1016643-98-3

Upstream product

• 103882-09-3 N-Boc-4-I-Phe-OH 
• 1016643-91-6 Boc-Bip(4-Ph)-OBn 
• 129150-58-9 benzyl Boc-4-iodophenylalanine 
• 24424-99-5 di-tert-butyl dicarbonate 
• 1200-07-3 3-(4-bromophenyl)acrylic acid 
• 24250-84-8 H-p-BrPhe-OH 
• 5122-94-1 4-biphenylboronic acid 
• 62129-39-9 4-bromo-N-{[(1,1-dimethylethyl)oxy]carbonyl}-L-phenylalanine 
• 643016-66-4 N-(tert-butoxycarbonyl)-4[(4’;1’,1”)biphenyl]-L-phenylalanine methyl ester 
• 112766-18-4 methyl N-(tert-butoxycarbonyl)-O-[(trifluoromethyl)sulfonyl]-L-tyrosinate 
• 4326-36-7 (S)-N-(tert-butoxycarbonyl)tyrosine methyl ester 
• 1080-06-4 L-Tyr-OMe 
• 60-18-4 L-tyrosine 

Relevant academic research and scientific papers

Chemoenzymatic Synthesis of Optically Pure l- and d-Biarylalanines through Biocatalytic Asymmetric Amination and Palladium-Catalyzed Arylation

A chemoenzymatic approach was developed and optimized for the synthesis of a range of N-protected nonnatural l- and d-biarylalanine derivatives. Starting from 4-bromocinnamic acid and 4-bromophenylpyruvic acid using a phenylalanine ammonia lyase (PAL) and an evolved d-amino acid dehydrogenase (DAADH), respectively, both enantiomers of 4-bromophenylalanine were obtained and subsequently coupled with a panel of arylboronic acids to give the target compounds in high yield and optical purity under mild aqueous conditions.

MEDICAL DEVICES AND MATERIALS COMPRISING BIODEGRADABLE POLYESTERS

The present invention relates to a formulation comprising a biodegradable polyester mixed with a compound of formula (I): AA-AA-AA-X-Y. The invention further relates to manufacturing methods of these formulations, medical devices such as sutures comprising said formulations and manufacturing methods of said devices.

Methods of peptide modification

The present invention relates to a method of improving the resistance of a peptide or peptidomimetic to degradation by trypsin which comprises incorporating into said peptide or peptidomimetic a C-terminal capping group of formula (I): X—Y—Z (I) wherein X is a N atom, which may be substituted by a branched or unbranched C1-C10 alkyl or aryl group which group may incorporate up to 2 heteroatoms selected from N, O and S; Y represents a group selected from —Ra—Rb—, —Ra—Rb—Rb,- and —Rb—Rb—Ra— wherein Ra is C, O, S or N, and Rb is C; each of Ra and Rb, may be substituted by C1-C4 alkyl groups or unsubstituted; and Z is a group comprising 1 to 3 cyclic groups each of 5 or 6 non-hydrogen atoms, 2 or more of the cyclic groups may be fused and one or more of the cyclic groups may be substituted; the Z. moiety incorporates a maximum of 15 non-hydrogen atoms; and wherein the bond between Y and Z is a covalent bond between Ra or Rb of Y and a non-hydrogen atom of one of the cyclic groups of Z.

Synthesis and biological evaluation of tyrosine modified analogues of the α4β7 integrin inhibitor biotin-R8ERY

The α4β7 integrin is a well-known target for the development of drugs against various inflammatory disease states including inflammatory bowel disease, type 1 diabetes and multiple sclerosis. The synthesis of a small library of cell-permeable β7 integrin inhibitors based on the peptide biotin-R8ERY is reported, in which the tyrosine residue has been modified by using the Suzuki-Miyaura cross-coupling reaction. The synthesised peptidomimetics were evaluated in a cell adhesion assay and shown to inhibit Mn2+-activated adhesion of mouse TK-1 T cells to mouse MAdCAM-1. All of the synthesised peptidomimetics are more active than our previously reported lead compound biotin-R8ERY with two of the analogues, 6 and 7, exhibiting IC50 values of 15 μM.

ANTIMICROBIAL COMPOUNDS

The present invention relates to a compound of formula (I) AA-AA-AA-R1—R2 (I) wherein, in any order, 2 of said AA (amino acid) moieties are cationic amino acids and 1 of said AA is an amino acid with a lipophilic R group, the R group having 14-27 non-hydrogen atoms; R1 is a N atom, which may be substituted by a branched or unbranched C1-C10 alkyl or aryl group, which group may incorporate up to 2 heteroatoms selected from N, O and S; and R2 is an aliphatic moiety having 2-20 non-hydrogen atoms, said moiety being linear, branched or cyclic. The invention further relates to formulations containing these compounds, solid supports having these compounds attached thereto, the use of these compounds in therapy, particularly as antimicrobial, anti-tumour or anti-biofilm agents and non-therapeutic uses of these compounds, particularly their use in inhibiting biofilm formation or removing a biofilm.

TREATMENT OF BIOFILMS

The present invention relates to a peptide or peptidomimetic for use in the treatment of a biofilm-associated infection in a subject, wherein said peptide or peptidomimetic a) carries a net positive charge, b) is 1 to 6 amino acids in length or is an equivalently sized peptidomimetic; and c) is amphipathic in nature, having one or more lipophilic groups, one of said lipophilic groups comprising at least 7 non-hydrogen atoms.