(S)-2-硝基-6-[[4-(三氟甲氧基)苄基]氧基]... (S)-2-Nitro-6-[[4-(trifluoro... 0.25g

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