Ibicuruzwa

Urusange (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 ubushakashatsi mu bya farumasi no guteza imbere ibiyobyabwenge. Uru ruganda ni urwego rwitwa azabicyclohexane carboxamide, izwiho kugira ibikorwa biologiya bikomeye.Nibintu bya chiral, birimo stereocenters zitandukanye, byerekanwe na (1R, 2S, 5S).Kubaho kwa chirality ni ngombwa kuko bishobora kugira ingaruka zikomeye kumiterere yibinyabuzima hamwe no guhuza intego yibinyabuzima.Bimwe mubishobora gukoresha iyi nteruro ni intego yo gushushanya no guhuza ibiyobyabwenge bishya.Imiterere yihariye hamwe na stereochemie itanga amahirwe kubikorwa byubaka-ibikorwa (SAR) no kuyobora neza.Abashakashatsi mu bya farumasi barashobora guhindura uturere dutandukanye twa molekile kugira ngo bakore iperereza ku buryo izo mpinduka zigira ingaruka ku mikoranire yazo n’ibinyabuzima, nka enzymes, reseptors, cyangwa abatwara ibintu.Ubu bumenyi burashobora gukoreshwa mugutezimbere imiti ikomeye kandi itoranya indwara zitandukanye.Ikindi kandi, imiterere yikigo yerekana ko ishobora kuba ifite ubushobozi bwo kubuza protease.Poroteyine ni imisemburo igira uruhare runini mu binyabuzima bitandukanye kandi igira uruhare mu ndwara nka kanseri, virusi itera sida, n'indwara ziterwa n'umuriro.Iboneza ryihariye hamwe nitsinda ryimikorere yuru ruganda bituma riba umukandida utanga ikizere cyo guteza imbere protease inhibitor zifite imbaraga noguhitamo neza.Ikindi kandi, kuba uru ruganda kuba rwitsinda rya cyano hamwe nimpeta ya pyrrolidine byerekana ko ishobora kuba ifite ibikorwa byo kurwanya indwara ziterwa na bagiteri cyangwa fungal.Impinduka zubaka zirashobora gukorwa kugirango zongere antibacterial cyangwa antifungal kandi biganisha ku iterambere ryimiti mishya ya mikorobe. Byongeye kandi, kuba hari itsinda rya trifluoroacetyl ryerekana ko uruganda rushobora kugira ubushobozi nka prodrug.Prodrugs idakora cyangwa idakora cyane ishobora guhinduka muburyo bukora mumubiri.Itsinda rya trifluoroacetyl rirashobora gukora nk'itsinda ririnda mask rishobora gukingurwa kugirango irekure molekile yibiyobyabwenge ikora aho wifuza gukorera.Izi ngamba zirashobora kunoza ibiyobyabwenge bioavailable, solubilité, cyangwa kugeza kumubiri wihariye. Mugusoza, ibice (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 ifite amasezerano nkurwego rwingirakamaro mubushakashatsi bwa farumasi no guteza imbere ibiyobyabwenge.Imiterere igoye, stereochemie, hamwe nitsinda ryimikorere bitanga amahirwe menshi yo gushushanya no guhuza imiti mishya, gushakisha uburyo bwo kubuza protease, guteza imbere imiti yica mikorobe, no gukoresha ingamba za prodrug.Ubundi bushakashatsi nubushakashatsi bwibikorwa byibinyabuzima hamwe nubushobozi bwa farumasi bishobora gutera intambwe mubice bitandukanye byo kuvura.