Megazol is a nitroimidazole based drug that cures some protozoan infections. A study of nitroimidazoles found the drug extremely effective against T. cruzi and T. brucei which cause Chagas disease and African sleeping sickness, respectively.
O-11 is an analog of the fully saturated, 14-carbon fatty acid myristic acid, in which the methylene group at position 11 is replaced with oxygen. It is highly effective and selective at killingTrypanosoma brucei, the protozoan parasite responsible for African sleeping sickness, exhibiting an LD50of less than 1 μM in a cell culture assay.1,2The toxic effects of O-11 appear to be caused by its ability to inhibit the incorporation of a single myristate into the GPI anchor of the variant surface glycoprotein (VSG), a protein critical for evading the host immune response.1O-11 exhibits essentially no anti-fungal activity when assayed usingC. neoformans, but does have a minor inhibitory effect on HIV-1 replication in T-lymphocytes.3 1.Doering, T.L., Raper, J., Buxbaum, L.U., et al.An analog of myristic acid with selective toxicity for African trypanosomesScience2521851-1854(1991) 2.Doering, T.L., Lu, T., Werbovetz, K.A., et al.Toxicity of myristic acid analogs toward African trypanosomesProceedings of the National Academy of Sciences of the United States of America919735-9739(1994) 3.Langner, C.A., Lodge, J.K., Travis, S.J., et al.4-Oxatetradecanoic acid is fungicidal for Cryptococcus neoformans and inhibits replication of human immunodeficiency virus IThe Journal of Biological Chemisty267(24)17159-17169(1992)
hCAI II-IN-2 (compound 2b) is a highly effective dual inhibitor of human carbonic anhydrase I and II (hCA I II), with Ki values of 40.97 nM, 15.15 nM, and 61.88 nM for hCA I, hCA II, and hCA IX, respectively. With its anti-hypoxic properties, hCAI II-IN-2 demonstrates activity against acute mountain sickness (AMS). Furthermore, this compound exhibits low cellular activity [1].
hCAI II-IN-4 (compound 6d) is a powerful inhibitor of both hCA I and hCA II enzymes, with Ki values of 16.95 nM and 15.22 nM, respectively. It demonstrates inhibitory activity against hCA IX with a Ki value of 27.04 nM. Additionally, hCAI II-IN-4 exhibits anti-hypoxia properties while maintaining low toxicity. This compound is suitable for investigating acute mountain sickness (AMS) in research studies [1].
hCAI II-IN-3 (compound 5b) is a highly effective dual inhibitor of hCA I II enzymes. It exhibits Ki values of 51.25, 13.15, and 42.18 nM for hCA I, hCA II, and hCA Ⅸ, respectively. hCAI II-IN-3 demonstrates anti-hypoxic properties against acute mountain sickness (AMS) and exhibits low cellular activity [1].
Cinnarizine clofibrate is a calcium channel protein inhibitor as well as an antihistamine channel blocker. The compound is a drug derivative of piperazine. Cinnarizine is used for the control of vomiting due to motion sickness. It acts by interfering with the signal transmission between vestibular apparatus of the inner ear and the vomiting centre of the hypothalamus