title: Synthesis of pyrryl aryl sulfones targeted at the HIV-1 reverse transcriptase.
abstract: Various aryl 1-pyrryl sulfones were synthesized and tested as inhibitors of HIV-1. 2-Nitrophenyl-2-ethoxycarbonyl-1-pyrryl sulfone, the most active among test derivatives, was selected as lead compound of the aryl pyrryl sulfone series. The in vitro anti-HIV-1 activity and cytotoxicity of 41 compounds is reported. Some structure-activity relationships are discussed also in comparison with the known NPPS (2-nitrophenyl phenyl sulfone).
authors.affiliation: Dipartimento di Studi Farmaceutici, Università di Roma, La Sapienza, Italy.
authors.forename: M
authors.initials: M
authors.lastname: Artico
authors.forename: R
authors.initials: R
authors.lastname: Silvestri
authors.forename: G
authors.initials: G
authors.lastname: Stefancich
authors.forename: S
authors.initials: S
authors.lastname: Massa
authors.forename: E
authors.initials: E
authors.lastname: Pagnozzi
authors.forename: D
authors.initials: D
authors.lastname: Musu
authors.forename: F
authors.initials: F
authors.lastname: Scintu
authors.forename: E
authors.initials: E
authors.lastname: Pinna
authors.forename: E
authors.initials: E
authors.lastname: Tinti
authors.forename: P
authors.initials: P
authors.lastname: La Colla
mesh_terms: D002470:Cell Survival / Q000187:drug effects; D054303:HIV Reverse Transcriptase; D015497:HIV-1 / Q000187:drug effects / Q000201:enzymology*; D015498:HIV-2 / Q000187:drug effects / Q000201:enzymology; D006801:Humans; D011758:Pyrroles / Q000138:chemical synthesis* / Q000494:pharmacology; D018894:Reverse Transcriptase Inhibitors; D013329:Structure-Activity Relationship; D013450:Sulfones / Q000138:chemical synthesis* / Q000494:pharmacology
chemical_list: D011758:Pyrroles; D018894:Reverse Transcriptase Inhibitors; D013450:Sulfones; D054303:HIV Reverse Transcriptase