Design, synthesis and antistaphylococcal activity of marine pyrrole alkaloid derivatives

被引:19
|
作者
Rane, Rajesh A. [1 ]
Sahu, Niteshkumar U. [1 ]
Shah, Chetan P. [1 ]
Shah, Nishant K. [1 ]
机构
[1] NMIMS Univ, SPP Sch Pharm & Technol Management, Bombay 400056, Maharashtra, India
关键词
Antistaphylococcal activity; bromopyrrole alkaloids; hydrazide derivatives; METHICILLIN-RESISTANT; ANTIBIOFILM ACTIVITY; IN-VITRO; STAPHYLOCOCCI; BIOFILM; BROMOPYRROLE; DAPTOMYCIN; INHIBITORS; BACTERIA; MODEL;
D O I
10.3109/14756366.2013.793183
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
A novel set of 16 hybrids of bromopyrrole alkaloids with aroyl hydrazone were designed, synthesized and evaluated for antibacterial and antibiofilm activities against methicillin-resistant Staphylococcus aureus (MRSA; ATCC 43866), methicillin-susceptible Staphylococcus aureus (MSSA; ATCC 35556) and Staphylococcus epidermidis (SE, S. epidermidis ATCC 35984). Of the 16 tested hybrids, 14 exhibited equal or superior antibiofilm activity against MSSA and MRSA relative to standard vancomycin. Compound 4m showed highest potency with antibiofilm activity of 0.39 mu g/mL and 0.78 mu g/mL against MSSA and MRSA, respectively. Thus, this compound could act as a potential lead for further development of new antistaphylococcal drugs.
引用
收藏
页码:401 / 407
页数:7
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