SYNTHESIS AND THE ANTIPEROXIDASE ACTIVITY OF SELENO ANALOGS OF THE ANTITHYROID DRUG PROPYLTHIOURACIL

被引：18

作者：

ABOULENEIN, HY ^{[1
]}

AWAD, AA ^{[1
]}

ALANDIS, NM ^{[1
]}

机构：

[1] KING SAUD UNIV,COLL SCI,DEPT ORGAN CHEM,RIYADH 11405,SAUDI ARABIA

来源：

JOURNAL OF ENZYME INHIBITION | 1993年 / 7卷 / 02期

关键词：

SELENO ANALOGS OF PROPYLTHIOURACIL; ANTITHYROID ACTIVITY; ANTIPEROXIDASE ACTIVITY; STRUCTURE-ACTIVITY RELATIONSHIPS;

D O I：

10.3109/14756369309040756

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

The synthesis of 6-n-propyl-2-selenouracil (PSeU, Ib) and its methyl derivative (MSeU, Ic) are described. Replacement of the sulfur atom at C2 by selenium increased with antiperoxidase activity of these analogues five fold when compared to the clinically used antithyroid drug propylthiouracil (PTU). The structure-activity relationships of these agents are discussed.

引用

页码：147 / 150

页数：4

共 8 条

[1] STUDIES IN CHEMOTHERAPY .10. ANTITHYROID COMPOUNDS - SYNTHESIS OF 5-SUBSTITUTED AND 6-SUBSTITUTED 2-THIOURACILS FROM BETA-OXOESTERS AND THIOUREA [J].

ANDERSON, GW ;

HALVERSTADT, IF ;

MILLER, WH ;

ROBLIN, RO .

JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, 1945, 67 (12) :2197-2200

[2]

DEESCOBAR GM, 1967, RECENT PROG HORM RES, V23, P87

[3]

ENEIN HYA, 1990, TOXICOL ENVIRON CHEM, V26, P83

[4]

KREMENTZ ET, 1957, SURGERY, V41, P619

[5] SOLUBILIZATION ISOLATION AND IDENTIFICATION OF A PEROXIDASE FROM MICROSOMAL FRACTION OF BEEF THYROID [J].

LJUNGGREN, JG ;

AKESON, A .

ARCHIVES OF BIOCHEMISTRY AND BIOPHYSICS, 1968, 127 (1-3) :346-+

[6]

LOWRY OH, 1951, J BIOL CHEM, V193, P265

[7] SELENOURACIL DERIVATIVES ARE POTENT INHIBITORS OF THE SELENOENZYME TYPE-I IODOTHYRONINE DEIODINASE [J].

VISSER, TJ ;

KAPTEIN, E ;

ABOULENEIN, HY .

BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS, 1992, 189 (03) :1362-1367

[8]

YU MW, 1973, P SOC EXP BIOL MED, V143, P672

← 1 →