Thiostreptonsamfuri ne na ƙwayoyin cuta na halitta mai sarƙaƙƙiya wanda ake amfani da shi azaman kayan shafamaganin rigakafi na dabbobisannan kuma yana da aikin maganin zazzabin cizon sauro da na ciwon daji.A halin yanzu, an haɗa shi gaba ɗaya ta hanyar sinadarai.
Thiostrepton, wanda aka keɓe da farko daga ƙwayoyin cuta a cikin 1955, yana da aikin ƙwayoyin cuta na yau da kullun: yana hana gina jiki biosynthesis ta ɗaure ga RNA ribosomal da sunadarai masu alaƙa.Dorothy Crowfoot Hodgkin, ɗan Burtaniya crystallographer kuma wanda ya lashe kyautar Nobel a 1964, ya gano tsarin a cikin 1970.
Thiostrepton ya ƙunshi zobba 10, 11 peptide bonds, m unsaturation, da 17 stereocenters.Ko da mafi kalubale shine gaskiyar cewa yana da matukar damuwa ga acid da tushe.Shi ne mahallin mahaifa kuma mafi hadaddun memba na dangin maganin rigakafi na thiopeptide.
Yanzu wannan fili ya mika wuya ga magana mai dadi na roba Farfesa KS Nicolaou da abokan aikinsa daga Cibiyar Nazarin Scripps da Jami'ar California a San Diego [Angew.Chem.kasa da kasa.Masu gyara, 43, 5087 da 5092 (2004)].
Christopher J. Moody, Babban Jami’in Bincike a Sashen Kimiyyar Kimiya na Jami’ar Exeter, UK, ya yi sharhi: “Wannan wani abu ne mai ban mamaki da kuma babbar nasara ta ƙungiyar Nicolaou.”doxorubicin D.
Makullin tsarinTHIOSTREPTONshine zoben dehydropperidine, wanda ke goyan bayan wutsiyar didehydroalanine da macrocycles guda biyu - zoben thiazoline mai memba 26 da tsarin quinalcolic acid mai mambobi 27.Nicolaou da abokan aiki sun ƙirƙiri maɓalli na dehydropperidine zoben daga kayan farawa masu sauƙi ta amfani da amsawar iso-Diels-Alder dimerization na biomimetic.Wannan muhimmin mataki ya taimaka wajen tabbatar da shawarar 1978 cewa ƙwayoyin cuta suna amfani da wannan amsa don biosynthesize maganin rigakafi na thiopeptide.
Nicolaou da abokan aikinsa sun haɗa dehydropperidine cikin wani keken keke mai thiazoline.Sun haɗa wannan macrocycle tare da tsari mai ɗauke da quinalcolic acid da didehydroalanine precursor wutsiya.Sai suka tsarkake samfurin don samunthiostrepton.
Masu bitar takardun ƙungiyar guda biyu sun ce haɗakarwa "wani ƙwarewa ce da ke ba da haske kan fasahar zamani da buɗe sabon hangen nesa don bincike mai ma'ana kan tsari, aiki, da yanayin aiki."
Lokacin aikawa: Oktoba-31-2023