title: Triterpene based compounds with potent anti-maturation activity against HIV-1.
abstract: Efforts towards developing orally bioavailable HIV-1 maturation inhibitors starting from betulinic acid 1 are described. SAR resulted in improved potency, physicochemical properties, and enhanced oral absorption in rats.
authors.affiliation: Myriad Pharmaceuticals Inc., 320 Wakara Way, Salt Lake City, UT 84108, USA.
authors.forename: David
authors.initials: D
authors.lastname: Gerrish
authors.forename: In Chul
authors.initials: IC
authors.lastname: Kim
authors.forename: Dange V
authors.initials: DV
authors.lastname: Kumar
authors.forename: Harry
authors.initials: H
authors.lastname: Austin
authors.forename: Jennifer E
authors.initials: JE
authors.lastname: Garrus
authors.forename: Vijay
authors.initials: V
authors.lastname: Baichwal
authors.forename: Michael
authors.initials: M
authors.lastname: Saunders
authors.forename: Rena S
authors.initials: RS
authors.lastname: McKinnon
authors.forename: Mark B
authors.initials: MB
authors.lastname: Anderson
authors.forename: Robert
authors.initials: R
authors.lastname: Carlson
authors.forename: Esther
authors.initials: E
authors.lastname: Arranz-Plaza
authors.forename: Kraig M
authors.initials: KM
authors.lastname: Yager
mesh_terms: D000284:Administration, Oral; D000577:Amides / Q000737:chemistry; D000818:Animals; D019380:Anti-HIV Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D000998:Antiviral Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D002626:Chemistry, Pharmaceutical / Q000379:methods*; D015195:Drug Design; D015497:HIV-1 / Q000378:metabolism*; D006801:Humans; D020128:Inhibitory Concentration 50; D007963:Leukocytes, Mononuclear / Q000187:drug effects; D008956:Models, Chemical; D053978:Pentacyclic Triterpenes; D051381:Rats; D013729:Terpenes / Q000737:chemistry*; D014315:Triterpenes / Q000737:chemistry; D000094062:Betulinic Acid
chemical_list: D000577:Amides; D019380:Anti-HIV Agents; D000998:Antiviral Agents; D053978:Pentacyclic Triterpenes; D013729:Terpenes; D014315:Triterpenes; D000094062:Betulinic Acid