3 siyaabood oo xiiso leh oo ay farmashiistayaashu sanadkan u dhiseen iskudhisyo
by Bethany Halford
BANDHIGADA BIARYL EE LA DHISAY EE ENZYMES EE LA KORDHIYEY
Qorshaha oo muujinaya isku xidhka biaryl ee ensaym-ka kiciya.
Kiimikeeyayaashu waxay isticmaalaan molecules-ka biaryl, kuwaas oo ka kooban kooxo aryl ah oo isku xiran hal xidhmo, sida ligands chiral, baloogyada dhismaha walxaha, iyo daawooyinka. Laakiin sameynta qaabka biaryl oo leh falcelinta biraha lagu kiciyay, sida Suzuki iyo Negishi isku-xidhka, waxay caadi ahaan u baahan tahay dhowr tallaabo oo isku-dhafan si loo sameeyo lammaanayaasha isku-xidhka. Intaa waxaa dheer, falcelintan biraha lagu kiciyay way burburaan marka la samaynayo biaryls waaweyn. Iyada oo lagu dhiirigelinayo awoodda enzymes-ka ee ay ku kicin karaan falcelinta, koox ay hoggaaminayso Alison RH Narayan oo ka tirsan Jaamacadda Michigan ayaa isticmaashay horumar toos ah si loo abuuro enzyme cytochrome P450 ah oo dhisa molecule biaryl iyada oo loo marayo isku-xidhka oksaydhka ee isku-xidhka kaarboon-haydrogen-ka udgoonka leh. Ensaymku wuxuu isku daraa molecules-ka udgoonka leh si uu u abuuro hal stereoisomer oo ku wareegsan isku-xidhka oo leh wareeg caqabad leh (la tusay). Cilmi-baarayaashu waxay u maleynayaan in habkan bayoolojiga ah uu noqon karo isbeddel rooti-iyo-subag ah oo lagu sameeyo xidhmooyinka biaryl (Nature 2022, DOI: 10.1038/s41586-021-04365-7).
CUNTADA CUNTADA EE AMINE-KA SADEXAAD EE KU TALAGALAY CUSBO YAR
Qorshuhu wuxuu muujinayaa falcelin ka sameysan amiinada saddexaad kuwa labaad.
Isku darka kaaliyayaasha birta ee elektaroonigga u baahan iyo amiinada hodanka ku ah elektaroonigga ayaa badanaa dila kaaliyayaasha, sidaa darteed reagents-ka birta looma isticmaali karo in lagu dhiso amiinada saddexaad ee ka yimaada amiinada labaad. M. Christina White iyo asxaabteeda Jaamacadda Illinois Urbana-Champaign waxay ogaadeen inay ka gudbi karaan dhibaatadan haddii ay ku daraan xawaash milix leh cuntooyinkooda falgalka. Iyagoo amines-ka labaad u beddelaya cusbo amooniyam, farmashiyeyaashu waxay ogaadeen inay ka falcelin karaan isku-dhafkan iyagoo adeegsanaya olefins-ka terminal, oksaydh, iyo kaaliyayaasha palladium sulfoxide si ay u abuuraan amiinada saddexaad ee tiro badan oo leh kooxo shaqo oo kala duwan (tusaale la muujiyay). Farmashiyeyaashu waxay isticmaaleen falcelinta si ay u sameeyaan daawooyinka dhimirka Abilify iyo Semap iyo inay u beddelaan daawooyinka jira ee ah amiinada labaad, sida Prozac ee niyad-jabka, amiinada saddexaad, iyagoo muujinaya sida kiimikadu uga samayn karaan daawooyin cusub kuwa jira (Science 2022, DOI: 10.1126/science.abn8382).
AZAARENES waxay qaadatay qandaraas kaarboon ah
Qorshuhu wuxuu muujinayaa quinoline N-oxide oo isu beddelay N-acylindole.
Sannadkan kiimikooyinku waxay ku dareen dib-u-habaynta tafatirka molecular-ka, kuwaas oo ah falcelinno isbeddel ku sameeya xudunta molecules-ka adag. Hal tusaale, cilmi-baarayaashu waxay sameeyeen isbeddel adeegsanaya iftiin iyo aashito si ay u soo saaraan hal kaarboon oo ka mid ah lix xubnood oo azaarenes ah oo ku jira quinoline N-oxides si ay u sameeyaan N-cylindoles oo leh shan xubnood oo giraangirood ah (tusaale la muujiyay). Falcelinta, oo ay sameeyeen kiimikooyin kooxda Mark D. Levin ee Jaamacadda Chicago, waxay ku salaysan tahay falgal ku lug leh laambad meerkuri ah, taas oo soo saarta hirar badan oo iftiin ah. Levin iyo asxaabtiisu waxay ogaadeen in isticmaalka diode iftiin soo saaraya oo iftiin ku bixiya 390 nm uu siiyay xakameyn wanaagsan oo u oggolaaday inay falcelinta guud ka dhigaan kuwa quinoline N-oxides. Falcelinta cusub waxay siinaysaa sameeyayaasha molecule-ka hab ay dib ugu habeeyaan xudunta isku-dhafka adag waxayna ka caawin kartaa kiimikooyinka daawada ee raadinaya inay ballaariyaan maktabadahooda musharaxiinta daroogada (Sayniska 2022, DOI: 10.1126/science.abo4282).
Waqtiga boostada: Diseembar-19-2022