92033-74-4

Upstream product

• 35661-60-0 Fmoc-Leu-OH 
• 103-71-9 phenyl isocyanate 
• 65-85-0 benzoic acid 
• 61-90-5 L-leucine 
• 86298-24-0 N-phenyl-1H-benzo[d][1,2,3]triazole-1-carboxamide 
• 2748-02-9 L-leucine tert-butyl ester hydrochloride 
• 21691-53-2 L-leucine tert-butyl ester 
• 1259946-52-5 N-(phenylcarbamoyl)-leucine tert-butyl ester 
• 88576-97-0 N-(N-phenylcarbamoyl-leucyl)-glycine 
• 168471-11-2 (S)-4-Methyl-2-(3-phenyl-ureido)-pentanoic acid benzyl ester 
• 2899-43-6 DL-leucine ethyl ester 

Downstream Products

• 1259946-59-2 (N-phenylcarbamoyl)leucine 1,2-dimethylhydrazide 
• 1259945-85-1 N-(phenylcarbamoyl)-leucyl-methylazaalanine-nitrile 
• 168471-14-5 5-Methyl-2-{(R)-2-(1-methyl-1H-indol-3-yl)-1-[(S)-4-methyl-2-(3-phenyl-ureido)-pentanoylamino]-ethyl}-oxazole-4-carboxylic acid benzyl ester 
• 2221-06-9 5-isobutyl-3-phenylimidazolidine-2,4-dione 
• 104060-50-6 phenylcarbamoyl-L-leucine methyl ester 

Relevant academic research and scientific papers

One-pot preparation of carbamoyl benzotriazoles and their applications in the preparation of ureas, hydrazinecarboxamides and carbamic esters

Carbamoyl benzotriazoles were conveniently synthesized in one-pot from carboxylic acids, diphenyl phosphorazidate (DPPA) and 1H-benzotriazole (BtH). The reactivity and applications of carbamoyl benzotriazoles were also explored. Carbamoyl benzotriazoles react smoothly with amino acids, hydrazines and alcohols, thus providing facile access to the corresponding ureas, hydrazinecarboxamides and carbamic esters, respectively, in good to excellent yields.

Structural optimization of azadipeptide nitriles strongly increases association rates and allows the development of selective cathepsin inhibitors

Using the example of cathepsin K, we demonstrate the design of highly potent and selective azadipeptide nitrile inhibitors. A systematic scan with respect to P2 and P3 substituents was carried out. Structural modifications strongly affected the enzyme-inh

Solid-phase synthesis of oligourea peptidomimetics

A procedure for the solid-phase synthesis of oligourea peptidomimetics starting from Boc-protected monomers is described. The compounds are prepared on Tentagel resin and can be obtained selectively rather as the C-terminal free acids with UV irradiation

Azole endothelin antagonists. 2. Structure-activity studies

Structure-activity studies have been performed in an attempt to improve the potency of a novel series of azole-based endothelin-A (ET(A)) selective antagonists. Modifications of the hydrophobic group on the terminal urea produced substantial effects on receptor affinity; in particular, the choice of cyclohexyl- or arylureas led to substantial improvements in activity. Conformational restriction of these groups provides an additional benefit. N- Methylation of the indole moiety which is part of the heterocyclic dipeptide surrogate also improves potency. The effects of these two modifications appear to be synergistic, with the best of the resultant doubly modified analogs (e.g. 14q, 15y, and 15ff) exhibiting an 80-200-fold improvement over the original leads.

Aldehyde derivatives and their use as calpain inhibitors

Aldehyde derivatives with a specific calpain inhibiting activity and a platelet-aggregation inhibiting effect with formula (I) or formula (II): wherein R1 represents an aromatic hydrocarbon group, a heterocyclic group, or a group of-X-R3 in which X represents O,-S(O)m-(m = 0, 1, or 2), and R3 represents an aromatic hydrocarbon group, a heterocyclic group, or an alkyl group; Z represents R?-Y-or R?O-CH(R?)-in which Y represents a 3-to 7-membered nitrogen-containing saturated heterocyclic group, or a single cyclic saturated hydrocarbon group, R? represents an alkyl group, an alkenyl group, an alkynyl group, an acyl group, a sulfonyl group, an alkoxycarbonyl group, a carbamoyl group, or a thiocarbamoyl group, R? represents hydrogen, an alkyl group, or an aromatic hydrocarbon group, and R? represents an acyl group, a carbamoyl group, a thiocarbamoyl group, or an alkyl group; and n is an integer of 1 to 5. wherein R?, R?, R?, and R1? are defined in the specification.