151607-70-4Relevant articles and documents
Method for synthesizing 1 - methyl - 1H -1, 2 and 4 - triazol -3 - methyl formate
-
Paragraph 0034-0036, (2021/11/26)
The invention discloses a synthetic 1 - methyl - 1H -1. The invention discloses a method for 2,4 - triazole -3 - methyl formate and belongs to the technical field of organic synthesis. The reaction of 1,2 and 4 - triazole as a raw material is followed by
PYRIDAZINE DERIVATIVES AS RORC MODULATORS
-
Page/Page column 163, (2018/05/24)
Compounds of formula (I): (I) or pharmaceutical salts thereof, wherein m, n,, p, q A, B, Ri, R2, R3, R4, R5, R6and R7are as defined herein. Also disclosed are methods of making the compounds and using the compounds as RORs modulators for treatment of inflammatory diseases such as arthritis.
Discovery of novel, highly potent, and selective matrix metalloproteinase (MMP)-13 inhibitors with a 1,2,4-triazol-3-yl moiety as a zinc binding group using a structure-based design approach
Nara, Hiroshi,Kaieda, Akira,Sato, Kenjiro,Naito, Takako,Mototani, Hideyuki,Oki, Hideyuki,Yamamoto, Yoshio,Kuno, Haruhiko,Santou, Takashi,Kanzaki, Naoyuki,Terauchi, Jun,Uchikawa, Osamu,Kori, Masakuni
, p. 608 - 626 (2017/02/05)
On the basis of a superposition study of X-ray crystal structures of complexes of quinazoline derivative 1 and triazole derivative 2 with matrix metalloproteinase (MMP)-13 catalytic domain, a novel series of fused pyrimidine compounds which possess a 1,2,4-triazol-3-yl group as a zinc binding group (ZBG) was designed. Among the herein described and evaluated compounds, 31f exhibited excellent potency for MMP-13 (IC50 = 0.036 nM) and selectivities (greater than 1,500-fold) over other MMPs (MMP-1, -2, -3, -7, -8, -9, -10, and -14) and tumor necrosis factor-α converting enzyme (TACE). Furthermore, the inhibitor was shown to protect bovine nasal cartilage explants against degradation induced by interleukin-1 and oncostatin M. In this article, we report the discovery of extremely potent, highly selective, and orally bioavailable fused pyrimidine derivatives that possess a 1,2,4-triazol-3-yl group as a novel ZBG for selective MMP-13 inhibition.