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Imidazo[1,2-a]pyridines as NNRTIs

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dc.contributor.author Bode, ML
dc.contributor.author Gravestock, D
dc.contributor.author Moleele, S
dc.contributor.author Van der Westhuyzen, Christiaan W
dc.contributor.author Hoppe, H
dc.contributor.author Khan, T
dc.contributor.author Pelly, SC
dc.date.accessioned 2010-10-04T11:57:18Z
dc.date.available 2010-10-04T11:57:18Z
dc.date.issued 2010-01
dc.identifier.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 en
dc.identifier.uri http://hdl.handle.net/10204/4441
dc.description 11th Frank Warren Conference of the South African Chemical Institute. Pietermaritzburg, South Africa, 17-21 January 2010 en
dc.description.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. en
dc.language.iso en en
dc.subject Imidazo[1,2-a]pyridines en
dc.subject Allosteric site en
dc.subject Nucleoside reserve transcriptase inhibitors en
dc.subject NRTI en
dc.subject Cell based anti HIV MAGI assay en
dc.subject Structural elements en
dc.subject Reverse transcriptase en
dc.subject RT en
dc.title Imidazo[1,2-a]pyridines as NNRTIs en
dc.type Conference Presentation en
dc.identifier.apacitation Bode, 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/10204/4441 en_ZA
dc.identifier.chicagocitation Bode, 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/10204/4441 en_ZA
dc.identifier.vancouvercitation Bode 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 . en_ZA
dc.identifier.ris 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 - en_ZA


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