When developing chemical systems it’s of course important to gain a deep understanding of the chemical reaction process. In an article, author is Chen, Yan, once mentioned the application of 2579-22-8, Name is 3-Phenylpropiolaldehyde, molecular formula is C9H6O, molecular weight is 130.14, MDL number is MFCD00006995, category is thiomorpholine. Now introduce a scientific discovery about this category, Application of 2579-22-8.
The design and synthesis of a series of C28 amine-based betulinic acid derivatives as HIV-1 maturation inhibitors is described. This series represents a continuation of efforts following on from previous studies of C-3 benzoic acid-substituted betulinic acid derivatives as HIV-1 maturation inhibitors (MIs) that were explored in the context of C-28 amide substituents. Compared to the C-28 amide series, the C-28 amine derivatives exhibited further improvements in HIV-1 inhibitory activity toward polymorphisms in the Gag polyprotein as well as improved activity in the presence of human serum. However, plasma exposure of basic amines following oral administration to rats was generally low, leading to a focus on moderating the basicity of the amine moiety distal from the triterpene core. The thiomorpholine dioxide (TMD) 20 emerged from this study as a compound with the optimal antiviral activity and an acceptable pharmacokinetic profile in the C-28 amine series. Compared to the C-28 amide 3, 20 offers a 2-to 4-fold improvement in potency towards the screening viruses, exhibits low shifts in the EC50 values toward the V370A and Delta V370 viruses in the presence of human serum or human serum albumin, and demonstrates improved potency towards the polymorphic T371A and V362I virus variants. (C) 2018 Elsevier Ltd. All rights reserved.
The design and synthesis of related molecules that are more effective, more selective, and less toxic than aspirin are important objectives of biomedical research. You can also check out more blogs about 2579-22-8. Electric Literature of 2579-22-8.
Reference:
Thiomorpholine – Wikipedia,
,Thiomorpholine | C4H9NS – PubChem