Synthesis and radiation stability of novel biologically active sulfur compounds derived from 1,2-bis(4-amino-5-mercapto-s-triazol-3-yl)ethane

被引:56
作者
Ghorab, MM
El-Sharief, AMS
Ammar, YA
Mohamed, SI
机构
[1] Natl Ctr Radiat Res & Technol, Dept Drug Radiat Res, Cairo, Egypt
[2] Al Azhar Univ, Fac Sci, Dept Chem, Cairo, Egypt
来源
FARMACO | 2000年 / 55卷 / 05期
关键词
triazoles; triazolothiadiazine; triazolothiadiazole; antifungal activity; gamma-rays;
D O I
10.1016/S0014-827X(00)00051-3
中图分类号
R9 [药学];
学科分类号
1007 [药学];
摘要
Some novel 1,2-bis(s-triazolo[3,4b][1,3,4]thiadiazino-3-yl)ethane (4-7); 1,2-bis(s-triazolo[3,4b][1,3,4]thiadiazol-3-yl)ethane (16a,b) and 1,2-bis(s-triazolo[3,4b][1,3,4]thiadiazepino-3-yl)ethane (17) were synthesized via reaction of 1,2-bis(4-amino-5-mercapto-s-triazol-3-yl)ethane (3) with different reagents. Identification of the new compounds was established by elemental analyses, TR, H-1 NMR and mass spectral data. Compounds 12, 13, 16b and 17 were promising antifungal activity. The biologically active compounds 13, 16b and 17 were radioresistant retaining their structures unchanged up to 40 k Gy. Radiosterilization of these compounds in the dry state may prove to be applicable. (C) 2000 Elsevier Science S.A. All rights reserved.
引用
收藏
页码:354 / 361
页数:8
相关论文
共 15 条
[1]
Influence of radiation treatment on pharmaceuticals - A review: Alkaloids, morphine derivatives, and antibiotics [J].
Boess, C ;
Bogl, KW .
DRUG DEVELOPMENT AND INDUSTRIAL PHARMACY, 1996, 22 (06) :495-529
[2]
SYNTHESIS OF SOME S-TRIAZOLES WITH POTENTIAL ANALGETIC AND ANTIINFLAMMATORY ACTIVITIES [J].
GEORGE, T ;
MEHTA, DV ;
TAHILRAMANI, R ;
DAVID, J ;
TALWALKER, PK .
JOURNAL OF MEDICINAL CHEMISTRY, 1971, 14 (04) :335-+
[3]
Ghorab MM, 1996, PESTIC SCI, V48, P31, DOI 10.1002/(SICI)1096-9063(199609)48:1&lt
[4]
31::AID-PS430&gt
[5]
3.0.CO
[6]
2-#
[7]
Ghorab Moustafa M., 1999, Acta Pharmaceutica (Zagreb), V49, P1
[8]
GIRI S, 1978, J INDIAN CHEM SOC, V55, P168
[9]
SYNTHESIS AND BIOLOGICAL-ACTIVITY OF BRIDGEHEAD NITROGEN-HETEROCYCLES [J].
GOSWAMI, BN ;
KATAKY, JCS ;
BARUAH, JN .
JOURNAL OF HETEROCYCLIC CHEMISTRY, 1986, 23 (05) :1439-1442
[10]
HOLLA BS, 1988, INDIAN J CHEM B, V27, P683