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The design and discovery of novel amide CCR5 antagonists |
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| Authors: | David C Pryde Martin Corless David R Fenwick Helen J Mason Blanda C Stammen Peter T Stephenson David Ellis David Bachelor David Gordon Christopher G Barber Anthony Wood Donald S Middleton David C Blakemore Gemma C Parsons Rachel Eastwood Michelle Y Platts Keith Statham Kerry A Paradowski Catherine Burt Wolfgang Klute |
| Institution: | Department of Chemistry, Pfizer Global Research and Development, Ramsgate Road, Sandwich, Kent CT13 9NJ, UK |
| Abstract: | The synthesis of a range of novel amine-containing structures and their primary potency as inhibitors of HIV-1 fusion via blocking of the CCR5 receptor is described. The development of the medicinal chemistry strategy and SAR’s which led to the identification of the piperidine amide compounds 33 and 36 as excellent leads for further evaluation is described, along with key physicochemical data which highlighted their lead potential. |
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