104886-22-8Relevant articles and documents
Nickel-catalyzed removal of alkene protecting group of phenols, alcohols via chain walking process
Meng, Chenkai,Niu, Haolin,Ning, Juehan,Wu, Wengang,Yi, Jun
supporting information, (2020/02/04)
An efficient nickel-catalyzed removal of alkene protection group under mild condition with high functional group tolerance through chain walking process has been established. Not only phenolic ethers, but also alcoholic ethers can be tolerated with the retention of stereocenter adjacent to hydroxyl group. The new reaction brings the homoallyl group into a start of new type of protecting group.
COMPOUNDS AND METHODS FOR TREATING AIDS AND HIV INFECTIONS
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Page/Page column 33, (2010/12/17)
Macrocycle containing carbamate compounds that inhibit HIV proteolytic enzymes and processes for preparing them are described. Compositions and methods for treating a patient infected with HIV are described.
Design, synthesis, protein-ligand X-ray structure, and biological evaluation of a series of novel macrocyclic human immunodeficiency virus-1 protease inhibitors to combat drug resistance
Ghosh, Arun K.,Kulkarni, Sarang,Anderson, David D.,Hong, Lin,Baldridge, Abigail,Wang, Yuan-Fang,Chumanevich, Alexander A.,Kovalevsky, Andrey Y.,Tojo, Yasushi,Amano, Masayuki,Koh, Yasuhiro,Tang, Jordan,Weber, Irene T.,Mitsuya, Hiroaki
experimental part, p. 7689 - 7705 (2010/05/19)
The structure-based design, synthesis, and biological evaluation of a series of nonpeptidic macrocyclic HIV protease inhibitors are described. The inhibitors are designed to effectively fill in the hydrophobic pocket in the S1′ - S2′ subsites and retain all major hydrogen bonding interactions with the protein backbone similar to darunavir (1) or inhibitor 2. The ring size, the effect of methyl substitution, and unsaturation within the macrocyclic ring structure were assessed. In general, cyclic inhibitors were significantly more potent than their acyclic homologues, saturated rings were less active than their unsaturated analogues and a preference for 10- and 13-membered macrocylic rings was revealed. The addition of methyl substituents resulted in a reduction of potency. Both inhibitors 14b and 14c exhibited marked enzyme inhibitory and antiviral activity, and they exerted potent activity against multidrug-resistant HIV-1 variants. Protein - ligand X-ray structures of inhibitors 2 and 14c provided critical molecular insights into the ligand-binding site interactions.
