Thiostreptonke sehlahisoa sa baktheria sa tlhaho se rarahaneng haholo se sebelisoang e le topicallithibela-mafu tsa bongaka ba liphoofolohape e na le tšebetso e ntle ea ho thibela malaria le mofetše.Hona joale, e entsoe ka lik'hemik'hale ka ho feletseng.
Thiostrepton, e qalileng ho arohana le baktheria ka 1955, e na le ts'ebetso e sa tloaelehang ea lithibela-mafu: e thibela protheine biosynthesis ka ho tlama ho ribosomal RNA le liprotheine tse amanang le eona.Dorothy Crowfoot Hodgkin, ralitaba oa Brithani le mohapi oa Khau ea Nobel ka 1964, o ile a sibolla sebopeho sena ka 1970.
Thiostrepton e na le mehele ea 10, li-bond tsa peptide tse 11, unsaturation e pharaletseng, le li-stereocenters tse 17.Ntho e thata le ho feta ke hore e na le kutloelo-bohloko haholo ho li-acids le metheo.Ke motsoako oa motsoali le setho se rarahaneng ka ho fetisisa sa lelapa la lithibela-mafu tsa thiopeptide.
Hona joale motsoako ona o inehetse puong e monate ea maiketsetso ea moprofesa oa k'hemistri KS Nicolaou le basebetsi-'moho le eena ba Scripps Research Institute le Univesithi ea California e San Diego [Angew.Chem.machaba.Bahlophisi, 43, 5087 le 5092 (2004)].
Christopher J. Moody, Mosebetsi-’moho e Moholo oa Lipatlisiso Lefapheng la K’hemistri Univesithing ea Exeter, UK, o ile a re: “Ena ke kopano e ikhethang le katleho e tsotehang ea sehlopha sa Nicolaou.”doxorubicin D.
Senotlolo sa sebopeho saTHIOSTREPTONke reng ea dehydropiperidine, e tšehetsang mohatla oa didehydroalanine le li-macrocycle tse peli - reng e nang le thiazoline e nang le litho tse 26 le tsamaiso ea quinalcolic acid e 27.Nicolaou le basebetsi mmoho ba thehile selikalikoe sa senotlolo sa dehydropiperidine ka lisebelisoa tse bonolo tsa ho qala ba sebelisa biomimetic iso-Diels–Alder dimerization reaction.Mohato ona oa bohlokoa o thusitse ho netefatsa tlhahiso ea 1978 ea hore libaktheria li sebelise karabelo ena ho biosynthesize lithibela-mafu tsa thiopeptide.
Nicolaou le basebetsi-'moho ba kentse dehydropiperidine ho macrocycle e nang le thiazoline.Ba kopanya macrocycle ena le sebopeho se nang le quinalcolic acid le selelekela sa mohatla oa didehydroalanine.Eaba ba hloekisa sehlahisoa ho fumanathiostrepton.
Bahlahlobisisi ba lipampiri tse peli tsa sehlopha ba boletse hore motsoako "ke mosebetsi o tsoileng matsoho o totobatsang theknoloji ea morao-rao le ho bula menyetla e mecha bakeng sa lipatlisiso tse nang le morero mabapi le sebopeho, ts'ebetso le mokhoa oa ketso."
Nako ea poso: Oct-31-2023