90508-20-6Relevant articles and documents
CALPAIN MODULATORS AND THERAPEUTIC USES THEREOF BACKGROUND
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Paragraph 0259, (2019/11/28)
Disclosed herein are small molecule calpain modulators, pharmaceutical compositions, preparation methods and their use as therapeutic agents. The therapeutic agents can be used for treating fibrotic disease or a resulting secondary disease state or condition. The small molecules can inhibit calpain through contact with CAPN1, CAPN2, and/or CAPN9 enzymes.
A mild copper catalyzed method for the selective deprotection of aryl allyl ethers
Hemming, David S.,Talbot, Eric P.,Steel, Patrick G.
supporting information, p. 17 - 20 (2016/12/23)
Copper boryl reagents enable the selective cleavage of aryl allyl ethers to the corresponding phenols in good to moderate yields.
Rational conversion of noncontinuous active region in proteins into a small orally bioavailable macrocyclic drug-like molecule: The HIV-1 CD4:gp120 paradigm
Hurevich, Mattan,Swed, Avi,Joubran, Salim,Cohen, Shira,Freeman, Noam S.,Britan-Rosich, Elena,Briant-Longuet, Laurence,Bardy, Martine,Devaux, Christian,Kotler, Moshe,Hoffman, Amnon,Gilon, Chaim
supporting information; experimental part, p. 5754 - 5761 (2010/10/01)
Rational conversion of noncontinuous active regions of proteins into a small orally bioavailable molecule is crucial for the discovery of new drugs based on inhibition of protein-protein interactions. We developed a method that utilizes backbone cyclization as an intermediate step for conversion of the CD4 noncontinuous active region into small macrocyclic molecules. We demonstrate that this method is feasible by preparing small inhibitor for human immunodeficiency virus infection. The lead compound, CG-1, proved orally available in the rat model.