606117-06-0

Upstream product

• 606091-78-5 C₉H₆N₄OS 
• 100-39-0 benzyl bromide 
• 58842-61-8 benzimidazole-5-carboxylic acid ethyl ester 
• 108038-52-4 1H-benzimidazole-5-carbohydrazide 
• 15788-16-6 5-benzimidazolecarboxylic acid 
• 606091-78-5 5-(1H-benzo[d]imidazol-6-yl)-1,3,4-oxadiazole-2-thiol 

Relevant academic research and scientific papers

Structure-activity relationships of benzimidazole-based glutaminyl cyclase inhibitors featuring a heteroaryl scaffold

Glutaminyl cyclase (hQC) has emerged as a new potential target for the treatment of Alzheimer's disease (AD). The inhibition of hQC prevents of the formation of the Aβ3(pE)-40,42 species which were shown to be of elevated neurotoxicity and are likely to act as a seeding core, leading to an accelerated formation of Aβ-oligomers and fibrils. This work presents a new class of inhibitors of hQC, resulting from a pharmacophore-based screen. Hit molecules were identified, containing benzimidazole as the metal binding group connected to 1,3,4-oxadiazole as the central scaffold. The subsequent optimization resulted in benzimidazolyl-1,3,4-thiadiazoles and -1,2,3-triazoles with an inhibitory potency in the nanomolar range. Further investigation into the potential binding mode of the new compound classes combined molecular docking and site directed mutagenesis studies.

NOVEL INHIBITORS OF GLUTAMINYL CYCLASE

The present invention relates to compounds of formula (I), combinations and uses thereof for disease therapy, Formula (I) wherein R1 represents heteroaryl, -carbocyclyl-heteroaryl, -alkenylheteroaryl or -alkylheteroaryl; R2 represents alkyl; carbocyclyl which may optionally be substituted by alkyl; alkenyl; alkynyl, provided a triple bond is not adjacent to X; -alkyl-aryl; -alkyl-heteroaryl; -alkyl-heterocyclyl in which heterocyclyl may optionally be substituted by alkyl; -alkyl-carbocyclyl in which carbocyclyl may optionally be substituted by alkyl; aryl; heteroaryl; or H; X represents S or NR3; R3 represents H or C1-4 alkyl.