Nā huahana

ʻO ka hui (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 he mea paʻakikī a kikoʻī loa me nā noi like ʻole i loko. ka noiʻi lāʻau lapaʻau a me ka hoʻomohala ʻana i ka lāʻau. Aia kēia pūhui i kahi papa i kapa ʻia ʻo azabicyclohexane carboxamides, i ʻike ʻia he hana koʻikoʻi koʻikoʻi.He pūhui chiral ia, aia nā stereocenters like ʻole, i hōʻike ʻia e ka (1R,2S,5S).He mea koʻikoʻi ka noho ʻana o ka chirality no ka mea hiki iā ia ke hoʻopili nui i nā waiwai ola o ka pūhui a me ka launa pū ʻana me nā pahuhopu olaola.Hāʻawi kona ʻano kūʻokoʻa a me ka stereochemistry i nā manawa kūpono no nā haʻawina hoʻolālā-activity relationship (SAR) a me ke alakaʻi maikaʻi ʻana.Hiki i nā mea noiʻi lāʻau lapaʻau ke hoʻololi i nā ʻāpana like ʻole o ka mole e noiʻi i ke ʻano o kēia mau hoʻololi i ka pili ʻana i kāna mau pilina me nā pahuhopu olaola, e like me nā enzymes, receptors, a transporters.Hiki ke hoʻohana ʻia kēia ʻike no ka hoʻomohala ʻana i nā lāʻau ʻoi aku ka ikaika a me ka koho no nā maʻi like ʻole.ʻO Proteases nā enzymes e pāʻani i nā kuleana koʻikoʻi i nā kaʻina hana olaola like ʻole a pili i nā maʻi e like me ke kanesa, HIV, a me nā maʻi ʻeha.ʻO ka hoʻonohonoho kikoʻī a me nā pūʻulu hana o kēia pūhui e lilo ia i moho hoʻohiki no ka hoʻomohala ʻana i nā mea pale protease me ka hoʻomaikaʻi ʻana i ka mana a me ka koho.Hiki ke hoʻololi i ka hoʻololiʻana i ka hoʻonuiʻana i kona mau mea antibacterial a iʻole antifungal a alakaʻi i ka uluʻana o nā mea antimicrobial hou.ʻO nā prodrugs nā pūhui hana ʻole a liʻiliʻi paha i hiki ke hoʻololi ʻia i ke ʻano hana i loko o ke kino.Hiki i ka hui trifluoroacetyl ke lawelawe ma ke ʻano he pūʻulu pale masked i hiki ke hoʻokaʻawale ʻia e hoʻokuʻu i ka moleke lāʻau ikaika ma kahi o ka hana i makemake ʻia.Hiki i kēia hoʻolālā ke hoʻomaikaʻi i ka bioavailability o ka lāʻau lapaʻau, solubility, a i ʻole ka hāʻawi ʻana i nā kiko kikoʻī. -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 paʻa i ka ʻōlelo hoʻohiki ma ke ʻano he hui waiwai i ka noiʻi lāʻau lapaʻau a me ka hoʻomohala ʻana i ka lāʻau.ʻO kāna ʻano paʻakikī, stereochemistry, a me nā hui hana e hāʻawi i nā manawa he nui no ka hoʻolālā ʻana a me ka synthesizing i nā lāʻau lapaʻau hou, ka ʻimi ʻana i ka pale protease, ka hoʻomohala ʻana i nā mea antimicrobial, a me ka hoʻohana ʻana i nā hoʻolālā prodrug.ʻO ka noiʻi hou ʻana a me ka ʻimi ʻana i kāna mau hana olaola a me ka hiki ke alakaʻi i ka holomua ma nā wahi lapaʻau like ʻole.