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 onye meriri ihe nrite Nobel na 1964, chọpụtara usoro a 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 Chemistry na Mahadum Exeter, UK, kwuru, sị: “Nke a bụ njikọ dị ịrịba ama na ihe dị ịrịba ama nke otu 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. 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 nke 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 ahụ “bụ ọmarịcha nka nke 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