Ibicuruzwa

Trans-1--Irangwa no kuba hari impeta ya pyrrolidine yasimbujwe na tert-butoxycarbonyl (Boc) irinda itsinda kuri atome ya azote hamwe nitsinda rya trifluoromethyl ku mpeta ya fenyl. Kimwe mu bintu by'ingenzi byakoreshejwe trans-1- (tert-Butoxycarbonyl) - - 4- (3-.Imiterere yihariye hamwe nitsinda ryimikorere bituma igira inyubako zinyuranye zo kubaka molekile zigoye.Itsinda rya Boc rikora nk'itsinda ririnda, rishobora gukurwaho mu buryo bwihariye kugira ngo ryerekane urubuga rugaragara kugira ngo ruhindurwe.Ibi bituma habaho ihinduka ryibinyabuzima kandi ryuzuye. Itsinda rya trifluoromethyl muri trans-1- (tert-Butoxycarbonyl) -4- (3- (trifluoromethyl) phenyl) pyrrolidine-3-karubasi ya acide nayo itanga ibintu byingenzi nibishobora gukoreshwa.Amatsinda ya Trifluoromethyl azwiho imiterere yo gukuramo electron na lipophilicity, ishobora kongera imbaraga, ihindagurika ryimikorere, hamwe na bioavailable yabakandida ibiyobyabwenge.Byongeye kandi, itsinda rya trifluoromethyl rirashobora guhindura imiterere ya fiziki ya chimique yikomatanyirizo, bikagira ingaruka kumuti, lipophilicity, hamwe na reseptor ihuza isano.Ikindi kandi, trans-1- (tert-Butoxycarbonyl) -4- (3- (trifluoromethyl) fenyl) pyrrolidine-3- acide karubike irashobora kwerekana ibikorwa byibinyabuzima ubwabyo cyangwa nka prodrug.Prodrugs ni ibinyabuzima bidakora biologiya bihindura imiti cyangwa enzymatique mumubiri kugirango bihindurwe ibiyobyabwenge.Rimwe na rimwe, itsinda ririnda Boc rishobora gukurwaho guhitamo muri vivo, gukora uruganda kugirango rutange ingaruka zifatika zo kuvura. Mugihe porogaramu zihariye hamwe nibishobora gukoreshwa kuri trans-1- (tert-Butoxycarbonyl) -4- (3- (trifluoromethyl) phenyl) pyrrolidine-3-karubasi ya acide ni myinshi, irindi perereza nubushakashatsi birakenewe kugirango tumenye ubushobozi bwuzuye.Ibi mubisanzwe birimo imiti ya chimie itezimbere, imiterere-ibikorwa byubushakashatsi, hamwe nisuzuma ryibinyabuzima.Mugusobanukirwa neza imiterere yikigo nigikorwa cyacyo, abahanga barashobora gusuzuma niba bikwiriye kwibasira indwara cyangwa imiterere yihariye, biganisha ku iterambere ry’abakandida b’ibiyobyabwenge cyangwa imiti ya catalitiki mu bihe biri imbere.