Njira zitatu zosangalatsa zomwe akatswiri a zamankhwala adapangira mankhwala chaka chino
by Bethany Halford
Ma enzyme osinthika amamanga ma bond a biaryl
Chithunzi chosonyeza kulumikizana kwa biaryl komwe kumayambitsidwa ndi enzyme.
Akatswiri a zamankhwala amagwiritsa ntchito mamolekyu a biaryl, omwe ali ndi magulu a aryl omangiriridwa limodzi ndi mgwirizano umodzi, monga ma chiral ligands, zomangira zinthu, ndi mankhwala. Koma kupanga biaryl motif ndi ma metal-catalyzed reactions, monga Suzuki ndi Negishi cross-couplings, nthawi zambiri kumafuna njira zingapo zopangira kuti apange ma coupling partners. Kuphatikiza apo, ma metal-catalyzed reactions awa amalephera popanga ma biaryl akuluakulu. Motsogozedwa ndi luso la ma enzymes loyambitsa ma reactions, gulu lotsogozedwa ndi Alison RH Narayan wa ku University of Michigan linagwiritsa ntchito directed evolution kuti lipange cytochrome P450 enzyme yomwe imapanga biaryl molecule kudzera mu oxidative coupling ya aromatic carbon-hydrogen bonds. Enzymeyi imagwirizanitsa ma aromatic molecules kuti ipange stereoisomer imodzi mozungulira mgwirizano ndi kuzungulira kolepheretsedwa (komwe kwawonetsedwa). Ofufuzawo akuganiza kuti njira iyi ya biocatalytic ikhoza kukhala kusintha kwa mkate ndi batala popanga ma biaryl bonds (Nature 2022, DOI: 10.1038/s41586-021-04365-7).
CHINSINSI CHA ANTHU AKULUAKULU CHODZEDWA PA MCHUNGU WANG'ONO
Chiwembu chikuwonetsa zomwe zimapangitsa ma amines atatu kuchokera ku achiwiri.
Kusakaniza ma catalyst achitsulo omwe amadya ma elekitironi ndi ma amine olemera ma elekitironi nthawi zambiri kumapha ma catalyst, kotero ma reagents achitsulo sangagwiritsidwe ntchito popanga ma amines atatu kuchokera ku ma amines achiwiri. M. Christina White ndi anzake ku University of Illinois Urbana-Champaign adazindikira kuti atha kuthana ndi vutoli ngati atawonjezera zonunkhira zamchere ku resipi yawo ya reactant. Mwa kusintha ma amines achiwiri kukhala ammonium salts, akatswiri a zamankhwala adapeza kuti amatha kuchita izi ndi ma olefins otsiriza, oxidant, ndi palladium sulfoxide catalyst kuti apange ma amines ambiri achitatu okhala ndi magulu osiyanasiyana ogwira ntchito (chitsanzo chawonetsedwa). Akatswiri a zamankhwala adagwiritsa ntchito reaction kupanga mankhwala oletsa matenda amisala Abilify ndi Semap ndikusintha mankhwala omwe alipo omwe ndi ma amines achiwiri, monga antidepressant Prozac, kukhala ma amines atatu, kuwonetsa momwe akatswiri a zamankhwala angapangire mankhwala atsopano kuchokera ku omwe alipo (Science 2022, DOI: 10.1126/science.abn8382).
AZAARENES ANAPEZEKA KUPEZEKA KWA KHABONI
Chithunzichi chikuwonetsa quinoline N-oxide yomwe yasinthidwa kukhala N-acylindole.
Chaka chino akatswiri a zamankhwala adawonjezera ku mndandanda wa kusintha kwa mamolekyulu, zomwe ndi zochita zomwe zimasintha ma cores a mamolekyulu ovuta. Mu chitsanzo chimodzi, ofufuza adapanga kusintha komwe kumagwiritsa ntchito kuwala ndi asidi kudula kaboni imodzi kuchokera ku azaarenes okhala ndi ziwalo zisanu ndi chimodzi mu quinoline N-oxides kuti apange N-acylíndoles yokhala ndi mphete zokhala ndi ziwalo zisanu (chitsanzo chawonetsedwa). Kuchitapo kanthu, komwe kunapangidwa ndi akatswiri a zamankhwala mu gulu la Mark D. Levin ku University of Chicago, kumachokera ku kuchitapo kanthu komwe kunaphatikizapo nyali ya mercury, yomwe imayatsa mafunde angapo a kuwala. Levin ndi anzake adapeza kuti kugwiritsa ntchito diode yotulutsa kuwala yomwe imatulutsa kuwala pa 390 nm kunawapatsa ulamuliro wabwino ndipo kunawalola kupanga kuchitapo kanthu konse kwa quinoline N-oxides. Kuchitapo kanthu kwatsopano kumeneku kumapatsa opanga mamolekyu njira yokonzanso ma cores a ma compounds ovuta ndipo kungathandize akatswiri azamankhwala omwe akufuna kukulitsa malaibulale awo a mankhwala omwe akufuna kugwiritsa ntchito (Science 2022, DOI: 10.1126/science.abo4282).
Nthawi yotumizira: Disembala-19-2022