On November 1, 2001, Lehmann, Thomas; Fischer, Ruediger; Albers, Markus; Roelle, Thomas; Mueller, Gerhard; Hessler, Gerhard; Tajimi, Masaomi; Ziegelbauer, Karl; Okigami, Hiromi; Bacon, Kevin; Hasegawa, Haruki published a patent.Product Details of 64987-16-2 The title of the patent was Preparation of cyclic carboxylic acid peptides as integrin antagonists. And the patent contained the following:
Peptides R6-X-A-N(R5)CR3R4-Y-DR1R2 [R1 represents a 4-9-membered (un)saturated aromatic cyclic residue which can contain 0-3 heteroatoms N, S or O and may be annulated and/or substituted; R2, R3, R4 and R5 represent H or (un)substituted C1-C10 alkyl, C2-C10 alkenyl or alkynyl, C6 or C10 aryl, C3-C7 cycloalkyl or a 4-9-membered (un)saturated heterocyclic residue containing up to 2 atoms O, N or S; R6 represents Ph or a 5- to 6-membered aromatic heterocyclic residue containing up to 3 atoms O, N and S and which may annulated or substituted; A represents CO, COCO, SO, SO2, PO, PO2, 2- or 4-pyrimidyl, 2-pyridyl, 2- or 4-imidazolyl, 2-benzimidazolyl or certain other rings which may be substituted; X represents CRX-1RX-2 (RX-1 and RX-2 are H, C1-C4 alkyl, C2-C4 alkenyl or alkynyl) or together with R6 forms a 4-7-membered ring, which can include up to 2 heteroatoms, up to two double bonds and be substituted; Y represents a bond, CO, SO, SO2, O, S, CRY-1RY-2 or NRY-3, where RY-1, RY-2 or RY-3 are a bond, H, (un)substituted C1-C4 alkyl, C2-C4 alkenyl or alkynyl] and their pharmaceutically acceptable salts were prepared for the treatment of inflammatory diseases. Thus, 2-MeC6H4NHCONH-p-C6H4CH2CO-L-Leu-NHC6H4CO2H-m was prepared and showed IC50 ≤ 0.5 μM in the Jurkat VCAM-1 assay. The experimental process involved the reaction of Methyl 2-(2-aminothiazol-4-yl)acetate(cas: 64987-16-2).Product Details of 64987-16-2
The Article related to cyclic carboxylic acid peptide preparation integrin antagonist inflammation inhibitor, Amino Acids, Peptides, and Proteins: Poly(Amino Acids) and Peptides and other aspects.Product Details of 64987-16-2
Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica