CAS:187235-37-6
187235-37-6
CAS号：187235-37-6
品名：Pretomanid
中文别名：Pretomanid
英文别名：Pretomanid(PA-824);PA-824;UNII-2XOI31YC4N;(S)-6-(4-(trifluoromethoxy)benzyloxy)-2-nitro-6,7-dihydro-5H-imidazo[2,1-b][1,3]oxazine;(6S)-2-nitro-6-[[4-(trifluoromethoxy)phenyl]methoxy]-6,7-dihydro-5H-imidazo[2,1-b][1,3]oxazine;
分子式：C14H12F3N3O5
分子量：359.257
精确质量：359.073
Psa：91.33
MDL号：MFCD06809939
密度：1.58g/cm3
沸点：462.3ºC at 760 mmHg
闪点：233.4ºC
折射率：1.588
蒸汽压：1E-08mmHg at 25°C
海关编码：2934999090
信号词：Warning
危险性防范说明：P280; P304 + P340 + P312; P305 + P351 + P338; P337 + P313
危险标志：GHS07
危险性描述：H315; H319; H335
简介：Pretomanid(PA-824)isanexperimentalanti-tuberculosisdrug.Pretomanidisabicyclicnitroimidazole-likemoleculewithaverycomplexmechanismofaction.Itisactiveagainstbothreplicatingandhypoxic,non-replicatingMycobacteriumtuberculosis.Microarrayanalysisofthemodeofactionofpretomanidshowedapuzzlingmixedeffectbothongenesresponsivetobothcellwallinhibition(likeisoniazid)andrespiratorypoisoning(likecyanide).Theaerobickillingmechanismofthisdrugappearstoinvolveinhibitionofcellwallmycolicacidbiosynthesisthroughanasyetunknownmolecularmechanism.Therespiratorypoisoningthroughnitricoxidereleaseseemedtobeacrucialelementofanaerobicactivitybypretomanid.Theeffectofpretomanidontherespiratorycomplexunderhypoxicnon-replicatingconditionswasalsomanifestedinarapiddropinintracellularATPlevels,againsimilartothatobservedbycyanidetreatment.Pretomanidrecentlywasshowntobesafe,welltolerated,andefficaciousatdosesof100–200mgdailyinadose-rangingstudyamongdrug-sensitive,sputumsmear–positive,adultpulmonaryTBpatients
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