Convergent synthesis and antibacterial activity of pyrazole and pyrazoline derivatives of diazepam

被引:70
作者
Berghot, MA [1 ]
Moawad, EB [1 ]
机构
[1] Mansoura Univ, Fac Sci, Dept Chem, Mansoura 35516, Egypt
关键词
diazepam; pyrazoles; pyrazolines;
D O I
10.1016/S0928-0987(03)00162-3
中图分类号
R9 [药学];
学科分类号
100702 [药剂学];
摘要
Polysubstituted pyrazoles (5)(a-l), pyrazolines (7)(a-c), (8)(a-c) and pyrazolotriazine (10) derivatives of diazepam were synthesized. The structures of hitherto unknown compounds were established by analytical and spectral methods. Some of these compounds were screened to test their antibacterial activity against gram-positive (B. subtilis) and gram-negative (P. aeruginosa). All compounds showed potent activity against these bacteria. (C) 2003 Elsevier B.V. All rights reserved.
引用
收藏
页码:173 / 179
页数:7
相关论文
共 13 条
[1]
C-13 NMR OF PYRAZOLES [J].
BEGTRUP, M ;
BOYER, G ;
CABILDO, P ;
CATIVIELA, C ;
CLARAMUNT, RM ;
ELGUERO, J ;
GARCIA, JI ;
TOIRON, C ;
VEDSO, P .
MAGNETIC RESONANCE IN CHEMISTRY, 1993, 31 (02) :107-168
[2]
Facile synthesis and biological evaluation of heterocyclic compounds containing diazepam [J].
Berghot, MA .
ARCHIVES OF PHARMACAL RESEARCH, 2001, 24 (04) :263-269
[3]
HETEROCYCLIC GROUPS [B]-ANNULATED TO THE 1,4-BENZODIAZEPINE SYSTEM [J].
BERGHOT, MA .
ARCHIV DER PHARMAZIE, 1992, 325 (05) :285-289
[4]
ELAGAMEY AGA, 1991, J PRAKT CHEM, V333, P333
[5]
STUDIES WITH POLYFUNCTIONALLY SUBSTITUTED HETEROAROMATICS - SYNTHESIS OF SEVERAL NEW THIAZOLES, PYRAZOLO[5,1-C]TRIAZINES AND OF POLYFUNCTIONALLY SUBSTITUTED PYRIDINES AND PYRIMIDINES [J].
ELGHANDOUR, AHH ;
IBRAHIM, MKA ;
ELSHIKH, SMM ;
ALI, FMM .
TETRAHEDRON, 1992, 48 (42) :9295-9304
[6]
GRUICKSHANK R, 1975, MED MICROBIOLOGY, V11, P190
[7]
DIAZEPINES .5. SYNTHESIS AND BIOLOGICAL ACTION OF 6-PHENYL-4H-PYRROLO[1,2-A][1,4]BENZODIAZEPINES [J].
HARA, T ;
KAYAMA, Y ;
MORI, T ;
ITOH, K ;
FUJIMORI, H ;
SUNAMI, T ;
HASHIMOTO, Y ;
ISHIMOTO, S .
JOURNAL OF MEDICINAL CHEMISTRY, 1978, 21 (03) :263-268
[8]
HOFFMANN F, 1980, VADEME CUMN ROCH PRO, P129
[9]
STEFANOVICH V, 1971, J PHARM SCI, V60, P78
[10]
Sternbach L H, 1978, Prog Drug Res, V22, P229