- Novel bivalent ligands carrying potential antinociceptive effects by targeting putative mu opioid receptor and chemokine receptor CXCR4 heterodimers
-
The functional interactions between opioid and chemokine receptors have been implicated in the pathological process of chronic pain. Mounting studies have indicated the possibility that a MOR-CXCR4 heterodimer may be involved in nociception and related ph
- Li, Mengchu,Ma, Hongguang,Nassehi, Nima,Pagare, Piyusha P.,Santos, Edna J.,Selley, Dana E.,Stevens Negus, S.,Wang, Huiqun,Zhang, Yan
-
-
- TRIPODAL SQUARAMIDE-BASED MONOMERS
-
The present invention relates to a tripodal squaramide-based monomer based monomer according to formula (I) for the formation of supramolecular polymers: wherein T represents a central atom; n is an integer of from 4 to 12; and R1 is a group ac
- -
-
Page/Page column 23; 24
(2019/09/04)
-
- Solid-Phase-Based Synthesis of Ureidopyrimidinone-Peptide Conjugates for Supramolecular Biomaterials
-
Supramolecular polymers have shown to be powerful scaffolds for tissue engineering applications. Supramolecular biomaterials functionalized with ureidopyrimidinone (UPy) moieties, which dimerize via quadruple hydrogen-bond formation, are eminently suitable for this purpose. The conjugation of the UPy moiety to biologically active peptides ensures adequate integration into the supramolecular UPy polymer matrix. The structural complexity of UPy-peptide conjugates makes their synthesis challenging and until recently low yielding, thus restricted the access to structurally diverse derivatives. Here we report optimization studies of a convergent solid-phase based synthesis of UPy-modified peptides. The peptide moiety is synthesized using standard Fmoc solid-phase synthesis and the UPy fragment is introduced on the solid-phase simplifying the synthesis and purification of the final UPy-peptide conjugate. The convergent nature of the synthesis reduces the number of synthetic steps in the longest linear sequence compared to other synthetic approaches. We demonstrate the utility of the optimized route by synthesizing a diverse range of biologically active UPy-peptide bioconjugates in multimilligram scale for diverse biomaterial applications. 1 Introduction 2 Divergent Synthesis 3 Convergent Synthesis 4 UPy-Amine Strategy 5 UPy-Carboxylic Acid Strategy 6 Conclusion.
- De Feijter, Isja,Goor, Olga J. G. M.,Hendrikse, Simone I. S.,Comellas-Aragonès, Marta,S?ntjens, Serge H. M.,Zaccaria, Sabrina,Fransen, Peter P. K. H.,Peeters, Joris W.,Milroy, Lech-Gustav,Dankers, Patricia Y. W.
-
supporting information
p. 2707 - 2713
(2015/11/27)
-
- Ligand-directed selective protein modification based on local single-electron-transfer catalysis
-
A photocatalyst ([Ru(bpy)3]2+) bound to a protein ligand was essential for the title method. Local single-electron transfer from the catalyst resulted in the formation of tyrosyl radicals. N′-Acetyl-N,N- dimethyl-1,4-phenylenediamine was used as the tyrosyl radical trapping agent and used in a radical addition to afford selective modification of the target protein. Copyright
- Sato, Shinichi,Nakamura, Hiroyuki
-
supporting information
p. 8681 - 8684
(2013/09/12)
-
- Synthesis and characterization of well-defined l-lactic acid-caprolactone co-oligomers and their rhenium (I) and technetium(I) conjugates
-
Staring from l-lactide and ε-caprolactone, the corresponding lactic-caprolactone cooligomer with hydroxyl and carboxylic acid groups were synthesized. These oligomers were connected with chelating groups through a long chain tether, ready for transition metal binding. Coordination of organometallic rhenium(I) and technetium(I) complexes generated the conjugates in high yield and short time, satisfying the requirements for short-lived radiopharmaceuticals in clinical applications. A reasonable pharmacophore model has been established to guide the design of well-defined lactic acid oligomer for nuclear medicine.
- Zhu, Hua,Yang, Zhi,Li, Nan,Wang, Xue-Juan,Wang, Feng,Su, Hua,Xie, Qing,Zhang, Yan,Ma, Yun-Xia,Lin, Bao-He
-
-
- Role of the guanidine group in the N-terminal fragment of PTH(1-11)
-
A series of PTH hybrids containing a diamine [NH2(CH 2) n NH2; n = 4, 5, 6] in the C-terminal position was synthesized based on the H-Aib-Val-Aib-Glu-Ile-Gln-Leu-Nle-His-Gln- Har-NH2 (Har = homoargini
- Caporale, Andrea,Woznica, Iwona,Schievano, Elisabetta,Mammi, Stefano,Peggion, Evaristo
-
experimental part
p. 1269 - 1275
(2010/07/16)
-
- ORGANIC COMPOUNDS USEFUL FOR THE TREATMENT OF NEURODEGENERATIVE DISEASES, USES AND METHODS FOR THE PREPARATION THEREOF
-
Compounds having a general formula (I) are used for the treatment of neurodegenerative diseases, wherein at least one of R1 ed R8 is chosen from the group consisting of (II), (III), (V), (VI), (XVII).
