Thiostreptonbụ ngwaahịa nje bacteria dị mgbagwoju anya nke a na-eji eme ihe n'eluọgwụ nje anụmanụma nwekwara ezigbo ọrụ mgbochi ịba na mgbochi ọrịa kansa.Ka ọ dị ugbu a, a na-emepụta ya kpamkpam.
Thiostrepton, nke dịpụrụ adịpụ na nje bacteria na 1955, nwere ọrụ ọgwụ nje pụrụ iche: ọ na-egbochi protein biosynthesis site na ijikọ ribosomal RNA na protein ndị metụtara ya.Dorothy Crowfoot Hodgkin, onye Britain crystallographer na 1964 onye meriri ihe nrite Nobel, chọpụtara ihe owuwu ahụ na 1970.
Thiostrepton nwere mgbanaka 10, 11 peptide bond, nnukwu unsaturation na 17 stereocenters.Ọbụna ihe ịma aka karị bụ eziokwu ahụ bụ na ọ na-enwe mmetụta nke ọma na acids na bases.Ọ bụ ogige nne na nna na onye kachasị mgbagwoju anya nke ezinụlọ ọgwụ nje thiopeptide.
Ugbu a ogige a abanyela n'okwu ụtọ sịntetik nke prọfesọ kemịkalụ KS Nicolaou na ndị ọrụ ibe ya sitere na Scripps Research Institute na Mahadum California na San Diego [Angew.Chem.mba ụwa.Ndị editọ, 43, 5087 na 5092 (2004)].
Christopher J. Moody, Onye Ọkachamara Onye Nchọnchọ Na Ngalaba Na-ahụ Maka Chemistry na Mahadum Exeter, UK, kwuru, sị: “Nke a bụ njikọ dị ịrịba ama na ihe dị ịrịba ama nke òtù Nicolaou rụpụtara.”doxorubicin D.
Isi ihe owuwu nkeỤlọ ọrụ THIOSTREPTONbụ mgbanaka dehydropperidine, nke na-akwado ọdụ didehydroalanine na macrocycles abụọ - mgbanaka thiazoline nwere 26 na usoro 27 quinalcolic acid.Nicolaou na ndị ọrụ ibe mebere mgbanaka dehydropperidine igodo site na ihe mmalite dị mfe site na iji mmeghachi omume iso-Diels-Alder dimerization biomimetic.Nzọụkwụ a dị mkpa nyere aka kwado atụmatụ 1978 na nje bacteria na-eji mmeghachi omume a mee ihe na biosynthesize ọgwụ nje thiopeptide.
Nicolaou na ndị ọrụ ibe webatara dehydropperidine n'ime igwe igwe nwere thiazoline.Ha jikọtara macrocycle a na nhazi nwere quinalcolic acid na didehydroalanine ọdụ precursor.Ha wee mee ka ngwaahịa ahụ dị ọcha ka ha nwetathiostrepton.
Ndị na-enyocha akwụkwọ akụkọ abụọ nke otu ahụ kwuru na njikọ a “bụ ọmarịcha ihe na-eme ka teknụzụ ọgbara ọhụrụ pụta ìhè ma meghee ọhụụ ọhụrụ maka nyocha bara uru gbasara nhazi, ọrụ, na usoro omume.”
Oge nzipu: Ọktoba 31-2023