58015-08-0Relevant articles and documents
Systematic research of H2dedpa derivatives as potent inhibitors of New Delhi Metallo-β-lactamase-1
Bai, Meng-Meng,Cui, De-Yun,Han, Jiang-Xue,Kong, Hong-Tao,Liu, Yi-Shuang,Shen, Bo-Yuan,Wang, Cong-Cong,Xiao, Chun-Ling,Yan, Da-Chao,Yang, Yi,Zhang, En
, (2020/06/01)
New Delhi Metallo-β-lactamase-1 (NDM-1), a Zn (II)-dependent enzyme, can catalyze the hydrolysis of almost all β-lactam antibiotics including carbapenems, resulting in bacterial antibiotic resistance, which threatens public health globally. Based on our finding that H2dedpa is as an efficient NDM-1 inhibitor, a series of H2dedpa derivatives was systematically prepared. These compounds exhibited significant activity against NDM-1, with IC50 values 0.06–0.94 μM. In vitro, compounds 6k and 6n could restore the activity of meropenem against Klebsiella pneumoniae, Escherichia coli and Proteus mirabilis possessing either NDM or IMP. In particular, the activity of meropenem against E. coli producing NDM-4 could be improved up to 5333 times when these two compounds were used. Time–kill cell-based assays showed that 99.9% of P. mirabilis were killed when treated with meropenem in combination with compound 6k or 6n. Furthermore, compounds 6k and 6n were nonhemolytic (HC50 > 1280 μg/mL) and showed low toxicity toward mammalian (HeLa) cells. Mechanistic studies indicated that compounds 6k and 6n inhibit NDM-1 by chelating the Zn2+ ion of the enzyme.
Synthesis, antimicrobial activity and structure-activity relationship study of N,N-dibenzyl-cyclohexane-1,2-diamine derivatives
Sharma, Mukul,Joshi, Penny,Kumar, Nitin,Joshi, Seema,Rohilla, Rajesh K.,Roy, Nilanjan,Rawat, Diwan S.
experimental part, p. 480 - 487 (2011/03/19)
We report herein synthesis and antimicrobial activity of a series of N,N-dibenzyl-cyclohexane-1,2-diamine derivatives. In order to study the structure-activity relationship of substituted dibenzyl-cyclohexane-1,2-diamine derivatives, 44 structurally diverse compounds were synthesized and tested against Gram-positive and Gram-negative bacterial strains. Among them, compounds 17-20, 26, 37, 38 were found to be more active than tetracycline with MIC value ranging 0.0005-0.032 μg/mL and no hemolysis upto 1024 μg/mL in mammalian erythrocytes was observed. Some of the compounds have also shown very promising antifungal activity against Candida albicans, Candida glabrata and Geotrichum candidium.
Tetrahydroimidazoles - A promising group of expected NSAIDS - Their synthesis and anti-inflammatory activity
Khan,Chawla, Gita
, p. 653 - 663 (2007/10/03)
Several new 1, 2, 3-trisubstituted tetrahydroimidazoles (11-28) have been synthesised and their structures elucidated on the basis of spectral data. These compounds show promising anti-inflammatory activity by carrageenin induced paw edema test in rats and few of them showed an activity better than indomethacin.