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Literature summary for 2.5.1.21 extracted from

  • Ishihara, T.; Kakuta, H.; Moritani, H.; Ugawa, T.; Yanagisawa, I.
    Synthesis and biological evaluation of novel propylamine derivatives as orally active squalene synthase inhibitors (2004), Bioorg. Med. Chem., 12, 5899-5908.
    View publication on PubMed

Application

Application Comment Organism
medicine 1-allyl-2-[3-(benzylamino)propoxy]-9H-carbazole shows 50% inhibition of enzyme at 63 nM, significant reduction of both plasma cholesterol and plasma triglyceride levels following oral dosing Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
1,3-diallyl-2-[3-(isopropylamino)propoxy]-9H-carbazole 50% inhibition at 250 nM Rattus norvegicus
1-allyl-2-(3-anilinopropoxy)-9H-carbazole 50% inhibition at above 0.001 mM nM Rattus norvegicus
1-allyl-2-[3-(benzylamino)propoxy]-9H-carbazole 50% inhibition at 63 nM Homo sapiens
1-allyl-2-[3-(benzylamino)propoxy]-9H-carbazole hydrochloride 50% inhibition at 150 nM Rattus norvegicus
1-allyl-2-[3-(cyclohexylamino)propoxy]-9H-carbazole 50% inhibition at 310 nM Rattus norvegicus
1-allyl-2-[3-(cyclopropylamino)propoxy]-9H-carbazole 50% inhibition at 230 nM Rattus norvegicus
1-allyl-2-[3-(isobutylamino)propoxy]-9H-carbazole 50% inhibition at 400 nM Rattus norvegicus
1-allyl-2-[3-(isopropylamino)propoxy]-9H-carbazole 50% inhibition at 32 nM Homo sapiens
1-allyl-2-[3-(isopropylamino)propoxy]-9H-carbazole 50% inhibition at 66 nM Rattus norvegicus
1-allyl-2-[3-(isopropylamino)propoxy]-9H-xanthen-9-one 50% inhibition at 120 nM Homo sapiens
1-allyl-2-[3-(isopropylamino)propoxy]-9H-xanthen-9-one 50% inhibition at 120 nM Rattus norvegicus
2-[3-(isopropylamino)propoxy]-1-ethyl-9H-carbazole 50% inhibition at 460 nM Rattus norvegicus
2-[3-(isopropylamino)propoxy]-9H-carbazole 50% inhibition at 810 nM Homo sapiens
2-[3-(isopropylamino)propoxy]-9H-carbazole 50% inhibition at 110 nM Rattus norvegicus
2-[[(2Z)-2-(1-azabicyclo(2.2.2)oct-3-ylidene)-2-fluoroethyl]oxy]-9H-carbazole i.e. YM-53601, 50% inhibition at 90 nM Rattus norvegicus
3-(4-quinolin-6-ylphenyl)quinuclidin-3-ol i.e. RPR107393, 50% inhibition at 57 nM Homo sapiens
3-(4-quinolin-6-ylphenyl)quinuclidin-3-ol i.e. RPR107393, 50% inhibition at 68 nM Rattus norvegicus
N-isopropyl-biphenyloxypropylamine 50% inhibition at 93 nM Rattus norvegicus

Organism

Organism UniProt Comment Textmining
Homo sapiens
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Rattus norvegicus
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Source Tissue

Source Tissue Comment Organism Textmining
Hep-G2 cell
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Homo sapiens
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hepatoma cell
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Homo sapiens
-