Triterpene based compounds with potent anti-maturation activity against HIV-1.
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.
Gerrish
David
D
Myriad Pharmaceuticals Inc., 320 Wakara Way, Salt Lake City, UT 84108, USA.
Kim
In Chul
IC
Kumar
Dange V
DV
Austin
Harry
H
Garrus
Jennifer E
JE
Baichwal
Vijay
V
Saunders
Michael
M
McKinnon
Rena S
RS
Anderson
Mark B
MB
Carlson
Robert
R
Arranz-Plaza
Esther
E
Yager
Kraig M
KM
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
D000577:Amides; D019380:Anti-HIV Agents; D000998:Antiviral Agents; D053978:Pentacyclic Triterpenes; D013729:Terpenes; D014315:Triterpenes; D000094062:Betulinic Acid