Ngwaahịa

Ngwakọta (1R,2S,5S) -N-[(1S) -1-cyano-2-[(3S) -2-oxopyrrolidin-3-yl] ethyl]-3-[(2S) -3,3- dimethyl-2-[(2,2,2-trifluoroacetyl) amino] butanoyl] -6,6-dimethyl-3-azabicyclo[3.1.0] hexane-2-carboxamide bụ ihe mgbagwoju anya na nke ukwuu kpọmkwem ogige nwere ngwa dị iche iche nwere ike na. nyocha ọgwụ na mmepe ọgwụ. Ngwa a bụ nke klas a na-akpọ azabicyclohexane carboxamides, nke a maara na ọ nwere nnukwu ọrụ ndu.Ọ bụ ngwakọta chiral, nwere stereocenters dị iche iche, nke (1R,2S,5S) gosipụtara.Ọnụnọ nke chirality dị mkpa n'ihi na ọ nwere ike imetụta ihe ndị mejupụtara ya na mmekọrịta ya na ebumnuche ndu. Otu nwere ike iji onyinye a bụ ebumnuche maka imepụta na imepụta ọgwụ ọhụrụ.Ọdịdị ya pụrụ iche na stereochemistry na-enye ohere maka ọmụmụ ihe nhazi-mmekọrịta ihe (SAR) na njikarịcha ndu.Ndị na-eme nchọpụta ọgwụ nwere ike gbanwee mpaghara dị iche iche nke molecule ka ha nyochaa otú mgbanwe ndị a si emetụta mmekọrịta ya na ebumnuche ndu, dị ka enzymes, ndị na-anabata ya, ma ọ bụ ndị na-ebugharị.Enwere ike iji ihe ọmụma a mee ihe iji mepụta ọgwụ ndị dị ike ma na-ahọrọ maka ọrịa dị iche iche. Ọzọkwa, nhazi nke ogige ahụ na-egosi na ọ nwere ike inwe ike dị ka onye na-egbochi protease.Proteases bụ enzymes nke na-arụ ọrụ dị mkpa na usoro ndu dị iche iche ma na-etinye aka na ọrịa ndị dị ka ọrịa cancer, HIV, na ọrịa mkpali.Nhazi a kapịrị ọnụ na ndị na-arụ ọrụ nke ogige a na-eme ka ọ bụrụ onye na-ekwe nkwa na-emepe emepe protease inhibitors na ike dị mma na selectivity. Ọzọkwa, ọnụnọ nke ogige nke otu cyano na mgbanaka pyrrolidine na-egosi na ọ nwere ike inwe ọrụ megide nje bacteria ma ọ bụ fungal.Enwere ike ime mgbanwe nhazi iji kwalite ihe ndị na-egbu egbu ma ọ bụ ọgwụ nje ma na-eduga na mmepe nke ọhụrụ antimicrobial agents. Ọzọkwa, ọnụnọ nke otu trifluoroacetyl na-egosi na ogige ahụ nwere ike inwe ike dị ka prodrug.Prodrugs bụ ndị na-adịghị arụ ọrụ ma ọ bụ ndị na-adịghị arụ ọrụ ogige nke nwere ike ịtụgharị n'ime ụdị arụ ọrụ n'ime ahụ.Otu trifluoroacetyl nwere ike ije ozi dị ka otu nchekwa mkpuchi mkpuchi nke enwere ike ịkewaa iji hapụ molekul ọgwụ na-arụ ọrụ na saịtị achọrọ.Usoro a nwere ike imeziwanye bioavailability nke ọgwụ ahụ, solubility, ma ọ bụ nnyefe na anụ ahụ dị iche iche. N'ikpeazụ, ngwakọta (1R,2S,5S) -N-[(1S) -1-cyano-2-[(3S) -2-oxopyrrolidin -3-yl] ethyl] -3-[(2S) -3,3-dimethyl-2-[(2,2,2-trifluoroacetyl) amino] butanoyl]-6,6-dimethyl-3-azabicyclo[3.1. 0] hexane-2-carboxamide na-ekwe nkwa dị ka ihe bara uru na nyocha ọgwụ na mmepe ọgwụ.Ọdịdị ya dị mgbagwoju anya, stereochemistry, na otu ndị na-arụ ọrụ na-enye ọtụtụ ohere maka ịmepụta na ịmepụta ọgwụ ọhụrụ, nyochaa mgbochi protease, ịmepụta ihe ndị na-egbu nje na iji usoro ọgwụ ọjọọ eme ihe.Nnyocha ọzọ na nyocha nke ọrụ ndụ ya na ikike ọgwụ nwere ike ime ka ọ nwee ọganihu na mpaghara ọgwụgwọ dị iche iche.