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Mushonga (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 musanganiswa uye wakanyatsojeka une zvakasiyana-siyana zvinogona kushandiswa mu tsvakurudzo yemishonga nekuvandudzwa kwemishonga. Komboni iyi ndeyekirasi inonzi azabicyclohexane carboxamides, iyo inozivikanwa kuva ine chekuita nebiology yakakosha.Icho chiral compound, ine stereocenters yakasiyana, inoratidzwa ne (1R, 2S, 5S) zita.Kuvapo kwechirality kwakakosha sezvo kuchigona kukanganisa zvakanyanya zvipenyu zvemukomboni uye kudyidzana netarisiro yebiological.Kumwe kushandiswa kwekomboni iyi sechinangwa chekugadzira nekugadzira mishonga mitsva.Yayo yakasarudzika chimiro uye stereochemistry inopa mikana yemaitiro-chiitiko hukama (SAR) zvidzidzo uye inotungamira optimization.Vatsvagiri vemishonga vanogona kushandura matunhu akasiyana emorekuru kuti aongorore kuti shanduko idzi dzinokanganisa sei kusangana kwayo nezvinangwa zvebiological, senge ma enzymes, receptors, kana vatakuri.Ruzivo urwu runogona kuzoshandiswa kugadzira mishonga ine simba uye inosarudzwa yezvirwere zvakasiyana-siyana. Uyezve, chimiro chekomboni yacho inoratidza kuti inogona kunge ine simba seprotease inhibitor.MaProtease ma enzymes anotamba mabasa akakosha mumhando dzakasiyana dzehupenyu uye anobatanidzwa muzvirwere zvakaita segomarara, HIV, uye kuzvimba kusagadzikana.Izvo zvakagadziriswa uye mapoka anoshanda emukomboni uyu anoita kuti ave mumiriri anovimbisa wekugadzira protease inhibitors nekuvandudzwa kwe potency uye selectivity.Kuwedzera, kuvepo kwekomponi yeboka re cyano uye pyrrolidine ring inoratidza kuti inogona kunge iine basa rinopesana nehutachiona hwehutachiona kana fungal.Kugadziriswa kwemaitiro kunogona kuitwa kuti kuwedzere maitiro ayo antibacterial kana antifungal uye kutungamirira kukugadzirwa kwemishonga mitsva yemishonga inorwisa mabhakitiriya.Uyezve, kuvapo kweboka re trifluoroacetyl kunoreva kuti musanganiswa unogona kuva nekukwanisa seprodrug.Prodrugs haashande kana mashoma anoshanda makomisheni anogona kushandurwa kuita fomu inoshanda mukati memuviri.Boka retrifluoroacetyl rinogona kushanda seboka rakavharika rinodzivirira iro rinogona kutsemurwa kuti ribudise rinoshanda remushonga molecule panzvimbo inodiwa yekuita.Iyi nzira inogona kuvandudza bioavailability yemushonga, kunyungudika, kana kuendesa kune chaiwo matissue.Pakupedzisa, musanganiswa (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 ine chivimbiso sechinhu chakakosha mukutsvaga kwemishonga nekuvandudzwa kwezvinodhaka.Chimiro chayo chakaomarara, stereochemistry, uye mapoka anoshanda anopa mikana yakawanda yekugadzira nekugadzira zvinodhaka zvinodhaka, kuongorora protease inhibition, kugadzira antimicrobial agents, uye kushandisa nzira dzeprodrug.Kuwedzera kutsvagisa uye kuongororwa kwezviitwa zvayo zvebhayoloji uye kugona kwemishonga kunogona kutungamira mukubudirira munzvimbo dzakasiyana dzekurapa.