title: Pyrazole NNRTIs 1: design and initial optimisation of a novel template.
abstract: The design and synthesis of a novel series of non-nucleoside HIV reverse transcriptase inhibitors (NNRTIs) based on a pyrazole template is described. These compounds are active against wild type reverse transcriptase (RT) and retain activity against clinically important mutants.
authors.affiliation: Department of Discovery Chemistry, Pfizer Global Research and Development, Ramsgate Road, Sandwich, Kent CT13 9NJ, UK. Charles.Mowbray@Pfizer.Com
authors.forename: Charles E
authors.initials: CE
authors.lastname: Mowbray
authors.forename: Catherine
authors.initials: C
authors.lastname: Burt
authors.forename: Romuald
authors.initials: R
authors.lastname: Corbau
authors.forename: Manos
authors.initials: M
authors.lastname: Perros
authors.forename: Isabelle
authors.initials: I
authors.lastname: Tran
authors.forename: Paul A
authors.initials: PA
authors.lastname: Stupple
authors.forename: Rob
authors.initials: R
authors.lastname: Webster
authors.forename: Anthony
authors.initials: A
authors.lastname: Wood
mesh_terms: D019380:Anti-HIV Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D015195:Drug Design; D054303:HIV Reverse Transcriptase / Q000037:antagonists & inhibitors* / Q000378:metabolism; D006801:Humans; D008862:Microsomes, Liver / Q000378:metabolism; D011720:Pyrazoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D018894:Reverse Transcriptase Inhibitors / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D013329:Structure-Activity Relationship
chemical_list: D019380:Anti-HIV Agents; D011720:Pyrazoles; D018894:Reverse Transcriptase Inhibitors; C031280:pyrazole; C514824:reverse transcriptase, Human immunodeficiency virus 1; D054303:HIV Reverse Transcriptase