SYNTHESIS AND ANTIPROTOZOAL PROPERTIES OF 1,2,6-THIADIAZINE 1,1-DIOXIDE DERIVATIVES

被引：18

作者：

HERRERO, A ^{[1
]}

OCHOA, C ^{[1
]}

ATIENZA, J ^{[1
]}

ESCARIO, JA ^{[1
]}

GOMEZBARRIO, A ^{[1
]}

FERNANDEZ, ARM ^{[1
]}

机构：

[1] UNIV COMPLUTENSE,FAC FARM,DEPT PARASITOL,E-28040 MADRID,SPAIN

来源：

ARCHIV DER PHARMAZIE | 1992年 / 325卷 / 08期

关键词：

D O I：

10.1002/ardp.19923250811

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The synthesis and spectroscopical data of 1,2,6-thiadiazine 1,1-dioxides, designed as antiprotozoal agents, are reported. The in vitro trichomonacidal and trypanocidal activities of new compounds and their precursors were evaluated against Trichomonas vaginalis and Trypanosoma cruzi. The chemoprophylactic activity on mice treated with blood infected with T. cruzi and their mortalitY percentage were tested. Compounds 2 and 8b show a higher chemoprophylactic activity and lower mortality percentage than Nifurtimox used as reference drug.

引用

页码：509 / 514

页数：6

共 16 条

[1]

ALKORTA I, 1986, J CHEM SOC P1, P643

[2]

ARAN VJ, 1986, IL FARMACO, V41, P863

[3]

ATIENZA J, 1987, 3 P INT C PHARM SCI, P455

[4]

Brener Z, 1975, Adv Pharmacol Chemother, V13, P1, DOI 10.1016/S1054-3589(08)60229-X

[5] SENSITIVITY OF PARASITES TO FREE-RADICAL DAMAGE BY ANTIPARASITIC DRUGS [J].

DOCAMPO, R .

CHEMICO-BIOLOGICAL INTERACTIONS, 1990, 73 (01) :1-27

[6]

DOYLE PS, 1989, EXP PARASITOL, V68, P320

[7] NUCLEAR MAGNETIC-RESONANCE OF AROMATIC HETEROCYCLICS .8. COMPARATIVE STUDY OF H-1 AND C-13 SPECTRA OF SOME 2-SUBSTITUTED FURANS, THIOPHENES, SELENOPHENES AND TELLUROPHENES [J].

FRINGUELLI, F ;

GRONOWIT.S ;

HORNFELD.AB ;

JOHNSON, I ;

TATICCHI, A .

ACTA CHEMICA SCANDINAVICA SERIES B-ORGANIC CHEMISTRY AND BIOCHEMISTRY, 1974, B 28 (02) :175-184

[8] 1,2,6-THIADIAZIN-3,5(2H,6H)-DIONE 1,1-DIOXIDE DERIVATIVES - CRYSTAL-STRUCTURE, PHYSICOCHEMICAL AND BIOLOGICAL PROPERTIES [J].

GOYA, P ;

NIEVES, R ;

OCHOA, C ;

RODELLAS, C ;

MARTINEZRIPOLL, M ;

GARCIABLANCO, S .

CANADIAN JOURNAL OF CHEMISTRY-REVUE CANADIENNE DE CHIMIE, 1987, 65 (02) :298-302

[9] N-15 AND C-13 NMR-SPECTROSCOPY OF 1,2,6-THIADIAZINE 1,1-DIOXIDE DERIVATIVES AND FUSED SYSTEMS [J].

GOYA, P ;

OCHOA, C ;

ROZAS, I ;

ALEMANY, A ;

JIMENO, ML .

MAGNETIC RESONANCE IN CHEMISTRY, 1986, 24 (05) :444-450

[10]

GRONOWITZ S, 1975, CHEM SCRIPTA, V7, P76

← 1 2 →