5-Nitroisatin CAS 611-09-6

1. Cov tshuaj tua kab mob thiab tshuaj tua kab mob
5-nitroindigo thiab nws cov derivatives tau pom muaj peev xwm tseem ceeb hauv kev tsim cov tshuaj tua kab mob thiab tshuaj tua kab mob. Los ntawm kev hloov kho cov qauv, cov molecules nquag tsom rau cov kab mob tshwj xeeb tuaj yeem tsim. Piv txwv li, nws cov pab pawg nitro tuaj yeem hloov mus rau hauv ib pawg amino los ntawm kev txo cov tshuaj tiv thaiv, thiab tom qab ntawd koom nrog kev ua kom muaj zog, sulfonation thiab lwm yam kev cuam tshuam los tsim cov pob txha heterocyclic nrog cov tshuaj tua kab mob. Cov tebchaw no tuaj yeem ua rau lawv cov teebmeem los ntawm kev cuam tshuam nrog microbial cell phab ntsa synthesis lossis inhibiting cov haujlwm tseem ceeb enzyme.

2. Tshuaj synthesis
Lub synthesis ntawm cov leeg relaxant fluoroquinolone: ​​5-nitroindole-3-acetic anhydride (tau los ntawm ntxiv nitration ntawm 5-nitroindole-3-acetic acid) yog ib qho tseem ceeb nruab nrab ntawm cov synthesis ntawm fluoroquinolone. Fluquinolone tau tsim los ntawm Tanabe Corporation hauv Nyij Pooj thiab thawj zaug tau tsim tawm hauv xyoo 1983. Nws yog ib qho kev so nrog kev kho mob zoo ntawm lub ntsej muag thiab caj dab cov leeg nqaij. Txoj kev synthesis feem ntau pib los ntawm indigo carmine anhydride, uas yog tom qab ntawd nitration kom tau 5-nitroindigo carmine anhydride. Qhov tseem ceeb nruab nrab yog tom qab sib txuas los ntawm kev txo qis, acetylation, thiab lwm cov kauj ruam los ua fluoroquinolone thaum kawg.

Kev tshawb fawb thiab kev loj hlob ntawm cov tshuaj tiv thaiv tuberculosis: 5-nitroindigo carmine muaj peev xwm siv tau rau hauv kev tshawb fawb thiab kev loj hlob ntawm cov tshuaj tiv thaiv tuberculosis. Piv txwv li, nws cov derivatives tuaj yeem ua cov tshuaj tiv thaiv tuberculosis, siv cov tshuaj kho mob los ntawm inhibiting kev loj hlob lossis kev loj hlob ntawm Mycobacterium tuberculosis.

Kev tshawb nrhiav thiab kev txhim kho cov tshuaj tiv thaiv kab mob HIV: 5-nitroindigo carmine thiab nws cov derivatives tau pom muaj peev xwm hauv kev txhim kho cov tshuaj tiv thaiv HIV. Los ntawm kev hloov kho cov qauv, cov tebchaw tshiab nrog kev tiv thaiv HIV yuav raug tsim, muab cov kev xaiv tshiab rau kev kho mob AIDS.

Cov tshuaj Antispasmodic: Ntxiv nrog rau fluoroquinolone, 5-nitroindigo kuj tuaj yeem siv los ua ke rau lwm cov tshuaj antispasmodic, uas txo cov leeg nqaij los ntawm kev tswj cov neurotransmitters lossis ion channels.

Tshuaj architecture
Lub synthesis ntawm spiro [indole-thiazol-4-ib]: 5-nitroindigo yog ib qho tseem ceeb nruab nrab rau cov synthesis ntawm spiro [indole-thiazol-4-one]. Spiro [indole-thiazol-4-one] yog ib qho chaw uas muaj peev xwm ua haujlwm lom neeg, uas tej zaum yuav muaj cov kab mob tua kab mob, tshuaj tua kab mob, lossis tshuaj tiv thaiv qog.

Enzyme inhibitor
Glutamine transferase inhibitors: 5-nitroindigo thiab nws cov derivatives tuaj yeem ua glutamine transferase inhibitors rau kev kho mob ntawm cov kab mob cuam tshuam nrog cov metabolism hauv glutamine.
Acetylcholinesterase inhibitors: Los ntawm kev hloov kho cov qauv, 5-nitroindigo tuaj yeem tsim cov tshuaj sib xyaw nrog acetylcholinesterase inhibitory kev ua haujlwm rau kev kho cov kab mob neurodegenerative xws li Alzheimer's disease.

2. Cov tshuaj tiv thaiv kab mob

5-nitroindigo derivatives tau tsim los ua cov tshuaj tiv thaiv kab mob tiv thaiv kab mob xws li Mycobacterium tuberculosis. Cov nitro thiab indole rings nyob rau hauv nws cov qauv molecular muaj peev xwm tsim hydrogen bonds los yog π - π stacking kev sib cuam tshuam nrog lub hom phiaj proteins, pab txhawb kev affinity ntawm cov tshuaj nrog cov kab mob. Los ntawm kev siv computer-aided tshuaj tsim (CADD) thev naus laus zis, nws muaj peev xwm kwv yees nws txoj kev sib txuas nrog cov enzymes tseem ceeb hauv mycobacteria thiab qhia kev txhim kho cov qauv.

3. Cov tshuaj tiv thaiv spasmodic

5-Nitroindigo carmine yog ib qho tseem ceeb nruab nrab ntawm cov nqaij ntshiv fluoroquinolone. Fluoroquinolone yog tsim los ntawm Tanabe Corporation nyob rau hauv Nyiv thiab yog siv los kho lub ntsej muag thiab caj dab spasms. Txoj kev sib txuas siv indigo anhydride ua raw khoom, uas yog tom qab ntawd nitration los tsim 5-nitroindigo anhydride. Qhov tseem ceeb nruab nrab N - (2-amino-5-acetamidobenzoyl) ortho toluidine yog tau los ntawm kev txo qis, acetylation, thiab lwm yam, thiab thaum kawg fluoroquinolone yog synthesized. Daim ntawv thov kev kho mob ntawm cov tshuaj no tau ua pov thawj nws txoj kev kho mob tseem ceeb ntawm lub ntsej muag nqaij spasms.

4. Tib neeg Glutamine Transferase Inhibitors

5-Nitroisatinderivatives tau tsim los ua glutamine transferase inhibitors, uas tuaj yeem cuam tshuam cov glutamine metabolism hauv cov qog hlwb, thaiv lawv lub zog thiab biosynthesis. Hom tshuaj inhibitor no muaj peev xwm siv tau rau hauv kev txhim kho cov tshuaj tiv thaiv -cov qog nqaij hlav, tshwj xeeb tshaj yog rau cov qog nqaij hlav glutamine.

Tshuaj tua kab:
Qee qhov 5-nitroindigo derivatives nthuav tawm cov tshuaj tua kab, tejzaum nws cuam tshuam nrog cov kab mob hauv lub paj hlwb lossis lub zog metabolism hauv txoj hauv kev. Cov nitro thiab indole rings nyob rau hauv nws cov qauv molecular tuaj yeem khi rau cov kab mob parasitic cov proteins, thaiv cov kev taw qhia tseem ceeb.

6. Tshuaj tiv thaiv kab mob HIV

Hauv kev tsim cov tshuaj tiv thaiv kab mob HIV, 5-nitroindigo derivatives yog tsim los ua thim rov qab transcriptase inhibitors lossis integrase inhibitors. Los ntawm kev txhim kho cov txheej txheem, nws lub hom phiaj thiab kev tiv thaiv kev tiv thaiv kab mob HIV tuaj yeem txhim kho, thiab nws cov tshuaj lom tuaj yeem txo.

7. Cov tshuaj tiv thaiv kab mob
Rau kev kho mob tuberculosis, 5-nitroindigo derivatives tuaj yeem ua lub luag haujlwm los ntawm inhibiting cov enzymes tseem ceeb ntawm Mycobacterium tuberculosis lossis cuam tshuam nrog cell phab ntsa synthesis. Nitro thiab indole rings hauv nws cov qauv molecular tuaj yeem txhim kho kev sib cuam tshuam ntawm cov tshuaj thiab cov hom phiaj, txhim kho kev ua haujlwm ntawm cov kab mob.

8. Acetylcholinesterase inhibitors
5-nitroindigo derivatives tau tsim los ua acetylcholinesterase inhibitors thiab tuaj yeem siv los kho cov kab mob neurodegenerative xws li Alzheimer's disease. Cov inhibitors no txhim kho kev txawj ntse los ntawm inhibiting acetylcholinesterase kev ua haujlwm, nce qib synaptic acetylcholine.

