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Literature summary for 1.8.1.12 extracted from

  • Blackie, M.A.; Saravanamuthu, A.; Fairlamb, A.H.; Chibale, K.
    Inhibition of trypanothione reductase and glutathione reductase by ferrocenic 4-aminoquinoline ureas (2008), ARKIVOC, 2008, 52-60.
No PubMed abstract available
Search for more literature for 1.8.1.12

Application

Application Comment Organism
medicine promising TryR inhibitors Leishmania donovani
medicine promising TryR inhibitors Trypanosoma cruzi
medicine promising TryR inhibitors Trypanosoma brucei rhodesiense

Inhibitors

Inhibitors Comment Organism Structure
1-[2-(7-chloro-quinolin-4-ylamino)-ethyl]-1-[2-(N'',N''-dimethyl-aminomethyl)-ferrocenylmethyl]-3-p-chloro-phenyl-urea ferrocenic 4-aminoquinoline urea compound 9, growth inhibition Leishmania donovani
1-[2-(7-chloro-quinolin-4-ylamino)-ethyl]-1-[2-(N'',N''-dimethyl-aminomethyl)-ferrocenylmethyl]-3-p-chloro-phenyl-urea ferrocenic 4-aminoquinoline urea compound 9, growth inhibition Trypanosoma brucei rhodesiense
1-[2-(7-chloro-quinolin-4-ylamino)-ethyl]-1-[2-(N'',N''-dimethyl-aminomethyl)-ferrocenylmethyl]-3-p-chloro-phenyl-urea ferrocenic 4-aminoquinoline urea compound 9, enzyme and growth inhibition Trypanosoma cruzi
1-[2-(7-chloro-quinolin-4-ylamino)-ethyl]-1-[2-(N'',N''-dimethyl-aminomethyl)ferrocenylmethyl]-3-[2,6-bis-(trifluoromethyl)-phenyl]-urea ferrocenic 4-aminoquinoline urea compound 8 Trypanosoma cruzi
1-[2-(7-chloro-quinolin-4-ylamino)-ethyl]-1-[2-(N'',N''-dimethylaminomethyl)-ferrocenylmethyl]-3-p-methoxyphenyl-urea ferrocenic 4-aminoquinoline urea compound 6, growth inhibition Leishmania donovani
1-[2-(7-chloro-quinolin-4-ylamino)-ethyl]-1-[2-(N'',N''-dimethylaminomethyl)-ferrocenylmethyl]-3-p-methoxyphenyl-urea ferrocenic 4-aminoquinoline urea compound 6, growth inhibition Trypanosoma brucei rhodesiense
1-[2-(7-chloro-quinolin-4-ylamino)-ethyl]-1-[2-(N'',N''-dimethylaminomethyl)-ferrocenylmethyl]-3-p-methoxyphenyl-urea ferrocenic 4-aminoquinoline urea compound 6, enzyme and growth inhibition Trypanosoma cruzi
1-[2-(7-chloro-quinolin-4-ylamino)-ethyl]-1-[2-(N'',N''-dimethylaminomethyl)-ferrocenylmethyl]-3-p-tolyl-urea ferrocenic 4-aminoquinoline urea compound 5 Trypanosoma cruzi
1-[2-(7-chloro-quinolin-4-ylamino)-ethyl]-1-[2-(N'',N''-dimethylaminomethyl)-ferrocenylmethyl]-3-[2,4-bis-(trifluoromethyl)-phenyl]-urea ferrocenic 4-aminoquinoline urea compound 7 Trypanosoma cruzi
3-benzyl-1-[2-(7-chloro-quinolin-4-ylamino)-ethyl]-1-[2-(N'',N''-dimethylaminomethyl)-ferrocenylmethyl]urea growth inhibition Leishmania donovani
3-benzyl-1-[2-(7-chloro-quinolin-4-ylamino)-ethyl]-1-[2-(N'',N''-dimethylaminomethyl)-ferrocenylmethyl]urea growth inhibition Trypanosoma brucei rhodesiense
3-benzyl-1-[2-(7-chloro-quinolin-4-ylamino)-ethyl]-1-[2-(N'',N''-dimethylaminomethyl)-ferrocenylmethyl]urea enzyme and growth inhibition Trypanosoma cruzi
3-Benzyl-1-[3-(7-chloro-quinolin-4-ylamino)-propyl]-1-[2-(N'',N''-dimethylaminomethyl)-ferrocenylmethyl]urea
-
 Trypanosoma cruzi
3-Benzyl-1-[4-(7-chloro-quinolin-4-ylamino)-butyl]-1-[2-(N'',N''-dimethylaminomethyl)-ferrocenylmethyl]urea
-
 Trypanosoma cruzi
3-Benzyl-1-[6-(7-chloro-quinolin-4-ylamino)-hexyl]-1-[2-(N'',N''-dimethylaminomethyl)-ferrocenylmethyl]urea
-
 Trypanosoma cruzi
benznidazole growth inhibition Trypanosoma cruzi
Chloroquine
-
 Trypanosoma cruzi
N-(7-Chloro-quinolin-4-yl)-N'-[2-(N'',N''-dimethyl-aminomethyl)ferrocenylmethyl]-butane-1,4-diamine
-
 Trypanosoma cruzi
N-(7-Chloro-quinolin-4-yl)-N'-[2-(N'',N''-dimethyl-aminomethyl)ferrocenylmethyl]-ethane-1,2-diamine enzyme and growth inhibition Trypanosoma cruzi
N-(7-Chloro-quinolin-4-yl)-N'-[2-(N'',N''-dimethyl-aminomethyl)ferrocenylmethyl]-hexane-1,6-diamine
-
 Trypanosoma cruzi
N-(7-Chloro-quinolin-4-yl)-N'-[2-(N'',N''-dimethyl-aminomethyl)ferrocenylmethyl]-propane-1,3-diamine
-
 Trypanosoma cruzi
N-(7-Chloro-quinolin-4-yl)-N'-[2-(N'',N''-dimethylaminomethyl)ferrocenylmethyl]-ethane-1,2-diamine growth inhibition Leishmania donovani
N-(7-Chloro-quinolin-4-yl)-N'-[2-(N'',N''-dimethylaminomethyl)ferrocenylmethyl]-ethane-1,2-diamine growth inhibition Trypanosoma brucei rhodesiense
Pentamidine growth inhibition Trypanosoma brucei rhodesiense
pentostam growth inhibition Leishmania donovani

