Lihlahisoa

Motsoako (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 ke motsoako o rarahaneng le o khethehileng haholo o nang le lisebelisoa tse fapaneng lipatlisiso tsa meriana le nts'etsopele ea lithethefatsi.Motsoako ona ke oa sehlopha se bitsoang azabicyclohexane carboxamides, tse tsejoang ka hore li na le ts'ebetso ea bohlokoa ea likokoana-hloko.Ke motsoako oa chiral, o nang le li-stereocenters tse fapaneng, tse bontšitsoeng ke (1R,2S,5S).Ho ba teng ha chirality ho bohlokoa kaha ho ka ama haholo thepa ea tlhaho ea motsoako le ho sebelisana le sepheo sa likokoana-hloko. Tšebeliso e 'ngoe ea motsoako ona ke sepheo sa ho rala le ho kopanya lithethefatsi tse ncha.Sebopeho sa eona se ikhethileng le stereochemistry li fana ka menyetla ea lithuto tsa kamano ea sebopeho le ts'ebetso (SAR) le ntlafatso ea moetapele.Bafuputsi ba meriana ba ka fetola libaka tse fapaneng tsa molek'hule ho batlisisa hore na liphetoho tsena li ama litšebelisano tsa eona joang le sepheo sa tlhaho, joalo ka li-enzyme, li-receptor kapa lipalangoang.Tsebo ena joale e ka sebelisoa ho hlahisa litlhare tse matla le tse khethang bakeng sa mafu a fapaneng. Ho feta moo, sebopeho sa motsoako se fana ka maikutlo a hore e kanna ea ba le monyetla oa ho thibela protease inhibitor.Li-protease ke li-enzyme tse phethang karolo ea bohlokoa lits'ebetsong tse fapaneng tsa tlhaho 'me li ameha mafung a kang mofetše, HIV le mafu a ho ruruha.Lihlopha tse khethehileng tsa tlhophiso le tse sebetsang tsa motsoako ona li etsa hore e be mokhethoa ea tšepisang bakeng sa ho hlahisa li-protease inhibitors tse nang le matla a ntlafetseng le khetho.Liphetoho tsa sebopeho li ka etsoa ho ntlafatsa thepa ea eona ea antibacterial kapa antifungal le ho lebisa ho nts'etsopele ea li-antimicrobial agents tse ncha.Ho feta moo, ho ba teng ha sehlopha sa trifluoroacetyl ho bolela hore motsoako o ka ba le bokhoni ba ho ba prodrug.Lihlahisoa tsa lihlahisoa ke metsoako e sa sebetseng kapa e sa sebetseng haholo e ka fetoloang ka mokhoa o sebetsang ka hare ho 'mele.Sehlopha sa trifluoroacetyl se ka sebetsa e le sehlopha se sirelelitsoeng se sirelelitsoeng se ka koalehang ho lokolla molek'hule ea lithethefatsi e sebetsang sebakeng se lakatsehang sa ts'ebetso.Leano lena le ka ntlafatsa bioavailability ea lithethefatsi, solubility, kapa ho fana ka lisele tse itseng.Qetellong, motsoako (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 e na le tšepiso e le motsoako oa bohlokoa lipatlisisong tsa meriana le nts'etsopele ea lithethefatsi.Sebopeho sa eona se rarahaneng, stereochemistry, le lihlopha tse sebetsang li fana ka menyetla e mengata ea ho qapa le ho kopanya lithethefatsi tse ncha, ho hlahloba thibelo ea protease, ho hlahisa li-antimicrobial agents, le ho sebelisa maano a lihlahisoa.Lipatlisiso tse ling le tlhahlobo ea mesebetsi ea eona ea tlhaho le bokhoni ba pharmacological li ka lebisa katlehong libakeng tse fapaneng tsa kalafo.