9. Muaj peev xwm tiv thaiv tuberculosis
Ntxiv nrog rau kev ua haujlwm ncaj qha los tiv thaiv kab mob, 5-nitroindigo derivatives kuj tseem tuaj yeem tiv thaiv kab mob tiv thaiv kab mob los ntawm kev txhim kho lub cev tiv thaiv kab mob los yog cuam tshuam nrog kev ua phem ntawm Mycobacterium tuberculosis.

1. Spiro [indole-thiazol-4-one] skeleton
5-nitroindigo yog ib qho tseem ceeb precursor rau tsim complex heterocyclic compounds xws li spiro [indole-thiazol-4-one]. Hom pob txha no muaj dav nyob rau hauv cov khoom ntuj tsim thiab bioactive molecules, nrog rau ntau yam kev ua ub no xws li tshuaj tua kab mob, tiv thaiv qog, tiv thaiv kab mob, thiab lwm yam.

2. Synthesis ntawm heterocyclic compounds
Los ntawm cov tswv yim xws li cyclization cov tshuaj tiv thaiv thiab kev hloov pauv nucleophilic, 5-nitroindigo tuaj yeem hloov mus rau ntau yam nitrogen-muaj heterocyclic compounds. Piv txwv li, nws muaj peev xwm hnov ​​​​mob nrog amine tebchaw los tsim indole amine derivatives, uas muaj peev xwm ua rau lom.

3. Dyes thiab pigments
5-nitroindigo thiab nws cov derivatives tuaj yeem siv rau kev sib txuas ntawm cov organic dyes thiab pigments. Lub conjugated system nyob rau hauv nws cov qauv molecular endows nws nrog zoo heev lub teeb absorption zog, ua rau nws haum rau teb xws li textiles thiab inks.

4. Fluorescent sojntsuam
Los ntawm kev qhia cov pab pawg fluorescent, 5-nitroindigo derivatives tuaj yeem tsim los ua fluorescent probes rau thaj chaw xws li kev kuaj ntshav thiab kev saib xyuas ib puag ncig. Nws txoj kev ua haujlwm fluorescence tuaj yeem tswj tau los ntawm kev hloov kho cov qauv molecular.

5. Cov khoom siv ua haujlwm
5-nitroindigo derivatives muaj peev xwm siv tau hauv kev ua haujlwm ntawm cov khoom siv, xws li cov khoom siv thauj khoom hluav taws xob, cov khoom siv kho qhov muag tsis zoo, thiab lwm yam. Lub nplhaib nitro thiab indole hauv nws cov qauv molecular tuaj yeem muab cov chaw txais hluav taws xob thiab cov chaw pub dawb, txhim kho cov khoom siv hluav taws xob optoelectronic.

1. Kev tshawb fawb txog cov protein-protein kev sib cuam tshuam
5-Nitroindigo derivatives tuaj yeem siv los ua kev sojntsuam molecules rau kev kawm txog kev sib cuam tshuam ntawm cov protein-protein. Nitro thiab indole rings nyob rau hauv nws cov qauv molecular tuaj yeem tsim tshwj xeeb khi nrog lub hom phiaj protein, thiab kev sib cuam tshuam tuaj yeem tshawb pom los ntawm cov tswv yim xws li fluorescence resonance zog hloov (FRET).

2. Enzyme kev ua haujlwm inhibition
5-nitroindigo derivatives tuaj yeem tsim los ua kev sib tw lossis tsis muaj kev sib tw inhibitors tsom rau cov chaw tshwj xeeb enzyme. Hom inhibitor no muaj nuj nqis tseem ceeb hauv kev tshawb fawb enzymatic thiab kev tsim tshuaj.

3. Kev tswj cov kev taw qhia ntawm tes
Los ntawm kev cuam tshuam cov kev ua ntawm intracellular signaling molecules,5-Nitroisatinderivatives tuaj yeem tswj cov txheej txheem xws li cell proliferation, sib txawv, thiab apoptosis. Nitro thiab indole rings nyob rau hauv nws cov qauv molecular muaj peev xwm cuam tshuam nrog cov teeb liab molecules thiab cuam tshuam cov teeb liab transduction txoj kev.