Thiostreptonwaa bakteeriyo dabiici ah oo aad u adag oo loo isticmaalo sidii daawo loogu talagalayantibiyootiga xoolahasidoo kale waxay leedahay firfircooni wanaagsan oo ka hortagga duumada iyo ka hortagga kansarka. Hadda, si buuxda ayaa loogu sameeyay kiimiko.
Thiostrepton, oo markii ugu horreysay laga soocay bakteeriyada sannadkii 1955, waxay leedahay firfircooni antibiyootiko oo aan caadi ahayn: waxay joojisaa biosynthesis-ka borotiinka iyadoo ku xidha ribosomal RNA iyo borotiinnada la xiriira. Dorothy Crowfoot Hodgkin, oo ah sawir-qaade kiristaal ah oo Ingiriis ah iyo ku guuleystay abaalmarinta Nobel Prize 1964, ayaa daahfurtay qaab-dhismeedka sannadkii 1970.
Thiostrepton wuxuu ka kooban yahay 10 giraan, 11 xidhmo peptide ah, aan dheregsanayn oo ballaaran, iyo 17 xarumood oo stereocenter ah. Xitaa ka sii adag ayaa ah xaqiiqda ah inay aad ugu nugul tahay asiidhyada iyo saldhigyada. Waa isku-darka waalidka iyo xubinta ugu adag ee qoyska antibiyootiga thiopeptide.
Hadda isku-dhafkan wuxuu u hoggaansamay hadal macaan oo macmal ah oo ay jeediyeen borofisar kimistar KS Nicolaou iyo asxaabtiisa ka socda Machadka Cilmi-baarista Scripps iyo Jaamacadda California ee San Diego [Angew. Chem. caalami ah. Tifaftirayaasha, 43, 5087 iyo 5092 (2004)].
Christopher J. Moody, oo ah Cilmi-baare Sare oo ka tirsan Waaxda Kimistariga ee Jaamacadda Exeter, UK, ayaa yiri: "Tani waa isku-darka taariikhiga ah iyo guul la taaban karo oo ay gaareen kooxda Nicolaou." doxorubicin D.
Furaha qaab-dhismeedkaTHIOSTREPTONwaa giraanta dehydropiperidine, oo taageerta dabada didehydroalanine iyo laba macrocycles - giraanta thiazoline-ka ah oo 26 xubnood leh iyo nidaamka quinalcolic acid oo 27 xubnood leh. Nicolaou iyo asxaabtiisu waxay sameeyeen giraanta dehydropiperidine ee muhiimka ah iyagoo ka soo bilaabaya agab fudud iyagoo isticmaalaya fal-celinta dimerization iso-Diels-Alder ee biomimetic. Tallaabadan muhiimka ah waxay gacan ka geysatay xaqiijinta soo jeedinta 1978 ee ah in bakteeriyadu ay isticmaasho falcelintan si ay u beddesho antibiyootigyada thiopeptide ee biosynthesize.
Nicolaou iyo asxaabtiisa waxay ku dareen dehydropeperidine macrocycle-ka ku jira thiazoline. Waxay isku dareen macrocycle-kan qaab-dhismeed ka kooban quinalcolic acid iyo horusocod dabada didehydroalanine ah. Kadib waxay nadiifiyeen badeecada si ay u helaan.thiostrepton.
Dib-u-eegayaasha labada warqadood ee kooxda ayaa sheegay in isku-darka "uu yahay farshaxan muujinaya teknoolojiyada casriga ah isla markaana furaya aragtiyo cusub oo loogu talagalay cilmi-baaris macno leh oo ku saabsan qaab-dhismeedka, dhaqdhaqaaqa, iyo qaabka ficilka."
Waqtiga boostada: Oktoobar-31-2023