Non-peptidic HIV protease inhibitors: C2-symmetry-based design of bis-sulfonamide dihydropyrones.
Potent, non-peptidic, dihydropyrone sulfonamide HIV protease inhibitors have been previously described. Crystallographic analysis of dihydropyrone sulfonamide inhibitor/HIV protease complexes suggested incorporation of a second, C2 symmetry-related sulfonamide group. Selected bis-sulfonamide dihydropyrone analogues display high HIV protease inhibitory activity.
Janakiraman
M N
MN
Pharmacia & Upjohn, Inc., Kalamazoo, Michigan 49001, USA.
Watenpaugh
K D
KD
Tomich
P K
PK
Chong
K T
KT
Turner
S R
SR
Tommasi
R A
RA
Thaisrivongs
S
S
Strohbach
J W
JW
D019281:Dimerization; D015195:Drug Design; D016333:HIV Protease / Q000378:metabolism; D017320:HIV Protease Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D015497:HIV-1 / Q000201:enzymology; D007202:Indicators and Reagents; D008958:Models, Molecular; D008968:Molecular Conformation; D015394:Molecular Structure; D011753:Pyrones / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D013329:Structure-Activity Relationship; D013449:Sulfonamides / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology
D017320:HIV Protease Inhibitors; D007202:Indicators and Reagents; D011753:Pyrones; D013449:Sulfonamides; D016333:HIV Protease