Tiostreptonhe hua huakita taiao tino uaua ka whakamahia hei kaupapapaturopi kararehehe pai hoki te mahi antimalarial me te mate pukupuku.I tenei wa, kua oti te whakahiato matū.
Ko Thiostrepton, i wehe tuatahi mai i te huakita i te tau 1955, he mahi paturopi rerekee: ka aukati i te koiora pūmua ma te here ki te RNA ribosom me ona pūmua e hono ana.I kitea e Dorothy Crowfoot Hodgkin, he kairataata o Ingarangi me te toa Nobel Prize 1964, i te hanganga i te tau 1970.
Kei roto i te Thiostrepton nga mowhiti 10, nga here peptide 11, te koretake nui, me nga pokapū stereo 17.Ko te mea he tino uaua ki te waikawa me te kawakore.Koia te huinga matua me te mema tino uaua o te whanau paturopi thiopeptide.
Inaianei kua hinga tenei puhui ki nga korero reka a te ahorangi matū a KS Nicolaou me ana hoa mai i te Scripps Research Institute me te Whare Wananga o California i San Diego [Angew.Chem.te ao.Etita, 43, 5087 me 5092 (2004)].
Ko Christopher J. Moody, Kairangahau Matua i roto i te Tari Matū i te Whare Wananga o Exeter, UK, i korero: "He kohinga tohu tenei me te whakatutukitanga whakamiharo a te roopu Nicolaou."doxorubicin D.
Key to the structure ofTIOSTREPTONko te mowhiti dehydropiperidine, e tautoko ana i te hiku didehydroalanine me nga macrocycles e rua - he 26-membered thiazoline-containing ring me te 27-membered quinalcolic acid system.I hangaia e Nicolaou me nga hoa mahi te whakakai dehydropiperidine matua mai i nga rauemi timatanga ngawari ma te whakamahi i te tauhohenga dimerization iso-Diels-Alder biomimetic.I awhina tenei mahi nui ki te whakau i te tono o te tau 1978 ka whakamahia e te huakita tenei tauhohenga ki te biosynthesize paturopi thiopeptide.
I whakauruhia e Nicolaou me o hoa mahi te dehydropiperidine ki roto i te macrocycle kei roto thiazoline.I honoa e ratou tenei macrocycle me tetahi hanganga kei roto te waikawa quinalcolic me te hiku o mua o te didehydroalanine.Na ka purea e ratou te hua kia whiwhitiostrepton.
Ko nga kai-arotake o nga pepa e rua a te roopu i kii ko te whakahiatotanga "he mahi rangatira e whakaatu ana i nga hangarau hou o te ao me te whakatuwhera i nga waahi hou mo te rangahau whai kiko ki te hanganga, te mahi, me te momo mahi."
Te wa tuku: Oketopa-31-2023