title: Tetrazole thioacetanilides: potent non-nucleoside inhibitors of WT HIV reverse transcriptase and its K103N mutant.
abstract: A series of aryltetrazolylacetanilides was synthesized and evaluated as HIV-1 non-nucleoside reverse transcriptase inhibitors on wild-type virus and on the clinically relevant K103N mutant strain. Extensive SAR investigation led to potent compounds, with nanomolar activity on K103N, and orally bioavailable in rats.
authors.affiliation: Department of Medicinal Chemistry, IRBM/MRL Rome, Via Pontina Km 30,600, 00040 Pomezia, Rome, Italy. Ester_Muraglia@merck.com
authors.forename: Ester
authors.initials: E
authors.lastname: Muraglia
authors.forename: Olaf D
authors.initials: OD
authors.lastname: Kinzel
authors.forename: Ralph
authors.initials: R
authors.lastname: Laufer
authors.forename: Michael D
authors.initials: MD
authors.lastname: Miller
authors.forename: Gregory
authors.initials: G
authors.lastname: Moyer
authors.forename: Vandna
authors.initials: V
authors.lastname: Munshi
authors.forename: Federica
authors.initials: F
authors.lastname: Orvieto
authors.forename: Maria Cecilia
authors.initials: MC
authors.lastname: Palumbi
authors.forename: Giovanna
authors.initials: G
authors.lastname: Pescatore
authors.forename: Michael
authors.initials: M
authors.lastname: Rowley
authors.forename: Peter D
authors.initials: PD
authors.lastname: Williams
authors.forename: Vincenzo
authors.initials: V
authors.lastname: Summa
mesh_terms: D000083:Acetanilides / Q000737:chemistry / Q000494:pharmacology*; D000818:Animals; D054303:HIV Reverse Transcriptase / Q000037:antagonists & inhibitors*; D015497:HIV-1 / Q000187:drug effects* / Q000201:enzymology / Q000235:genetics; D009154:Mutation; D051381:Rats; D018894:Reverse Transcriptase Inhibitors / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D000083:Acetanilides; D018894:Reverse Transcriptase Inhibitors; D054303:HIV Reverse Transcriptase; C039632:thioacetanilide