Thiostreptonwaa badeeco dabiici ah oo aad u adag oo loo isticmaalo sida jirka la mariyoantibiyootiga xoolahaiyo sidoo kale waxay leedahay waxqabad wanaagsan oo ka hortagga duumada iyo kansarka.Waqtigan xaadirka ah, si buuxda ayaa kiimiko ahaan loo farsameeyay.
Thiostrepton, oo markii ugu horreysay ka soocday bakteeriyada 1955, waxay leedahay firfircooni antibiyootiko ah oo aan caadi ahayn: waxay joojisaa biosynthesis borotiinka iyada oo ku xidhan RNA ribosomal iyo borotiinada la xidhiidha.Dorothy Crowfoot Hodgkin, crystallographer Ingiriis ah iyo 1964 ku guuleystey abaalmarinta Nobel Prize, ayaa daahfurtay qaabdhismeedka 1970.
Thiostrepton waxa uu ka kooban yahay 10 siddo, 11 peptide bonds, unsaturation ballaaran, iyo 17 stereocenter.Xitaa dhib badan ayaa ah xaqiiqda ah in ay aad ugu nugul tahay asiidhka iyo saldhigyada.Waa xarunta waalidka iyo xubinta ugu adag ee qoyska antibiyootiga thiopeptide.
Hadda xaruntani waxa ay u gacan gashay hadalka macaan ee synthetic ee borofisar kimistari KS Nicolaou iyo asxaabtiisa oo ka socday Machadka Cilmi-baarista Scripps iyo Jaamacadda California ee San Diego [Angew.Chem.caalaminimada.Tifaftirayaasha, 43, 5087 iyo 5092 (2004)].
Christopher J. Moody, Fellow Sare oo Cilmi-baadhis ah oo ka tirsan Waaxda Chemistry-ga ee Jaamacadda Exeter, UK, ayaa faallo ka bixiyay: "Tani waa isku-dubarid taariikhi ah iyo guul la taaban karo oo ay gaadheen kooxda Nicolaou."doxorubicin D.
Furaha qaab-dhismeedkaTHIOSTREPTONwaa giraanta dehydropperidine, taas oo taageerta dabada didehydroalanine iyo laba macrocycles - giraanti thiazoline ka kooban oo 26 xubnood ah iyo nidaamka 27-xubnood ee quinalcolic acid.Nicolaou iyo asxaabtiisuba waxay ka abuureen giraanta dehydropperidine ee furaha agabka bilawga ah iyagoo isticmaalaya falcelin-dimerization iso-Diels-Alder.Tallaabadan muhiimka ah waxay gacan ka gaysatay xaqiijinta soo jeedintii 1978 ee ah in bakteeriyadu u isticmaasho falcelintan si ay biosynthesize antibiyootiga thiopeptide.
Nicolaou iyo asxaabtiisa waxay ku dareen dehydropperidine thiazoline ka kooban baaskiil.Waxay isku darka baaskiilkan iyo qaab-dhismeed ka kooban quinalcolic acid iyo horreeyaha dabada didehydroalanine.Kadibna waxay nadiifiyeen alaabta si ay u helaanthiostrepton.
Dib-u-eegayaasha labada waraaqood ee kooxdu waxay yiraahdeen isku-dubbaridu "waa farshaxan-sare oo muujinaya tignoolajiyada casriga ah oo furaysa aragtiyo cusub oo cilmi-baaris macno leh oo ku saabsan qaab-dhismeedka, dhaqdhaqaaqa, iyo qaabka ficilka."
Waqtiga boostada: Oct-31-2023