Chemo-enzymatic cascade processes are invaluable due to their ability to rapidly construct high-value products from available feedstock chemicals in a one-pot relay manner. Application In Synthesis of Benzo[b]thiophene-4-carboxylic acid, In an article, mentioned the application of 10134-95-9, Name is Benzo[b]thiophene-4-carboxylic acid, molecular formula is C9H6O2S
Application of Bivalent Bioisostere Concept on Design and Discovery of Potent Opioid Receptor Modulators
Here, we described the structural modification of previously identified mu opioid receptor (MOR) antagonist NAN, a 6alpha-N-7?-indolyl substituted naltrexamine derivative, and its 6beta-N-2?-indolyl substituted analogue INTA by adopting the concept of “bivalent bioisostere”. Three newly prepared opioid ligands, 25 (NBF), 31, and 38, were identified as potent MOR antagonists both in vitro and in vivo. Moreover, these three compounds significantly antagonized DAMGO-induced intracellular calcium flux and displayed varying degrees of inhibition on cAMP production. Furthermore, NBF produced much less significant withdrawal effects than naloxone in morphine-pelleted mice. Molecular modeling studies revealed that these bivalent bioisosteres may adopt similar binding modes in the MOR and the “address” portions of them may have negative or positive allosteric modulation effects on the function of their “message” portions compared with NAN and INTA. Collectively, our successful application of the “bivalent bioisostere concept” identified a promising lead to develop novel therapeutic agents toward opioid use disorder treatments.
We’ll also look at important developments in the pharmaceutical industry because understanding organic chemistry is important in understanding health, medicine, the role of 10134-95-9, and how the biochemistry of the body works.Application In Synthesis of Benzo[b]thiophene-4-carboxylic acid
Reference：
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem