78020-52-7

Upstream product

• 6974-29-4 N-(2-hydroxyethyl)-2,2,2-trifluoroacetamide 
• 7693-46-1 4-Nitrophenyl chloroformate 

Downstream Products

• 1066867-14-8 C₂₇H₃₃F₃N₄O₆S₂ 
• 1066865-96-0 C₂₇H₃₆F₃N₃O₇S 
• 1066866-84-9 2-(2,2,2-trifluoroacetamido)ethyl ((2S,3R)-3-hydroxy-4-(N-((S)-2-methylbutyl)benzo[d]thiazole-6-sulfonamido)-1-phenylbutan-2-yl)carbamate 
• 1066865-66-4 2-(2,2,2-trifluoroacetamido)ethyl ((2S,3R)-3-hydroxy-4-(4-methoxy-N-((S)-2-methylbutyl)phenylsulfonamido)-1-phenylbutan-2-yl)carbamate 

Relevant academic research and scientific papers

Design, synthesis, and biological and structural evaluations of novel HIV-1 protease inhibitors to combat drug resistance

A series of new HIV-1 protease inhibitors (PIs) were designed using a general strategy that combines computational structure-based design with substrate-envelope constraints. The PIs incorporate various alcohol-derived P2 carbamates with acyclic and cyclic heteroatomic functionalities into the (R)-hydroxyethylamine isostere. Most of the new PIs show potent binding affinities against wild-type HIV-1 protease and three multidrug resistant (MDR) variants. In particular, inhibitors containing the 2,2-dichloroacetamide, pyrrolidinone, imidazolidinone, and oxazolidinone moieties at P2 are the most potent with Ki values in the picomolar range. Several new PIs exhibit nanomolar antiviral potencies against patient-derived wild-type viruses from HIV-1 clades A, B, and C and two MDR variants. Crystal structure analyses of four potent inhibitors revealed that carbonyl groups of the new P2 moieties promote extensive hydrogen bond interactions with the invariant Asp29 residue of the protease. These structure-activity relationship findings can be utilized to design new PIs with enhanced enzyme inhibitory and antiviral potencies.

Sisomicin derivatives, processes for their production and their medicinal use

The invention relates to sesomycin derivatives of Formula I, infra as well as processes for preparing said sisomycin derivatives. Also included in the invention are compositions containing said sisomycin derivatives and methods for the use of said compoun

Selectively protected 1-N-(ω-aminoalkoxycarbonyl)-sisomicin derivatives

The invention relates to selectively protected 1-N-(ω-aminoalkoxycarbonyl)-sisomicin derivatives and methods for their procurement. Said derivatives are useful as intermediates for the procurement of highly active antibacterial agents of low toxicity.