3 siyaabood oo xiiso leh oo farmashiyeyaashu u dhiseen iskudhis sanadkan
by Bethany Halford
EZYMES HORKACAY OO LAGU DHISAY BAANDHAHA BIARYL
Qorshaha muujinaya isku xidhka biaryl-katalyzed ee enzyme-ka.
Chemists-ku waxay isticmaalaan molecules biaryl, kuwaas oo ka kooban kooxaha aryl ee midba midka kale ku xiran yahay hal bond, sida ligands chiral, qalabka dhismaha, iyo daawooyinka.Laakin samaynta motif biaryl leh falcelin bir-catalyzed, sida Suzuki iyo Negishi isku-tallaabta-isku-xidhka, sida caadiga ah waxay u baahan tahay dhowr tillaabo oo isku-dhafan si loo sameeyo lammaaneyaasha isku-xidhka.Waxa intaa ka sii badan, fal-celinta birta-catalyzed-ku waa ay daciiftaa marka la samaynayo biaryls-ka weyn.Waxaa dhiirigeliyay awoodda ensaymes 'si ay u kiciyaan falcelinta, koox ay hogaamiso Jaamacadda Michigan's Alison RH Narayan waxay adeegsatay horumar toos ah si ay u abuurto cytochrome P450 enzyme kaas oo dhisa molecule biaryl ah iyada oo loo marayo isku dhafka oksaydhka ee curaarta carbon-hydrogen.Insaymku wuxuu guursadaa unugyo caraf udgoon si uu u abuuro hal isteeroisomer oo ku wareegsan dammaanad wareeg ah oo xanniban (muujin).Cilmi-baadhayaashu waxay u maleynayaan in habkan biocatalytic uu noqon karo isbeddel rooti iyo subag ah oo loogu talagalay samaynta curaarta biaryl (Nature 2022, DOI: 10.1038 / s41586-021-04365-7).
RECIPE LOOGU TALAGALAY AMINES SADDEXAAD WAXAY KU TIIRSATAY IN YAR OO milix ah
Nidaamku waxa uu muujinayaa falcelin ka samaynaysa aminyada jaamacadeed kuwa sare.
Isku darka biraha gaajaysan ee elektarooniga ah iyo aminyada elektarooniga ah ee hodanka ku ah ayaa sida caadiga ah dila kiciyayaasha, sidaa awgeed reagents biraha looma isticmaali karo in lagu dhiso aminyada sare ee aminyada sare.M. Christina White iyo asxaabtiisa Jaamacadda Illinois Urbana-Champaign waxay garwaaqsadeen inay ka bixi karaan dhibaatadan haddii ay ku daraan xoogaa cusbo leh cunto karintooda.Iyaga oo u beddelaya aminyada sare ee cusbada ammonium, farmashiyeyaashu waxay ogaadeen inay ka falcelin karaan xeryahooda olefins terminal, oksaydhant, iyo kicinta palladium sulfoxide si ay u abuuraan aminiin jaamacadeed aan tiro badan lahayn oo leh kooxo kala duwan oo shaqeynaya (tusaale la muujiyay).Farmashiyeyaashu waxay isticmaaleen falcelinta si ay u sameeyaan dawooyinka dhimirka ka hortagga Abilify iyo Semap iyo inay u beddelaan dawooyinka jira ee amines sare ah, sida Prozac antidepressant, amines jaamacadeed, iyagoo muujinaya sida farmashiyayaashu ay dawooyin cusub uga samayn karaan kuwa jira (Sayniska 2022, DOI: 10.1126/sayniska.abn8382).
AZAARENES OO LAGU QABTAY QANDARAAS KAAROON
Nidaamku wuxuu muujinayaa quinoline N-oxide oo isu beddelay N-acylindole.
Sanadkan khubarada farmasiyadu waxay ku biiriyeen tafatirka molecular, kuwaas oo ah falcelino isbedel ku sameeya xudunta molecules-ka adag.Hal tusaale, cilmi-baarayaashu waxay sameeyeen isbeddel isticmaalaya iftiinka iyo aashitada si ay u gooyaan hal kaarboon oo ka mid ah azaarenes lix ka kooban oo ku jira quinoline N-oxides si ay u sameeyaan N-acylindoles oo leh siddo shan xubnood ah (tusaale la muujiyay).Dareen-celinta, oo ay sameeyeen farmashiyaal ka tirsan kooxda Mark D. Levin ee Jaamacadda Chicago, waxay ku salaysan tahay fal-celin ku lug leh laambad meerkuri, kaas oo damiya mowjadaha iftiinka ee badan.Levin iyo asxaabtiisuba waxay ogaadeen in isticmaalka diode iftiin-bixiya oo iftiimiya iftiinka 390 nm ay siisay koontarool wanaagsan waxayna u oggolaadeen inay sameeyaan falcelinta guud ee quinoline N-oxides.Dareen-celinta cusubi waxay siinaysaa kuwa sameeya molecule hab ay dib ugu habeeyaan xudunta isku dhafka isku dhafan waxayna ka caawin kartaa farmashiyeyaasha daawada ee raadinaya inay ballaariyaan maktabadahooda musharixiinta daroogada (Sayniska 2022, DOI: 10.1126/science.abo4282).
Waqtiga boostada: Dec-19-2022