Bvumbi, Mpelegeng VVan der Westhuyzen, Christiaan WMmutlane, EMNgwane, A2022-01-032022-01-032021-07Bvumbi, M.V., Van der Westhuyzen, C.W., Mmutlane, E. & Ngwane, A. 2021. Riminophenazine derivatives as potential antituberculosis agents: Synthesis, biological, and electrochemical evaluations. <i>Molecules, 26(14).</i> http://hdl.handle.net/10204/122061420-3049https://doi.org/10.3390/molecules26144200http://hdl.handle.net/10204/12206A series of novel riminophenazine derivatives, having ionizable alkyl substituents at N-5 and a variety of substituents on the C-3 imino nitrogen, at C-8 and on the pendant aryl group, have been designed and synthesized. Preliminary investigations into the relationship between lipophilicity, redox potential, and antimycobacterial activity were conducted, using the in vitro activity against Mycobacterium tuberculosis H37Rv, mammalian cytotoxicity, and the redox potential of the compounds determined by cyclic voltammetry as measures. Results revealed an activity “cliff” associated with C-8 substitution (10l and 10m) that, along with defined redox activity, point to a new class of riminophenazines as potential anti-tuberculosis agents having reasonable activity (MIC99 ~1 µM).FulltextenRiminophenazinesAlkyl substituentDrug discoveryMycobacterium tuberculosisTuberculosisTBArticleBvumbi, M. V., Van der Westhuyzen, C. W., Mmutlane, E., & Ngwane, A. (2021). Riminophenazine derivatives as potential antituberculosis agents: Synthesis, biological, and electrochemical evaluations. <i>Molecules, 26(14)</i>, http://hdl.handle.net/10204/12206Bvumbi, Mpelegeng V, Christiaan W Van der Westhuyzen, EM Mmutlane, and A Ngwane "Riminophenazine derivatives as potential antituberculosis agents: Synthesis, biological, and electrochemical evaluations." <i>Molecules, 26(14)</i> (2021) http://hdl.handle.net/10204/12206Bvumbi MV, Van der Westhuyzen CW, Mmutlane E, Ngwane A. Riminophenazine derivatives as potential antituberculosis agents: Synthesis, biological, and electrochemical evaluations. Molecules, 26(14). 2021; http://hdl.handle.net/10204/12206.TY - Article AU - Bvumbi, Mpelegeng V AU - Van der Westhuyzen, Christiaan W AU - Mmutlane, EM AU - Ngwane, A AB - A series of novel riminophenazine derivatives, having ionizable alkyl substituents at N-5 and a variety of substituents on the C-3 imino nitrogen, at C-8 and on the pendant aryl group, have been designed and synthesized. Preliminary investigations into the relationship between lipophilicity, redox potential, and antimycobacterial activity were conducted, using the in vitro activity against Mycobacterium tuberculosis H37Rv, mammalian cytotoxicity, and the redox potential of the compounds determined by cyclic voltammetry as measures. Results revealed an activity “cliff” associated with C-8 substitution (10l and 10m) that, along with defined redox activity, point to a new class of riminophenazines as potential anti-tuberculosis agents having reasonable activity (MIC99 ~1 µM). DA - 2021-07 DB - ResearchSpace DP - CSIR J1 - Molecules, 26(14) KW - Riminophenazines KW - Alkyl substituent KW - Drug discovery KW - Mycobacterium tuberculosis KW - Tuberculosis KW - TB LK - https://researchspace.csir.co.za PY - 2021 SM - 1420-3049 T1 - Riminophenazine derivatives as potential antituberculosis agents: Synthesis, biological, and electrochemical evaluations TI - Riminophenazine derivatives as potential antituberculosis agents: Synthesis, biological, and electrochemical evaluations UR - http://hdl.handle.net/10204/12206 ER -25197