66895-91-8Relevant academic research and scientific papers
BRIDGED TRICYCLIC CARBAMOYLPYRIDONE COMPOUNDS AND THEIR PHARMACEUTICAL USE
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, (2020/10/20)
Compounds for use in treating or preventing human immunodeficiency virus (HIV) infection are disclosed. The compounds have the following formula (I): including stereoisomers and pharmaceutically acceptable salts thereof, wherein R1, R2, L, W1, W2, X, Y, and Z are as defined herein. Methods associated with the preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.
Progresses in the pursuit of aldose reductase inhibitors: The structure-based lead optimization step
Ramunno, Anna,Cosconati, Sandro,Sartini, Stefania,Maglio, Vita,Angiuoli, Sara,La Pietra, Valeria,Di Maro, Salvatore,Giustiniano, Mariateresa,La Motta, Concettina,Da Settimo, Federico,Marinelli, Luciana,Novellino, Ettore
, p. 216 - 226 (2012/07/16)
Aldose reductase (ALR2) is a crucial enzyme in the development of the major complications of diabetes mellitus. Very recently it has been demonstrated that the ARL2 inhibitor, fidarestat, significantly prevents inflammatory signals (TNF-α, LPS) that cause cancer (colon, breast, prostate and lung), metastasis, asthma, and other inflammatory diseases. Currently, fidarestat is in phase III clinical trial for diabetic neuropathy and was found to be safe. Thus the finding of novel, potent ARL2 inhibitors is today more than in the past in great demand as they can pave the way for a novel therapeutic approach for a number of diseases besides the diabetes. Herein, starting from the virtual screening-derived ALR2 inhibitor S12728 (1), a rational receptor-based lead optimization has been undertaken. The design and synthetic efforts here reported led to the discovery of several new compounds endowed with low micromolar/submicromolar activities.
Solid Phase Synthesis of N-Alkyl Sulfonamides
Dankwardt, Sharon M.,Smith, David B.,Porco Jr., John A.,Nguyen, Cindy H.
, p. 854 - 856 (2007/10/03)
Polymer-supported sulfonamides were alkylated using alkyl halides in the presence of DBU or with alcohols via the Mitsunobu reaction.
