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Please use this identifier to cite or link to this item: http://hdl.handle.net/10204/4441

Title: Imidazo[1,2-a]pyridines as NNRTIs
Authors: Bode, ML
Gravestock, D
Moleele, S
Van Der Westhuyzen, CW
Hoppe, H
Khan, T
Pelly, SC
Keywords: Imidazo[1,2-a]pyridines
Allosteric site
Nucleoside reserve transcriptase inhibitors
NRTI
Cell based anti HIV MAGI assay
Structural elements
Reverse transcriptase
RT
Issue Date: Jan-2010
Citation: Bode, 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, pp
Abstract: 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.
Description: 11th Frank Warren Conference of the South African Chemical Institute. Pietermaritzburg, South Africa, 17-21 January 2010
URI: http://hdl.handle.net/10204/4441
Appears in Collections:General science, engineering & technology
Discovery chemistry

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