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Pyrantel and Oxantel Pamoate
Published in M. Lindsay Grayson, Sara E. Cosgrove, Suzanne M. Crowe, M. Lindsay Grayson, William Hope, James S. McCarthy, John Mills, Johan W. Mouton, David L. Paterson, Kucers’ The Use of Antibiotics, 2017
Pyrantel, E-1,4,5,6-tetrahydro-1-methyl-2-[2-(2-thienyl)vinyl]-pyrimidine, is an imidazothiazole-derived tetrahydropyrimidine. Its anthelmintic activity was first identified in 1966 (Austin et al., 1966). It has been used as a broad-spectrum anthelmintic in both veterinary and human medicine since the 1970s (Kopp et al., 2007b). In humans, it is clinically useful for therapy of three major nematode infections: hookworm (Ancylostoma duodenale and Necator americanus), roundworm (Ascaris lumbricoides), and pinworm (Enterobius vermicularis). In addition, pyrantel pamoate appears to have activity against Trichinella spiralis and Trichostrongylus spp. Pyrantel pamoate is available as a tablet (including chewable) or oral suspension; common preparations include Combantrin (Pfizer), Antiminth (Goerig), and Pyrantrin (Niemeth).
Imidazothiazole-based potent inhibitors of V600E-B-RAF kinase with promising anti-melanoma activity: biological and computational studies
Published in Journal of Enzyme Inhibition and Medicinal Chemistry, 2020
Hanan S. Anbar, Mohammed I. El-Gamal, Hamadeh Tarazi, Bong S. Lee, Hong R. Jeon, Dow Kwon, Chang-Hyun Oh
Based on our previous knowledge of inhibitory effect of imidazothiazole derivatives against V600E-B-RAF and RAF1 11,12, we decided to start our biological investigation with testing all the 34 final compounds against both kinases. The target compounds were tested at 1 µM concentration, and the compounds that produced promising inhibitory effect, more than 75% inhibition, were further tested in 10-dose mode to measure their IC50 values. The inhibition percentage and IC50 values are demonstrated in Table 1. The target compounds are generally more active against V600E-B-RAF than RAF1. A comparative computational study was carried out to investigate it.
Combining locoregional CAR-T cells, autologous + allogeneic tumor lysate vaccination and levamisole in treatment of glioblastoma
Published in Immunopharmacology and Immunotoxicology, 2022
Meric A. Altinoz, Alp Ozpinar, Emily Hacker, Aysel Ozpinar
Levamisole has been used in many countries since the 1970s as the most preferred member of the imidazothiazole anti-helminthics. Levamisole improves the chemotaxis properties of phagocytes and improves the activity of lymphocytes by regulating IgG and C3 activity and receptor binding properties [34]. It has been found that parenteral administration once every 3 days or once a week can stimulate the immune system more effectively, whereas long-term daily administration may suppress the immune system.