Oloa

O le tuufaatasiga (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 o se faʻalavelave faʻapitoa ma sili ona faʻapitoa faʻatasi ma faʻaoga eseese i totonu. su'esu'ega vaila'au ma le atina'eina o vaila'au.O lenei fa'alapotopotoga e a'afia i se vasega e ta'ua o azabicyclohexane carboxamides, lea e iloa e iai ni gaioiga fa'ale-aganu'u.O se fa'aputuga o le chiral, o lo'o i ai nofoaga fa'apitoa eseese, fa'ailoa mai e le (1R,2S,5S) fa'ailoga.E taua tele le iai o le fa'ata'ita'iga ona e mafai ona matua a'afia ai le fa'aogaina o mea ola ma le fegalegaleai ma fa'amoemoega. O le tasi le fa'aogaina o lenei vaila'au e fai ma fa'amoemoe mo le mamanuina ma le tu'ufa'atasia o vaila'au fou.O lona fausaga tulaga ese ma le stereochemistry e ofoina atu avanoa mo suʻesuʻega faʻavae-gaoioiga (SAR) ma taʻitaʻia sili.E mafai e tagata su'esu'e vaila'au su'esu'e ona fesuia'i vaega 'ese'ese o le mole e su'esu'e pe fa'afefea ona a'afia e nei suiga ana fegalegaleai ma fa'amoemoega fa'aola, pei ole enzymes, receptors, po'o felauaiga.O lenei malamalama e mafai ona faʻaaogaina e atiaʻe ai vailaʻau sili atu ona malosi ma filifilia mo faʻamaʻi eseese. E le gata i lea, o le fausaga o le faʻapipiʻi e taʻu mai ai e ono mafai ona avea o se inhibitor protease.Proteases o enzymes e taua tele i gaioiga faʻale-aganuʻu eseese ma e aʻafia i faʻamaʻi e pei o le kanesa, HIV, ma faʻamaʻi pipisi.O le faʻatulagaina faʻapitoa ma vaega faʻatino o lenei faʻalapotopotoga ua avea ai ma sui tauva mo le atinaʻeina o inhibitors protease ma le faʻaleleia atili o le malosi ma le filifilia. E le gata i lea, o le i ai o le tuufaatasiga o se vaega cyano ma se mama pyrrolidine e fautua mai ai e ono i ai se gaioiga e faasaga i siama poʻo faʻamaʻi pipisi.E mafai ona faia suiga faʻavae e faʻaleleia ai ana mea faʻamaʻi poʻo mea faʻamaʻi ma taʻitaʻia ai le atinaʻeina o vailaʻau faʻamaʻi fou.Prodrugs o mea e le o toaga po'o le itiiti ifo le malosi e mafai ona liua i le tino galue i totonu o le tino.O le vaega o le trifluoroacetyl e mafai ona avea o se kulupu puipuia ufimata e mafai ona vaeluaina e faʻasaʻo ai le mole mole vailaʻau malosi i le nofoaga o loʻo manaʻomia.O lenei taʻiala e mafai ona faʻaleleia atili ai le bioavailability o vailaʻau, solubility, poʻo le tuʻuina atu i masini faʻapitoa. -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 o loʻo faʻamauina le folafolaga e avea o se tuufaatasiga taua i suʻesuʻega vailaʻau ma le atinaʻeina o vailaʻau.O lona fausaga lavelave, stereochemistry, ma vaega galue e maua ai le tele o avanoa mo le mamanuina ma le tuufaatasia o fualaau fou, suʻesuʻeina o le protease inhibition, atinaʻeina o vailaʻau faʻamaʻi, ma le faʻaogaina o fuafuaga faʻataʻitaʻi.O nisi su'esu'ega ma su'esu'ega o ana gaioioiga fa'ale-natura ma mea e mafai ona fa'afoma'i e mafai ona o'o atu ai i fa'alavelave i vaega fa'afoma'i eseese.