Dziwornu, Godwin Akpeko; Coertzen, Dina; Leshabane, Meta; Korkor, Constance M.; Cloete, Cleavon K.; Njoroge, Mathew; Gibhard, Liezl; Lawrence, Nina; Reader, Janette; van der Watt, Mariette; Wittlin, Sergio; Birkholtz, Lyn-Marie; Chibale, Kelly published their research in Journal of Medicinal Chemistry in 2021. The article was titled 《Antimalarial Benzimidazole Derivatives Incorporating Phenolic Mannich Base Side Chains Inhibit Microtubule and Hemozoin Formation: Structure-Activity Relationship and In Vivo Oral Efficacy Studies》.Formula: C7H5ClN2 The article contains the following contents:
A novel series of antimalarial benzimidazole derivatives incorporating phenolic Mannich base side chains at the C2 position, which possess dual asexual blood and sexual stage activities, is presented. Structure-activity relationship studies revealed that the 1-benzylbenzimidazole analogs possessed submicromolar asexual blood and sexual stage activities in contrast to the 1H-benzimidazole analogs, which were only active against asexual blood stage (ABS) parasites. Further, the former demonstrated microtubule inhibitory activity in ABS parasites but more significantly in stage II/III gametocytes. In addition to being bona fide inhibitors of hemozoin formation, the 1H-benzimidazole analogs also showed inhibitory effects on microtubules. In vivo efficacy studies in Plasmodium berghei-infected mice revealed that the frontrunner compound 41(I) exhibited high efficacy (98% reduction in parasitemia) when dosed orally at 4 × 50 mg/kg. Generally, the compounds were noncytotoxic to mammalian cells. In addition to this study using 2-Chloro-1H-benzo[d]imidazole, there are many other studies that have used 2-Chloro-1H-benzo[d]imidazole(cas: 4857-06-1Formula: C7H5ClN2) was used in this study.
2-Chloro-1H-benzo[d]imidazole(cas: 4857-06-1) binds to monoclonal antibodies, inhibiting their binding to their corresponding antigens. This activity may be due to its ability to bind covalently with amino groups on proteins and other molecules.Formula: C7H5ClN2
Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem