Synthesis, characterization and in vitro biological studies of novel cyano derivatives of N-alkyl and N-aryl piperazine

被引:19
作者
Chaudhary, Preeti
Nimesh, Surendra
Yadav, Veena
Verma, Akhilesh Kr. [1 ]
Kumar, Rupesh
机构
[1] Univ Delhi, Dr BR Ambedkar Ctr Biomed Res, Delhi 110007, India
[2] Univ Delhi, Dept Chem, Delhi 110007, India
关键词
piperazine; cyano; pathogenic strain; cytotoxicity; antibacterial; antifungal activity; antibiotics;
D O I
10.1016/j.ejmech.2006.10.009
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Cyano derivatives of N-alkyl and N-aryl piperazine have been synthesized and screened for antibacterial and antifungal activities. All the synthesized compounds showed the antibacterial activity against pathogenic strains of Staphylococcus aureus (MTCCB 737), Pseudomonas aeruginosa (MTCCB 741), Streptomyces epidermidis (MTCCB 1824) and Escherichia coli (MTCCB 1652) and antifungal activity against pathogenic strains of Aspergillus fumigatus (ITCC 4517), Aspergillus flavus (ITCC 5192) and Aspergillus niger (ITCC 5405). All compounds showed mild to moderate antimicrobial activity. However, compounds 3c, 4a and 6 showed potent antibacterial activity against pathogenic strains used in the study. Compounds 3a, 3b, 4b, and 4d showed mild to moderate antifungal activity against Aspergillus pathogenic strains. The compounds reported in this study were assessed for there cytotoxicity using MTT colorimetric assay on Hela cells. All the compounds showed cell viability more than the control drug gentamicin, with compound 2 having highest i.e. 95% cell viability. (c) 2006 Elsevier Masson SAS. All rights reserved.
引用
收藏
页码:471 / 476
页数:6
相关论文
共 26 条
[1]  
Ahmad Y. E., 1997, J MED CHEM, V40, P952, DOI DOI 10.1021/JM950759Z
[2]   The fluoroquinolone antibacterials: past, present and future perspectives [J].
Appelbaum, PC ;
Hunter, PA .
INTERNATIONAL JOURNAL OF ANTIMICROBIAL AGENTS, 2000, 16 (01) :5-15
[3]   Characterization of Staphylococcus species by SDS-PAGE of whole-cell and extracellular proteins [J].
Berber, I ;
Cokmus, C ;
Atalan, E .
MICROBIOLOGY, 2003, 72 (01) :42-47
[4]   Synthesis and antibacterial activity of U-100592 and U-100766, two oxazolidinone antibacterial agents for the potential treatment of multidrug-resistant Gram-positive bacterial infections [J].
Brickner, SJ ;
Hutchinson, DK ;
Barbachyn, MR ;
Manninen, PR ;
Ulanowicz, DA ;
Garmon, SA ;
Grega, KC ;
Hendges, SK ;
Toops, DS ;
Ford, CW ;
Zurenko, GE .
JOURNAL OF MEDICINAL CHEMISTRY, 1996, 39 (03) :673-679
[5]  
BRICKNER SJ, 1995, 35 INT C ANT AG CHEM, V208, P149
[6]  
GREGORY WA, 1988, J MED CHEM, V32, P1218
[7]  
Harbarth S, 2001, Lancet Infect Dis, V1, P251, DOI 10.1016/S1473-3099(01)00120-7
[8]   Syntheses of optically active tetrahydro-1H-pyrrolo[1,2-a]imidazol-2-ones and hexahydroimidazo[1,2-α]pyridin-2(3H)-ones [J].
Katritzky, AR ;
He, HY ;
Wang, J .
JOURNAL OF ORGANIC CHEMISTRY, 2002, 67 (14) :4951-4956
[9]   Convenient syntheses of unsymmetrical imidazolidines [J].
Katritzky, AR ;
Suzuki, K ;
He, HY .
JOURNAL OF ORGANIC CHEMISTRY, 2002, 67 (09) :3109-3114
[10]   Properties and synthetic utility of N-substituted benzotriazoles [J].
Katritzky, AR ;
Lan, XF ;
Yang, JZ ;
Denisko, OV .
CHEMICAL REVIEWS, 1998, 98 (02) :409-548