ISOPHTHALIC ACID-DERIVATIVES - AMINO-ACID SURROGATES FOR THE INHIBITION OF HIV-1 PROTEASE

被引：17

作者：

KALDOR, SW ^{[1
]}

DRESSMAN, BA ^{[1
]}

HAMMOND, M ^{[1
]}

APPELT, K ^{[1
]}

BURGESS, JA ^{[1
]}

LUBBEHUSEN, PP ^{[1
]}

MUESING, MA ^{[1
]}

HATCH, SD ^{[1
]}

WISKERCHEN, MA ^{[1
]}

BAXTER, AJ ^{[1
]}

机构：

[1] AGOURON PHARMACEUT INC,SAN DIEGO,CA 92121

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1995年 / 5卷 / 07期

关键词：

D O I：

10.1016/0960-894X(95)00102-Y

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Using the X-ray crystal structure of the inhibitor 1 complexed to HIV-1 protease, a new series of HIV-1 protease inhibitors was developed incorporating substituted isophthalic acid derivatives as amino acid surrogates. Through iterative structure-based design, the lead compound 2 was optimized to produce a variety of non-peptide HIV-1 protease inhibitors with significant antiviral activity. In contrast to 1, several members of this series exhibit significant oral absorption in animals.

引用

页码：721 / 726

页数：6

共 50 条

[21] STUDIES ON AMINO-ACID DERIVATIVES .6. REACTION OF METHOXYMETHYLENE MELDRUMS ACID WITH AMINO-ACID DERIVATIVES
CHIBA, T
SAKAKI, JI
KANEKO, C
YAKUGAKU ZASSHI-JOURNAL OF THE PHARMACEUTICAL SOCIETY OF JAPAN, 1986, 106 (02): : 154 - 157
[22] INHIBITION OF UREASE ACTIVITY BY HYDROXAMIC ACID-DERIVATIVES OF AMINO-ACIDS
KOBASHI, K
TAKEBE, S
TERASHIMA, N
HASE, J
JOURNAL OF BIOCHEMISTRY, 1975, 77 (04): : 837 - 843
[23] POTENTIAL ANTI-AIDS NAPHTHALENESULFONIC ACID-DERIVATIVES - SYNTHESIS AND INHIBITION OF HIV-1 INDUCED CYTOPATHOGENESIS AND HIV-1 AND HIV-2 REVERSE-TRANSCRIPTASE ACTIVITIES
TAN, GT
WICKRAMASINGHE, A
VERMA, S
SINGH, R
HUGHES, SH
PEZZUTO, JM
BABA, M
MOHAN, P
JOURNAL OF MEDICINAL CHEMISTRY, 1992, 35 (26) : 4846 - 4853
[24] AN AMINO-TERMINAL AMINO-ACID AFFECTS THE ELECTROPHORETIC MOBILITY OF THE HIV-1 NEF PROTEIN
OBARU, K
DECLUE, JE
HASELTINE, WA
JOURNAL OF ACQUIRED IMMUNE DEFICIENCY SYNDROMES AND HUMAN RETROVIROLOGY, 1992, 5 (03): : 308 - 312
[25] COMPETITIVE-INHIBITION OF HIV-1 PROTEASE BY WARFARIN DERIVATIVES
TUMMINO, PJ
FERGUSON, D
HUPE, D
BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS, 1994, 201 (01) : 290 - 294
[26] REGULATION OF AUTOPROTEOLYSIS OF THE HIV-1 AND HIV-2 PROTEASES WITH ENGINEERED AMINO-ACID SUBSTITUTIONS
ROSE, JR
SALTO, R
CRAIK, CS
JOURNAL OF BIOLOGICAL CHEMISTRY, 1993, 268 (16) : 11939 - 11945
[27] STRUCTURAL REQUIREMENTS FOR AMINO-ACID INHIBITION OF SYNAPTOSOMAL AMINO-ACID UPTAKE
RAGHUPATHY, E
PETERSON, NA
FEBS LETTERS, 1977, 73 (02) : 151 - 154
[28] NEW AMINO-ACID DERIVATIVES
GANTE, J
MOHR, G
CHEMISCHE BERICHTE-RECUEIL, 1975, 108 (01): : 174 - 180
[29] AMINO-ACID DERIVATIVES OF AZIRIDINE
YEREMEYEV, AV
KRUTIUS, ON
KHIMIYA GETEROTSIKLICHESKIKH SOEDINENII, 1982, (12): : 1627 - 1630
[30] Amino-Acid Derivatives of Pyranocoumarins
I. V. Krasylov
V. S. Moskvina
S. V. Shilin
V. P. Khilya
Chemistry of Natural Compounds, 2020, 56 : 832 - 836

← 1 2 3 4 5 →