352204-70-7Relevant academic research and scientific papers
Design, synthesis and biological evaluation of biphenylglyoxamide-based small molecular antimicrobial peptide mimics as antibacterial agents
Yu, Tsz Tin,Kuppusamy, Rajesh,Yasir, Muhammad,Hassan, Md. Musfizur,Alghalayini, Amani,Gadde, Satyanarayana,Deplazes, Evelyne,Cranfield, Charles,Willcox, Mark D. P.,Black, David Stc,Kumar, Naresh
, p. 1 - 38 (2020)
There has been an increasing interest in the development of antimicrobial peptides (AMPs) and their synthetic mimics as a novel class of antibiotics to overcome the rapid emergence of antibiotic resistance. Recently, phenylglyoxamide-based small molecular
Fragment-Based Discovery of 5-Arylisatin-Based Inhibitors of Matrix Metalloproteinases 2 and 13
Agamennone, Mariangela,Belov, Dmitry S.,Laghezza, Antonio,Ivanov, Vladimir N.,Novoselov, Anton M.,Andreev, Ivan A.,Ratmanova, Nina K.,Altieri, Andrea,Tortorella, Paolo,Kurkin, Alexander V.
supporting information, p. 1892 - 1898 (2016/10/06)
Matrix metalloproteinases (MMPs) are well-established targets for several pathologies. In particular, MMP-2 and MMP-13 play a prominent role in cancer progression. In this study, a structure-based screening campaign was applied to prioritize metalloproteinase-oriented fragments. This computational model was applied to a representative fragment set from the publically available EDASA Scientific compound library. These fragments were prioritized, and the top-ranking hits were tested in a biological assay to validate the model. Two scaffolds showed consistent activity in the assay, and the isatin-based compounds were the most interesting. These latter fragments have significant potential as tools for the design and realization of novel MMP inhibitors. In addition to their micromolar activity, the chemical synthesis affords flexible and creative access to their analogues.