- -
-
Page/Page column 22-23
(2009/04/25)
-
- 2, 5-Bis-Diamine [1,4] Benzoquinone-Derivatives
-
Synthesis of 2,5-bis-diamine-[1,4]benzoquinonic derivatives having the general formula (I), products and intermediates of said synthesis; the synthesis involves the use of p-benzoquinones having the general formula (IX) and diamines having the general for
- -
-
Page/Page column 9
(2009/04/24)
-
- Selective synthesis of carbamate protected polyamines using alkyl phenyl carbonates
-
Utilising alkyl phenyl carbonates, an economical, practical and versatile method for selective Boc, Cbz and Alloc protection of polyamines has been developed. This method allows Boc, Cbz and Alloc protection of primary amines in the presence of secondary amines by reaction of the polyamines with the alkyl phenyl carbonates. Also, this method allows mono carbamate protection of simple symmetrical aliphatic α,ω-alkanediamines in high yields with respect to the diamine. Finally, the method allows selective carbamate protection of a primary amine located on a primary carbon in the presence of a primary amine located on a secondary or a tertiary carbon in excellent yields.
- Pittelkow, Michael,Lewinsky, Rasmus,Christensen, Jorn Bolstad
-
p. 2195 - 2202
(2007/10/03)
-
- PROCESS FOR PREPARING SYNTHETIC MATRIX METALLOPROTEASE INHIBITORS
-
Synthetic mammalian matrix metalloprotease inhibitors are disclosed that are useful for treating or preventing diseases wherein said diseases are caused by unwanted mammalian matrix metalloprotease activity and include skin disorders, keratoconus, restenosis, rheumatoid arthritis, wounds, cancer, angiogenesis and shock.
- -
-
-
- MATRIX METALLOPROTEASE INHIBITORS
-
Compounds of the formulas STR1 wherein each R 1 is independently H or alkyl (1-8C) and R 2 is alkyl (1-8C) or wherein the proximal R 1 and R 2 taken together are--(CH 2) p--wherein p=3-5;R 3 is H or alkyl (1-4C);R 4 is fused or conjugated unsubstituted or substituted bicycloaryl methylene;n is 0, 1 or 2; m is 0 or 1; andX is OR 5 or NHR 5, wherein R. sup.5 is H or substituted or unsubstituted alkyl (1-12C), aryl (6-12C), aryl alkyl (6-16C); orX is an amino acid residue or amide thereof; orX is the residue of a cyclic amine or heterocyclic amine;wherein R 6 is H or lower alkyl (1-4C) and R 7 is H, lower alkyl (1-4C) or an acyl group, and wherein--CONR 3--is optionally in modified isosteric form are useful for treating conditions which are characterized by unwanted matrix metalloprotease activities.
- -
-
-
- MATRIX METALLOPROTEASE INHIBITORS
-
Compounds of the formulas STR1 wherein each R 1 is independently H or alkyl (1-8C) and R 2 is alkyl (1-8C) or wherein the proximal R 1 and R 2 taken together are--(CH 2) p--wherein p=3-5;R 3 is H or alkyl (1-4C);R. sup.4 is fused or conjugated unsubstituted or substituted bicycloaryl methylene;n is 0, 1 or 2; m is 0 or 1; andx is OR 5 or NHR 5, wherein R. sup.5 is H or substituted or unsubstituted alkyl (1-12C), aryl (6-12C), aryl alkyl (6-16C); orX is an amino acid residue or amide thereof; orX is the residue of a cyclic amine or heterocyclic amine;Y is selected from the group consisting of R 7 ONR 6 CONR 6-, R 6 2 NCONOR 7-, and R 6 CONOR. sup.7-, wherein each R 6 is independently H or lower alkyl (1-4C); R 7 is lower alkyl (1-4C) or an acyl group; andwherein--CONR. sup.3--is optionally in modified isoteric form are inhibitors of matrix metalloproteases.
- -
-
-
- INHIBITION OF ANGIOGENESIS BY SYNTHETIC MATRIX METALLOPROTEASE INHIBITORS
-
Synthetic mammalian matrix metalloprotease inhibitors are useful in controlling angiogenesis. These compounds are thus useful in controlling the growth of tumors and in controlling neovascular glaucomas.
- -
-
-
- Treatment for tissue ulceration
-
Compounds of the formulas STR1 wherein R1 is H and R2 is alkyl (3-8C) or wherein R1 and R2 taken together are --(CH2)n -- wherein n=3-5; R3 is H or alkyl (1-4C); R4 is a substituted or unsubstituted fused or conjugated bicycloaryl methylene; X is OR5 or NHR5, wherein R5 is H or substituted or unsubstituted alkyl (1-12C), aryl (6-12C), aryl alkyl (6-16C); or X is an amino acid residue or amide thereof; or X is the residue of a cyclic amine or heterocyclic amine are useful for treating or preventing ulceration of tissue, especially cornea.
- -
-
-
