Variations of the P2 group in HIV-1 protease inhibitors containing a tertiary alcohol in the transition-state mimicking scaffold

被引：16

作者：

Ekegren, Jenny K.

Gising, Johan

Wallberg, Hans

Larhed, Mats

Samuelsson, Bertil

Hallberg, Anders

机构：

[1] Uppsala Univ, BMC, Dept Med Chem, SE-75123 Uppsala, Sweden

[2] Medivir AB, SE-14144 Huddinge, Sweden

来源：

ORGANIC & BIOMOLECULAR CHEMISTRY | 2006年 / 4卷 / 16期

关键词：

D O I：

10.1039/b606859f

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

A short synthetic protocol leading to HIV-1 protease inhibitors with a tertiary alcohol based transition-state mimicking unit and different P2 side chains has been developed.

引用

页码：3040 / 3043

页数：4

共 16 条

[1]

BALANI SK, 1995, DRUG METAB DISPOS, V23, P266

[2] New aza-dipeptide analogues as potent and orally absorbed HIV-1 protease inhibitors:: Candidates for clinical development [J].

Bold, G ;

Fässler, A ;

Capraro, HG ;

Cozens, R ;

Klimkait, T ;

Lazdins, J ;

Mestan, J ;

Poncioni, B ;

Rösel, J ;

Stover, D ;

Tintelnot-Blomley, M ;

Acemoglu, F ;

Beck, W ;

Boss, E ;

Eschbach, M ;

Hürlimann, T ;

Masso, E ;

Roussel, S ;

Ucci-Stoll, K ;

Wyss, D ;

Lang, R .

JOURNAL OF MEDICINAL CHEMISTRY, 1998, 41 (18) :3387-3401

[3] HIV-1 protease: mechanism and drug discovery [J].

Brik, A ;

Wong, CH .

ORGANIC & BIOMOLECULAR CHEMISTRY, 2003, 1 (01) :5-14

[4]

Clavel F, 2004, NEW ENGL J MED, V350, P1023, DOI 10.1056/NEJM2ra025195

[5] New approaches toward anti-HIV chemotherapy [J].

De Clercq, E .

JOURNAL OF MEDICINAL CHEMISTRY, 2005, 48 (05) :1297-1313

[6]

de Mendoza C, 2004, CURR DRUG METAB, V5, P321

[7] L-735,524 - THE DESIGN OF A POTENT AND ORALLY BIOAVAILABLE HIV PROTEASE INHIBITOR [J].

DORSEY, BD ;

LEVIN, RB ;

MCDANIEL, SL ;

VACCA, JP ;

GUARE, JP ;

DARKE, PL ;

ZUGAY, JA ;

EMINI, EA ;

SCHLEIF, WA ;

QUINTERO, JC ;

LIN, JH ;

CHEN, IW ;

HOLLOWAY, MK ;

FITZGERALD, PMD ;

AXEL, MG ;

OSTOVIC, D ;

ANDERSON, PS ;

HUFF, JR .

JOURNAL OF MEDICINAL CHEMISTRY, 1994, 37 (21) :3443-3451

[8] Microwave-accelerated synthesis of p1′-extended HIV-1 protease inhibitors encompassing a tertiary alcohol in the transition-state mimicking scaffold [J].

Ekegren, JK ;

Ginman, N ;

Johansson, Å ;

Wallberg, H ;

Larhed, M ;

Samuelsson, B ;

Unge, T ;

Hallberg, A .

JOURNAL OF MEDICINAL CHEMISTRY, 2006, 49 (05) :1828-1832

[9] A new class of HIV-1 protease inhibitors containing a tertiary alcohol in the transition-state mimicking scaffold [J].

Ekegren, JK ;

Unge, T ;

Safa, MZ ;

Wallberg, H ;

Samuelsson, B ;

Hallberg, A .

JOURNAL OF MEDICINAL CHEMISTRY, 2005, 48 (25) :8098-8102

[10] Role of pharmacokinetics in the discovery and development of indinavir [J].

Lin, JH .

ADVANCED DRUG DELIVERY REVIEWS, 1999, 39 (1-3) :33-49

← 1 2 →