896746-87-5

Upstream product

• 896746-84-2 (R)-3-hydroxymethyl-5-phenyl-1,3-dihydro-benzo[e][1,4]diazepin-2-one 
• 18162-48-6 tert-butyldimethylsilyl chloride 
• 105-36-2 ethyl bromoacetate 
• 2835-77-0 (2-aminophenyl)(phenyl)methanone 
• 896746-83-1 (R)-4-(2-benzoyl-phenylcarbamoyl)-2,2-dimethyl-oxazolidine-3-carboxylic acid tert-butyl ester 
• 896746-85-3 (R)-3-(tert-butyl-dimethyl-silanyloxymethyl)-5-phenyl-1,3-dihydro-benzo[e][1,4]diazepin-2-one 

Downstream Products

• 1012860-21-7 2-[(3R)-3-({[tert-butyl(dimethyl)silyl]oxy}methyl)-2-oxo-5-phenyl-2,3-dihydro-1H-1,4-benzodiazepin-1-yl]-N-[(1S)-1-(2-phenylethyl)prop-2-en-1-yl]acetamide 
• 1234549-25-7 2-[(3R)-3-(tert-butyl-dimethyl-silanyloxymethyl)-2-oxo-5-phenyl-2,3-dihydro-benzo[e][1,4]diazepin-1-yl]-N-[(2R,3S)-2-tertbutylthio-5-oxo-tetrahydrofuran-3-yl]-acetamide 
• 1242185-32-5 2-((R)-3-((tert-butyldimethylsilyloxy)methyl)-2-oxo-5-phenyl-2,3-dihydro-1H-benzo[e][1,4]diazepin-1-yl)-N-(5-methylhex-1-en-3-yl)acetamide 
• 1012860-26-2 N-allyl-2-[(3R)-3-(hydroxymethyl)-2-oxo-5-phenyl-2,3-dihydro-1H-1,4-benzodiazepin-1-yl]acetamide 
• 1012860-24-0 {(3R)-1-[2-(allylamino)-2-oxoethyl]2-oxo-5-phenyl-2,3-dihydro-1H-1,4-benzodiazepin-3-yl}methyl[4-chloro-2-(trifluoromethyl)phenyl]carbamate 
• 1140908-16-2 (R,E)-methyl4-(2-(3((4-chloro-2-(trifluoromethyl)phenylcarbamoyloxy)methyl)-2-oxo-5-phenyl-2,3-dihydro-1H-benzo[e][1,4]diazepin-1-yl)acetamido)but-2-enoate 
• 896746-98-8 4-semicarbazone-3(S)-[2-(2-oxo-5-phenyl-3(R)-(4-chloro-2-trifluoromethylphenylcarbamoyloxymethyl)-2,3-dihydro-benzo[e][1,4]diazepin-1-yl)acetylamino]butyric acid tert-butyl ester 
• 896746-96-6 4-semicarbazone-3(S)-[2-(2-oxo-5-phenyl-3(R)-(2-bromo-4,6-difluorophenylcarbamoyloxymethyl)-2,3-dihydro-benzo[e][1,4]diazepin-1-yl)acetylamino]butyric acid tert-butyl ester 
• 896746-91-1 4-semicarbazone-3(S)-[2-(2-oxo-5-phenyl-3(R)-(1-naphthylcarbamoyloxymethyl)-2,3-dihydro-benzo[e][1,4]diazepin-1-yl)acetylamino]butyric acid tert-butyl ester 
• 896746-95-5 4-semicarbazone-3(S)-[2-(2-oxo-5-phenyl-3(R)-(2,4-difluorophenylcarbamoyloxymethyl)-2,3-dihydro-benzo[e][1,4]diazepin-1-yl)acetylamino]butyric acid tert-butyl ester 
• 896746-97-7 4-semicarbazone-3(S)-[2-(2-oxo-5-phenyl-3(R)-(4-chloro-2-methylphenylcarbamoyloxymethyl)-2,3-dihydro-benzo[e][1,4]diazepin-1-yl)acetylamino]butyric acid tert-butyl ester 
• 896746-94-4 4-semicarbazone-3(S)-[2-(2-oxo-5-phenyl-3(R)-(4-fluorophenylcarbamoyloxymethyl)-2,3-dihydro-benzo[e][1,4]diazepin-1-yl)acetylamino]butyric acid tert-butyl ester 

Relevant academic research and scientific papers

Synthesis and biological evaluation of novel peptidomimetics as rhodesain inhibitors

Novel rhodesain inhibitors were developed by combining an enantiomerically pure 3-bromoisoxazoline warhead with a 1,4-benzodiazepine scaffold as specific recognition moiety. All compounds were proven to inhibit rhodesain with K i values in the low-micromolar range. Their activity towards rhodesain was found to be coupled to an in vitro antitrypanosomal activity, with IC50 values ranging from the mid-micromolar to a low-micromolar value for the most active rhodesain inhibitor (R,S,S)-3. All compounds showed a good selectivity against the target enzyme since all of them were proven to be poor inhibitors of human cathepsin L.

NMR characterization and conformational analysis of a potent papain-family cathepsin L-like cysteine protease inhibitor with different behaviour in polar and apolar media

We recently reported the synthesis, of a potent papain-family cathepsin L-like cysteine protease inhibitor, as new lead compound for the development of new drugs that can be used as antiprotozoal agents. The investigation of its conformational profile is

Novel peptidomimetic cysteine protease inhibitors as potential antimalarial agents

The synthesis of a new class of peptidomimetics 1a-j, based on a 1,4-benzodiazepine scaffold and on a C-terminal aspartyl aldehyde building block, is described. Compounds 1a-j provided significant inhibitory activity against falcipains 2A and 2B (FP-2A an