118001-72-2Relevant academic research and scientific papers
Inhibitors of matrix metalloproteinases
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Page/Page column 14; 15, (2016/11/24)
Compounds of general formula (I), salts or solvates thereof and pharmaceutical compositions containing same: wherein Z is N or CH or the Z(R1) part is replaced with a covalent bond, m and n is 0, 1, 2 or 3; HET is heteroaryl; X is CF3, halogen, CO-heterocyclyl, COOR3 or CONHR3; R1 is H, (CH2)o-aryl, (CH2)p-heteroaryl, (CH2)q-biphenyl; C(O)—R5; S(O)2—R6; R2 is H, aryl, heteroaryl, Y—(CH2)r-aryl, Y—(CH2)s-heteroaryl, where some of the above substituents may be substituted; Y is O or S; with the exclusion of the compound where HET is 1,3-thiazol, X is COOH, R1 is 4-fluorophenyl and R2 is benzyloxy. The invention also relates to the use of a compound of general formula (I), salts or solvates thereof for the use in the prevention or treatment of diseases where the activation of MMPs is involved in the pathomechanism. In this aspect the use of the above excluded compound is also inventive.
Rational design and synthesis of 4-O-substituted phenylmethylenethiosemicarbazones as novel tyrosinase inhibitors
Yi, Wei,Cao, Rihui,Chen, Zhiyong,Yu, Liang,Wen, Huan,Yan, Qin,Ma, Lin,Song, Huacan
scheme or table, p. 752 - 754 (2010/07/15)
In continuing our program aimed to search for tyrosinase inhibitors, a series of novel 4-O-substituted phenylmethylenethiosemicarbazones were rational designed, synthesized and their inhibitory effects on the diphenolase activity of mushroom tyrosinase were also evaluated. A fair number of compounds were found to have significant tyrosinase inhibitiory activity. Particularly, the IC50 values of compounds 3a-g, 3j and 3s were of the same magnitude as tropolone, one of the best tyrosinase inhibitors known so far. Furthermore, the structure-activity relationships of these compounds were also investigated. All these data suggested that these molecules might be utilized for the development of new candidate for the treatment of dermatological disorders, and further development of such compounds may be of interest.
3-Benzyl-1,3-oxazolidin-2-ones as mGluR2 positive allosteric modulators: Hit-to lead and lead optimization
Duplantier, Allen J.,Efremov, Ivan,Candler, John,Doran, Angela C.,Ganong, Alan H.,Haas, Jessica A.,Hanks, Ashley N.,Kraus, Kenneth G.,Lazzaro Jr., John T.,Lu, Jiemin,Maklad, Noha,McCarthy, Sheryl A.,O'Sullivan, Theresa J.,Rogers, Bruce N.,Siuciak, Judith A.,Spracklin, Douglas K.,Zhang, Lei
scheme or table, p. 2524 - 2529 (2010/03/03)
The discovery, synthesis and SAR of a novel series of 3-benzyl-1,3-oxazolidin-2-ones as positive allosteric modulators (PAMs) of mGluR2 is described. Expedient hit-to-lead work on a single HTS hit led to the identification of a ligand-efficient and struct
Pyridine derivatives
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, (2008/06/13)
The invention concerns novel, pharmaceutically useful 1,3-dioxane alkenoic acid derivatives of the formula I containing a pyridyl moiety at position 4 of the dioxane ring and in which the groups at positions 2, 4 and 5 have cis-relative stereochemistry, X is hydrogen, alkoxy or hydroxy, Y is vinylene, n is 1 or 2, A1 is alkylene, the substituents R1 and R2 at position 2 of the dioxane ring have a variety of values defined hereinafter, and R4 is hydroxy, a physiologically acceptable alcohol residue or alkanesulphonamido, and the pharmaceutically acceptable salts thereof. The invention also includes processes for the manufacture and use of the acid derivatives as well as pharmaceutical compositions for therapeutic use in one or more of a variety of diseases such as ischaemic heart disease, cerebrovascular disease, asthmatic disease and/or inflammatory disease.
