A new class of type I protein geranylgeranyltransferase (GGTase I) inhibitor.
Replacement of the thiol groups in 1, a potent and highly selective Candida albicans GGTase I inhibitor discovered through screening, with an imidazole ring was achieved by using solid phase synthesis. A non-thiol compound, 7, was found as a representative of a new class of potent C. albicans GGTase I inhibitor with high selectivity against human GGTase I.
Sunami
Satoshi
S
Banyu Tsukuba Research Institute, Okubo-3, Tsukuba 300-2611, Ibaraki, Japan. sunamist@banyu.co.jp
Ohkubo
Mitsuru
M
Sagara
Takeshi
T
Ono
Jun
J
Asahi
Shuichi
S
Koito
Seita
S
Morishima
Hajime
H
D000935:Antifungal Agents / Q000737:chemistry / Q000145:classification / Q000494:pharmacology; D002176:Candida albicans / Q000201:enzymology; D020650:Combinatorial Chemistry Techniques; D004151:Dipeptides; D004791:Enzyme Inhibitors / Q000737:chemistry / Q000145:classification / Q000494:pharmacology*; D006801:Humans; D007093:Imidazoles; D020128:Inhibitory Concentration 50; D013329:Structure-Activity Relationship
D000935:Antifungal Agents; D004151:Dipeptides; D004791:Enzyme Inhibitors; D007093:Imidazoles; C029899:imidazole