title: Optimization of diarylamines as non-nucleoside inhibitors of HIV-1 reverse transcriptase.
abstract: Following computational analyses, potential non-nucleoside inhibitors of HIV-1 reverse transcriptase have been pursued through synthesis and assaying for anti-viral activity. The general class Het-NH-Ph-U has been considered, where Het is an aromatic heterocycle and U is an unsaturated, hydrophobic group. Results for compounds with Het=2-thiazoyl and 2-pyrimidinyl are the focus of this report.
authors.affiliation: Department of Chemistry, Yale University, New Haven, CT 06520-8107, USA.
authors.forename: Juliana
authors.initials: J
authors.lastname: Ruiz-Caro
authors.forename: Aravind
authors.initials: A
authors.lastname: Basavapathruni
authors.forename: Joseph T
authors.initials: JT
authors.lastname: Kim
authors.forename: Christopher M
authors.initials: CM
authors.lastname: Bailey
authors.forename: Ligong
authors.initials: L
authors.lastname: Wang
authors.forename: Karen S
authors.initials: KS
authors.lastname: Anderson
authors.forename: Andrew D
authors.initials: AD
authors.lastname: Hamilton
authors.forename: William L
authors.initials: WL
authors.lastname: Jorgensen
mesh_terms: D000588:Amines / Q000737:chemistry* / Q000494:pharmacology; D024921:Drug Resistance, Multiple, Viral; D015658:HIV Infections / Q000188:drug therapy / Q000821:virology; D054303:HIV Reverse Transcriptase / Q000037:antagonists & inhibitors*; D006571:Heterocyclic Compounds / Q000737:chemistry; D057927:Hydrophobic and Hydrophilic Interactions; D011743:Pyrimidines / Q000737:chemistry; D018894:Reverse Transcriptase Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D013329:Structure-Activity Relationship; D013844:Thiazoles / Q000737:chemistry
chemical_list: D000588:Amines; D006571:Heterocyclic Compounds; D011743:Pyrimidines; D018894:Reverse Transcriptase Inhibitors; D013844:Thiazoles; D054303:HIV Reverse Transcriptase