23234-32-4

Upstream product

• 3978-80-1 Boc-Tyr-OH 
• 7733-20-2 Boc-L-Tyr-Gly-OMe 
• 100-39-0 benzyl bromide 

Downstream Products

• 143799-85-3 (S)-2-((S)-O-benzyl-N-tert-butoxycarbonyltyrosylamino)ethanol 
• 143799-94-4 (S)-2-((S)-O-benzyl-N-tert-butoxycarbonyltyrosylamino)ethyl ethanethioate 
• 143799-89-7 (S)-1-bromo-2-((S)-O-benzyl-N-tert-butoxycarbonyltyrosylamino)ethane 
• 116394-11-7 L-tyrosyltaurine 
• 41296-45-1 N-Boc-Tyr(Bn)-Gly-OH 

Relevant academic research and scientific papers

Structure-Activity Relationships of cyclo(l -Tyrosyl- l -tyrosine) Derivatives Binding to Mycobacterium tuberculosis CYP121: Iodinated Analogues Promote Shift to High-Spin Adduct

A series of analogues of cyclo(l-tyrosyl-l-tyrosine), the substrate of the Mycobacterium tuberculosis enzyme CYP121, have been synthesized and analyzed by UV-vis and electron paramagnetic resonance spectroscopy and by X-ray crystallography. The introduction of iodine substituents onto cyclo(l-tyrosyl-l-tyrosine) results in sub-μM binding affinity for the CYP121 enzyme and a complete shift to the high-spin state of the heme FeIII. The introduction of halogens that are able to interact with heme groups is thus a feasible approach to the development of next-generation, tight binding inhibitors of the CYP121 enzyme, in the search for novel antitubercular compounds.

COMPOUNDS USEFUL AS MODULATORS OF THE PROTEASOME ACTIVITY

The present invention relates to the use of compounds of the following general formula (I): wherein no is 0 or 1, and when no is 1, X = CH2 or X = NCH2C6H5; R1 is OH, or a OR10 group, or a group of formula NH-(CH2)n1-R11; R2 is H, or an alkyl group, or a group of formula (CH2)n2-(CO)n3-NR13R14; R3 is H, or an alkyl group; R4 is H, or Boc, or Z; R5 is H, or Boc, or Z ; R6 is a OR16 group; R7 and R8 are H, or a halogen atom, as modulators of the proteasome activity, in the frame of the preparation of a medicament useful for the prevention or treatment of diseases wherein the proteasome is involved, or the preparation of cosmetic compositions, or of phytosanitary compositions.

Structural biochemistry XIII: Synthesis of luteinizing hormone-releasing hormone modification [Trp8]-LH-RH

A fragment condensation method was utilized for synthesis of the Trp8-substituted luteinizing hormone-releasing hormone (LHRH). tert-Butoxycarbonyl protection was employed for the α-amino positions, and benzyl protection was used for the phenol group of Tyr and the imidazole nitrogen of His. Peptide bond-forming reactions were performed using N-hydroxysuccinimide (for Trp), dicyclohexylcarbodiimide-1-hydroxybenzotriazole, 1-ethyl-3-(3'-dimethylaminopropyl)-carbodiimide hydrochloride, or mixed carbonic anhydride methods. Biological evaluation of [Trp8]-LH-RH indicated no luteinizing hormone-releasing activity or inhibition of luteinizing hormone release over the dose ranges studied.