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Nova maniero krei molekulojn por disvolviĝo de drogoj: Noviga procezo donas pli da kontrolo super liberaj radikaluloj

Kemiistoj ĉe The Ohio State University evoluigis novan kaj plibonigitan manieron generi molekulojn kiuj povas ebligi la dezajnon de novaj specoj de sintezaj drogoj.. Researchers say this new method of forming reactive intermediates called ketyl radicals offers scientists a way to use catalysts to convert simple molecules into complex structures in one chemical reaction. This is done in a less harsh, more sustainable and waste-free manner.

“The previous strategy for creating ketyl radicals is about a century old. We have a found a complementary way to access ketyl radicals using LED lights for the synthesis of complex, drug-like molecules,la esploristoj vidas grandan potencialon en ĉi tiu esplorado David Nagib, co-author of the new study and assistant professor of kemio kaj biokemio ĉe Ohio Ŝtato. The study was published Oct. 12 en la revuo Scienco.

David Nagib

David Nagib

The story starts with carbonyls, compounds that function as one of the most common building blocks in creating potential new drugs. Unlike classic carbonyl chemistry taught in introductory organic textbooks, when carbonyls are converted to their “radical” form, they become much more reactive. These radicals, containing an unpaired electron desperately seeking its partner, enable researchers to form new bonds, in order to create complex, drug-like products.

Ĝis nun, ketyl radical formation has required strong, harsh substances called reductants, like sodium or samarium, to act as catalysts. These reductants can be toxic, expensive and incompatible with creating medicines, Nagib said.

En ĉi tiu studo, the researchers found a way to use manganese as a catalyst that could be activated with a simple LED light.

“Manganese is very cheap and abundant, which makes it an excellent catalyst," li diris. “Also, it allows us to access radicals by a complementary atom-transfer mechanism, rather than the classic electron-transfer mechanism.”

Not only is manganese cheaper and more abundant, it actually is more selective in creating products with defined geometries, so they can fit into drug targets, the study found. The process is less wasteful, familio Jugladacoj, recycling the iodine atom used to make the radicals by including it in the more functional products.

This new method to generate ketyl radicals enables researchers to create more versatile and complex structures that could be useful in generating new medicines, Nagib said.


Fonto: news.osu.edu, de Jeff Grabmeier

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