title: Comparison of the non-nucleoside reverse transcriptase inhibitor lersivirine with its pyrazole and imidazole isomers.
abstract: Lersivirine is a potent non-nucleoside reverse transcriptase inhibitor with exceptional mutant resilience. Here, we compare the pharmacological and pharmacokinetic profile of lersivirine with its pyrazole and imidazole isomers and briefly explore the profile of these series. This work establishes lersivirine as the outstanding molecule in this set.
authors.forename: Lyn H
authors.initials: LH
authors.lastname: Jones
authors.forename: Gill
authors.initials: G
authors.lastname: Allan
authors.forename: Romuald
authors.initials: R
authors.lastname: Corbau
authors.forename: Donald S
authors.initials: DS
authors.lastname: Middleton
authors.forename: Charles E
authors.initials: CE
authors.lastname: Mowbray
authors.forename: Sandra D
authors.initials: SD
authors.lastname: Newman
authors.forename: Chris
authors.initials: C
authors.lastname: Phillips
authors.forename: Rob
authors.initials: R
authors.lastname: Webster
authors.forename: Mike
authors.initials: M
authors.lastname: Westby
mesh_terms: D000818:Animals; D015195:Drug Design; D015658:HIV Infections / Q000188:drug therapy / Q000821:virology; D054303:HIV Reverse Transcriptase / Q000037:antagonists & inhibitors* / Q000378:metabolism; D015497:HIV-1 / Q000187:drug effects / Q000201:enzymology / Q000235:genetics; D006801:Humans; D007093:Imidazoles / Q000737:chemistry / Q000493:pharmacokinetics*; D008862:Microsomes, Liver / Q000187:drug effects* / Q000201:enzymology; D008958:Models, Molecular; D009154:Mutation; D009570:Nitriles / Q000737:chemistry / Q000493:pharmacokinetics*; D011720:Pyrazoles / Q000737:chemistry / Q000493:pharmacokinetics*; D051381:Rats; D018894:Reverse Transcriptase Inhibitors / Q000737:chemistry / Q000493:pharmacokinetics*; D013329:Structure-Activity Relationship
chemical_list: D007093:Imidazoles; D009570:Nitriles; D011720:Pyrazoles; D018894:Reverse Transcriptase Inhibitors; C531151:UK 453,061; D054303:HIV Reverse Transcriptase