Design, synthesis and structure–activity relationship studies of novel indazole analogues as DNA gyrase inhibitors with Gram-positive antibacterial activity

2004 ◽  
Vol 14 (11) ◽  
pp. 2857-2862 ◽  
Author(s):  
Akihiko Tanitame ◽  
Yoshihiro Oyamada ◽  
Keiko Ofuji ◽  
Yoko Kyoya ◽  
Kenji Suzuki ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
Dna Gyrase ◽  
Structure Activity Relationship ◽  
Activity Relationship ◽  
Gram Positive ◽  
Design Synthesis ◽  
Structure Activity ◽  
Gyrase Inhibitors

ChemInform Abstract: Design, Synthesis, and Structure-Activity Relationship Studies of ATP Analogues as DNA Gyrase Inhibitors.

ChemInform ◽  
2010 ◽  
Vol 31 (30) ◽  
pp. no-no
Author(s):  
Thomas Luebbers ◽  
Peter Angehrn ◽  
Hans Gmuender ◽  
Silvia Herzig ◽  
Josef Kulhanek
Keyword(s):  
Dna Gyrase ◽  
Structure Activity Relationship ◽  
Activity Relationship ◽  
Design Synthesis ◽  
Structure Activity ◽  
Atp Analogues ◽  
Gyrase Inhibitors

scholarly journals Chemical Synthesis and Structure-Activity Relationship Study Yield Desotamide a Analogues with Improved Antibacterial Activity

Marine Drugs ◽  
2021 ◽  
Vol 19 (6) ◽  
pp. 303
Author(s):  
Run Xu ◽  
Yongxiang Song ◽  
Jun Li ◽  
Jianhua Ju ◽  
Qinglian Li
Keyword(s):  
Staphylococcus Aureus ◽  
Antibacterial Activity ◽  
Fold Increase ◽  
Antibacterial Activities ◽  
Structure Activity Relationship ◽  
Activity Relationship ◽  
Gram Positive ◽  
Methicillin Resistant ◽  
Structure Activity ◽  
Relationship Of

Desotamides A, a cyclohexapeptide produced by the deep-sea-derived Streptomyces scopuliridis SCSIO ZJ46, displays notable antibacterial activities against strains of Streptococcus pnuemoniae, Staphylococcus aureus, and methicillin-resistant Staphylococcus epidermidis (MRSE). In this study, to further explore its antibacterial potential and reveal the antibacterial structure-activity relationship of desotamides, 13 cyclopeptides including 10 new synthetic desotamide A analogues and wollamides B/B1/B2 were synthesized and evaluated for their antibacterial activities against a panel of Gram-positive and -negative pathogens. The bioactivity data reveal that residues at position II and VI greatly impact antibacterial activity. The most potent antibacterial analogues are desotamide A4 (13) and A6 (15) where l-allo-Ile at position II was substituted with l-Ile and Gly at position VI was simultaneously replaced by d-Lys or d-Arg; desotamides A4 (13) and A6 (15) showed a 2–4-fold increase of antibacterial activities against a series of Gram-positive pathogens including the prevalent clinical drug-resistant pathogen methicillin-resistant Staphylococcus aureus (MRSA) with MIC values of 8–32 μg/mL compared to the original desotamide A. The enhanced antibacterial activity, broad antibacterial spectrum of desotamides A4 and A6 highlighted their potential as new antibiotic leads for further development.

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