required for virus replication provides an alternative to targeting pathogen components and represents a promising approach to develop broad-spectrum antiviral therapeutics. High-throughput screening (HTS) identified two classes of inhibitors with broad-spectrum antiviral activity against ortho- and paramyxoviruses including influenza A virus (IAV), measles virus (MeV), respiratory syncytial virus (RSV), and human parainfluenza virus type 3 (HPIV3). Hit-to-lead optimization delivered inhibitor N-methyl-N-((1-methyl-4,5-diphenyl-1H-imidazol-2-yl)methyl)aniline, with EC₅₀ values of 0.88 and 0.81 μM against IAV strain WSN and MeV strain Edmonston, resp. It was also found that N-methyl-N-((1-methyl-4,5-diphenyl-1H-imidazol-2-yl)methyl)aniline delivers good stability in human liver S9 fractions with a half-life of 165 min. These data establish N-methyl-N-((1-methyl-4,5-diphenyl-1H-imidazol-2-yl)methyl)aniline as a promising lead for antiviral therapy through a host-directed mechanism.

ACS Medicinal Chemistry Letters published new progress about 332026-86-5. 332026-86-5 belongs to imidazoles-derivatives, auxiliary class Oxadiazole,Amine,Benzimidazole, name is 4-(1H-Benzo[d]imidazol-2-yl)-1,2,5-oxadiazol-3-amine, and the molecular formula is C9H7N5O, Recommanded Product: 4-(1H-Benzo[d]imidazol-2-yl)-1,2,5-oxadiazol-3-amine.

Referemce:
https://en.wikipedia.org/wiki/Imidazole,
Imidazole | C3H4N2 – PubChem

Sergievskii, A. V. published the artcileReactions of methyl 4-aminofurazan-3-carboximidate with nitrogen-containing nucleophiles, Synthetic Route of 332026-86-5, the publication is Russian Journal of Organic Chemistry (Translation of Zhurnal Organicheskoi Khimii) (2001), 37(5), 717-720, database is CAplus.

Me 4-aminofurazan-3-carboximidate reacts with aromatic amines and hydrazines to give the corresponding amidines and amidrazones. The reaction of the title compound with o-phenylenediamine yields 3-amino-4-(2-benzimidazoyl)furazan, and with acylhydrazines N²-acyl-4-aminofurazan-3-carbohydrazides are formed. The latter undergo thermal intramol. cyclization with formation of 3-amino-4-(1,2,4-triazol-3-yl)furazan derivatives containing various substituents in position 5 of the triazole ring.

Russian Journal of Organic Chemistry (Translation of Zhurnal Organicheskoi Khimii) published new progress about 332026-86-5. 332026-86-5 belongs to imidazoles-derivatives, auxiliary class Oxadiazole,Amine,Benzimidazole, name is 4-(1H-Benzo[d]imidazol-2-yl)-1,2,5-oxadiazol-3-amine, and the molecular formula is C10H14O, Synthetic Route of 332026-86-5.

Referemce:
https://en.wikipedia.org/wiki/Imidazole,
Imidazole | C3H4N2 – PubChem

Sergievskii, A. V. published the artcile4-Aminofurazan-3-carboxylic Acid Iminoester in Reactions with N,O-Nucleophiles, Formula: C9H7N5O, the publication is Russian Journal of Organic Chemistry (Translation of Zhurnal Organicheskoi Khimii) (2002), 38(6), 872-874, database is CAplus.

Reactions of 4-aminofurazan-3-carboxylic acid iminoester with o-aminophenol and ethylenediamine give rise resp. to 4-(1,3-benzoxazol-2-yl)- and 1-(4,5-dihydro-1H-imidazol-2-yl)-1,2,5-oxadiazol-3-amines, with aminoethanol arises 2-[(Z)-1-amino-1-(4-amino-1,2,5-oxadiazol-3-yl)methylideneamino]-1-ethanol. Treating of 3-amino-4-(1H-benzo[d]imidazol-2-yl)-1,2,5-oxadiazole with tri-Et orthoformate in acetic anhydride yielded benzo[4,5]imidazo[1,2-c][1,2,5]oxadiazolo[3,4-e]pyrimidine, and alkylation with haloalkanes furnished 3-amino-4-(1-R-benzo[d]imidazol-2-yl)-1,2,5-oxadiazoles.

Russian Journal of Organic Chemistry (Translation of Zhurnal Organicheskoi Khimii) published new progress about 332026-86-5. 332026-86-5 belongs to imidazoles-derivatives, auxiliary class Oxadiazole,Amine,Benzimidazole, name is 4-(1H-Benzo[d]imidazol-2-yl)-1,2,5-oxadiazol-3-amine, and the molecular formula is C7H8O3, Formula: C9H7N5O.

Referemce:
https://en.wikipedia.org/wiki/Imidazole,
Imidazole | C3H4N2 – PubChem