psammaplin-a and Trypanosomiasis--African

psammaplin-a has been researched along with Trypanosomiasis--African* in 2 studies

Other Studies

2 other study(ies) available for psammaplin-a and Trypanosomiasis--African

Article	Year
The marine sponge Diacarnus bismarckensis as a source of peroxiterpene inhibitors of Trypanosoma brucei, the causative agent of sleeping sickness. Journal of natural products, 2009, Feb-27, Volume: 72, Issue:2 Human African trypanosomiasis, also known as African sleeping sickness, is a neglected tropical disease with inadequate therapeutic options. We have launched a collaborative new lead discovery venture using our repository of extracts and natural product compounds as input into our growth inhibition primary screen against Trypanosoma brucei. Careful evaluation of the spectral data of the natural products and derivatives allowed for the elucidation of the absolute configuration (using the modified Mosher's method) of two new peroxiterpenes: (+)-muqubilone B (1a) and (-)-ent-muqubilone (3a). Five known compounds were also isolated: (+)-sigmosceptrellin A (4a), (+)-sigmosceptrellin A methyl ester (4b), (-)-sigmosceptrellin B (5), (+)-epi-muqubillin A (6), and (-)-epi-nuapapuin B methyl ester (7). The isolated peroxiterpenes demonstrated activities in the range IC(50) = 0.2-2 mug/mL. Topics: Animals; Humans; Marine Biology; Molecular Structure; Parasitic Sensitivity Tests; Peroxides; Porifera; Stereoisomerism; Terpenes; Trypanosoma brucei brucei; Trypanosomiasis, African	2009
Identification of novel inhibitors of UDP-Glc 4'-epimerase, a validated drug target for african sleeping sickness. Bioorganic & medicinal chemistry letters, 2006, Nov-15, Volume: 16, Issue:22 Novel inhibitors of Trypanosoma brucei and mammalian UDP-Glc 4'-epimerase were identified by screening a small library of natural products and commercially available drug-like molecules. The inhibitors possess low micromolar potency against the T. brucei and human enzymes in vitro, display a degree of selectivity between the two enzymes, and are cytotoxic to cultured T. brucei and mammalian cells. Topics: Animals; Enzyme Inhibitors; Humans; Models, Chemical; Trypanocidal Agents; Trypanosoma brucei brucei; Trypanosomiasis, African; UDPglucose 4-Epimerase	2006

Article

Year

The marine sponge Diacarnus bismarckensis as a source of peroxiterpene inhibitors of Trypanosoma brucei, the causative agent of sleeping sickness.

Journal of natural products, 2009, Feb-27, Volume: 72, Issue:2

Human African trypanosomiasis, also known as African sleeping sickness, is a neglected tropical disease with inadequate therapeutic options. We have launched a collaborative new lead discovery venture using our repository of extracts and natural product compounds as input into our growth inhibition primary screen against Trypanosoma brucei. Careful evaluation of the spectral data of the natural products and derivatives allowed for the elucidation of the absolute configuration (using the modified Mosher's method) of two new peroxiterpenes: (+)-muqubilone B (1a) and (-)-ent-muqubilone (3a). Five known compounds were also isolated: (+)-sigmosceptrellin A (4a), (+)-sigmosceptrellin A methyl ester (4b), (-)-sigmosceptrellin B (5), (+)-epi-muqubillin A (6), and (-)-epi-nuapapuin B methyl ester (7). The isolated peroxiterpenes demonstrated activities in the range IC(50) = 0.2-2 mug/mL.

Topics: Animals; Humans; Marine Biology; Molecular Structure; Parasitic Sensitivity Tests; Peroxides; Porifera; Stereoisomerism; Terpenes; Trypanosoma brucei brucei; Trypanosomiasis, African

2009

Identification of novel inhibitors of UDP-Glc 4'-epimerase, a validated drug target for african sleeping sickness.

Bioorganic & medicinal chemistry letters, 2006, Nov-15, Volume: 16, Issue:22

Novel inhibitors of Trypanosoma brucei and mammalian UDP-Glc 4'-epimerase were identified by screening a small library of natural products and commercially available drug-like molecules. The inhibitors possess low micromolar potency against the T. brucei and human enzymes in vitro, display a degree of selectivity between the two enzymes, and are cytotoxic to cultured T. brucei and mammalian cells.

Topics: Animals; Enzyme Inhibitors; Humans; Models, Chemical; Trypanocidal Agents; Trypanosoma brucei brucei; Trypanosomiasis, African; UDPglucose 4-Epimerase

2006