Thiostreptonwani samfuri ne mai matuƙar rikitarwa na ƙwayoyin cuta na halitta wanda ake amfani da shi azaman maganin shafawamaganin rigakafi na dabbobikuma yana da kyakkyawan aikin maganin zazzabin cizon sauro da kuma maganin ciwon daji. A halin yanzu, an haɗa shi gaba ɗaya ta hanyar sinadarai.
Thiostrepton, wanda aka fara ware shi daga ƙwayoyin cuta a shekarar 1955, yana da aikin maganin rigakafi na musamman: yana hana samar da furotin ta hanyar ɗaure shi da ribosomal RNA da sunadaran da ke da alaƙa da shi. Dorothy Crowfoot Hodgkin, wani mai zane-zanen kristal na Burtaniya kuma wanda ya lashe kyautar Nobel ta 1964, ya gano tsarin a shekarar 1970.
Thiostrepton ya ƙunshi zobba 10, haɗin peptide 11, rashin isasshen abinci mai yawa, da kuma cibiyoyin sitiriyo 17. Abin da ya fi ƙalubale shi ne gaskiyar cewa yana da matuƙar saurin kamuwa da acid da tushe. Ita ce mahaɗin iyaye kuma mafi rikitarwa a cikin dangin maganin rigakafi na thiopeptide.
Yanzu wannan mahaɗin ya yarda da maganar roba ta farfesa KS Nicolaou da abokan aikinsa daga Cibiyar Bincike ta Scripps da Jami'ar California da ke San Diego [Angew. Chem. internationality. Editoci, 43, 5087 da 5092 (2004)].
Christopher J. Moody, Babban Jami'in Bincike a Sashen Kimiyyar Sinadarai a Jami'ar Exeter, Birtaniya, ya yi tsokaci: "Wannan wani muhimmin tsari ne kuma babban nasara da ƙungiyar Nicolaou ta samu." doxorubicin D.
Mabuɗin tsarinTHIOSTREPTONzoben dehydropiperidine ne, wanda ke tallafawa wutsiyar didehydroalanine da macrocycles guda biyu - zoben thiazoline mai membobi 26 da tsarin quinalcolic acid mai membobi 27. Nicolaou da abokan aikinsa sun ƙirƙiri zoben dehydropiperidine mai mahimmanci daga kayan farawa masu sauƙi ta amfani da hanyar dimerization ta biomimetic iso-Diels-Alder. Wannan muhimmin mataki ya taimaka wajen tabbatar da shawarar 1978 cewa ƙwayoyin cuta suna amfani da wannan amsawar ga maganin rigakafi na thiopeptide.
Nicolaou da abokan aikinsa sun haɗa dehydropeperidine a cikin macrocycle mai ɗauke da thiazoline. Sun haɗa wannan macrocycle da wani tsari da ke ɗauke da quinalcolic acid da kuma wani precursor na wutsiya didehydroalanine. Sannan suka tsarkake samfurin don samunthiostrepton.
Masu bitar takardu biyu na ƙungiyar sun ce wannan tsari "wani babban aiki ne da ke haskaka fasahar zamani kuma yana buɗe sabbin hanyoyi don bincike mai ma'ana game da tsari, aiki, da kuma yanayin aiki."
Lokacin Saƙo: Oktoba-31-2023