Organism

Organism UniProt Comment Textmining
Leishmania donovani
-
-
-
Trypanosoma brucei rhodesiense
-
-
-
Trypanosoma cruzi
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
trypanothione + NADP+ using the recombinant enzyme Leishmania donovani trypanothione disulfide + NADPH + H+
-
 ?
trypanothione + NADP+ using the recombinant enzyme Trypanosoma cruzi trypanothione disulfide + NADPH + H+
-
 ?
trypanothione + NADP+ using the recombinant enzyme Trypanosoma brucei rhodesiense trypanothione disulfide + NADPH + H+
-
 ?

Synonyms

Synonyms Comment Organism
trypanothione reductase
-
 Trypanosoma cruzi
trypanothione reductase
-
 Trypanosoma brucei rhodesiense
trypanothione reductase TryR Leishmania donovani
TryR
-
 Trypanosoma cruzi
TryR
-
 Trypanosoma brucei rhodesiense

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.002
-
-
 Trypanosoma cruzi 1-[2-(7-chloro-quinolin-4-ylamino)-ethyl]-1-[2-(N'',N''-dimethyl-aminomethyl)ferrocenylmethyl]-3-[2,6-bis-(trifluoromethyl)-phenyl]-urea
0.0021
-
-
 Trypanosoma cruzi N-(7-Chloro-quinolin-4-yl)-N'-[2-(N'',N''-dimethyl-aminomethyl)ferrocenylmethyl]-hexane-1,6-diamine
0.0023
-
-
 Trypanosoma cruzi 1-[2-(7-chloro-quinolin-4-ylamino)-ethyl]-1-[2-(N'',N''-dimethylaminomethyl)-ferrocenylmethyl]-3-p-methoxyphenyl-urea
0.0024
-
-
 Trypanosoma cruzi 3-Benzyl-1-[6-(7-chloro-quinolin-4-ylamino)-hexyl]-1-[2-(N'',N''-dimethylaminomethyl)-ferrocenylmethyl]urea
0.0025
-
-
 Trypanosoma cruzi 1-[2-(7-chloro-quinolin-4-ylamino)-ethyl]-1-[2-(N'',N''-dimethyl-aminomethyl)-ferrocenylmethyl]-3-p-chloro-phenyl-urea
0.0027
-
-
 Trypanosoma cruzi N-(7-Chloro-quinolin-4-yl)-N'-[2-(N'',N''-dimethyl-aminomethyl)ferrocenylmethyl]-butane-1,4-diamine
0.0032
-
-
 Trypanosoma cruzi 3-Benzyl-1-[3-(7-chloro-quinolin-4-ylamino)-propyl]-1-[2-(N'',N''-dimethylaminomethyl)-ferrocenylmethyl]urea
0.0033
-
-
 Trypanosoma cruzi 3-Benzyl-1-[4-(7-chloro-quinolin-4-ylamino)-butyl]-1-[2-(N'',N''-dimethylaminomethyl)-ferrocenylmethyl]urea
0.0068
-
-
 Trypanosoma cruzi N-(7-Chloro-quinolin-4-yl)-N'-[2-(N'',N''-dimethyl-aminomethyl)ferrocenylmethyl]-propane-1,3-diamine
0.0105
-
-
 Trypanosoma cruzi 1-[2-(7-chloro-quinolin-4-ylamino)-ethyl]-1-[2-(N'',N''-dimethylaminomethyl)-ferrocenylmethyl]-3-[2,4-bis-(trifluoromethyl)-phenyl]-urea
0.015
-
-
 Trypanosoma cruzi 3-benzyl-1-[2-(7-chloro-quinolin-4-ylamino)-ethyl]-1-[2-(N'',N''-dimethylaminomethyl)-ferrocenylmethyl]urea
0.0476
-
-
 Trypanosoma cruzi N-(7-Chloro-quinolin-4-yl)-N'-[2-(N'',N''-dimethyl-aminomethyl)ferrocenylmethyl]-ethane-1,2-diamine