Bode, MLGravestock, DMoleele, SVan der Westhuyzen, Christiaan WHoppe, HKhan, TPelly, SC2010-10-042010-10-042010-01Bode, ML,Gravestock, D,Moleele, S, et al. 2010. Imidazo[1,2-a]pyridines as NNRTIs. 11th Frank Warren Conference of the South African Chemical Institute. Pietermaritzburg, South Africa, 17-21 January 2010, pphttp://hdl.handle.net/10204/444111th Frank Warren Conference of the South African Chemical Institute. Pietermaritzburg, South Africa, 17-21 January 2010The enzyme reverse transcriptase (RT) is a validated target for the development of anti-HIV drugs. Drugs acting against RT may act at either the catalytic site (NRTIs) or the allosteric site (NNRTIs). During random screening of a small in-house library of compounds, a sub-set of substituted imidazo[1,2-a]pyridines were found to be allosteric inhibitors of RT. A much larger library of these compounds was prepared in order to find compounds with improved RT activity. These compounds were prepared by the Groebke reaction, an example of which is shown in Scheme 1. The preparation of the compound library will be discussed, together with the results obtained from an enzymatic RT assay as well as a cell-based anti-HIV MAGI assay. Structural elements required for RT inhibition and in silico rationalisation of these results will also be addressed.enImidazo[1,2-a]pyridinesAllosteric siteNucleoside reserve transcriptase inhibitorsNRTICell based anti HIV MAGI assayStructural elementsReverse transcriptaseRTConference PresentationBode, M., Gravestock, D., Moleele, S., Van der Westhuyzen, C. W., Hoppe, H., Khan, T., & Pelly, S. (2010). Imidazo[1,2-a]pyridines as NNRTIs. http://hdl.handle.net/10204/4441Bode, ML, D Gravestock, S Moleele, Christiaan W Van der Westhuyzen, H Hoppe, T Khan, and SC Pelly. "Imidazo[1,2-a]pyridines as NNRTIs." (2010): http://hdl.handle.net/10204/4441Bode M, Gravestock D, Moleele S, Van der Westhuyzen CW, Hoppe H, Khan T, et al, Imidazo[1,2-a]pyridines as NNRTIs; 2010. http://hdl.handle.net/10204/4441 .TY - Conference Presentation AU - Bode, ML AU - Gravestock, D AU - Moleele, S AU - Van der Westhuyzen, Christiaan W AU - Hoppe, H AU - Khan, T AU - Pelly, SC AB - The enzyme reverse transcriptase (RT) is a validated target for the development of anti-HIV drugs. Drugs acting against RT may act at either the catalytic site (NRTIs) or the allosteric site (NNRTIs). During random screening of a small in-house library of compounds, a sub-set of substituted imidazo[1,2-a]pyridines were found to be allosteric inhibitors of RT. A much larger library of these compounds was prepared in order to find compounds with improved RT activity. These compounds were prepared by the Groebke reaction, an example of which is shown in Scheme 1. The preparation of the compound library will be discussed, together with the results obtained from an enzymatic RT assay as well as a cell-based anti-HIV MAGI assay. Structural elements required for RT inhibition and in silico rationalisation of these results will also be addressed. DA - 2010-01 DB - ResearchSpace DP - CSIR KW - Imidazo[1,2-a]pyridines KW - Allosteric site KW - Nucleoside reserve transcriptase inhibitors KW - NRTI KW - Cell based anti HIV MAGI assay KW - Structural elements KW - Reverse transcriptase KW - RT LK - https://researchspace.csir.co.za PY - 2010 T1 - Imidazo[1,2-a]pyridines as NNRTIs TI - Imidazo[1,2-a]pyridines as NNRTIs UR - http://hdl.handle.net/10204/4441 ER -