Back Cover: Design, Synthesis, and in vitro Antibacterial Activity of Fluoroquinolone Derivatives Containing a Chiral 3-(Alkoxyimino)-2-(aminomethyl)azetidine Moiety (ChemMedChem 7/2012)

ChemMedChem ◽  
2012 ◽  
Vol 7 (7) ◽  
pp. 1300-1300
Author(s):  
Kai Lv ◽  
Yexin Sun ◽  
Lanyin Sun ◽  
Zengquan Wei ◽  
Huiyuan Guo ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
Design Synthesis ◽  
Back Cover ◽  
In Vitro Antibacterial Activity ◽  
Cover Design ◽  
Fluoroquinolone Derivatives

Design, synthesis and antibacterial evaluation of ocotillol derivatives with polycyclic nitrogen-containing groups

2021 ◽  
Author(s):  
Yucheng Cao ◽  
Kaiyi Wang ◽  
Jiali Wang ◽  
Haoran Cheng ◽  
Mengxin Ma ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
Multidrug Resistant ◽  
Inhibitory Effect ◽  
Resistant Bacteria ◽  
Design Synthesis ◽  
In Vitro Antibacterial Activity ◽  
Strong Inhibitory Effect ◽  
Hospital Acquired ◽  
Derivatives Of

Aim: With the increasing abuse of antibacterial drugs, multidrug-resistant bacteria have become a burden on human health and the healthcare system. To find alternative compounds effective against hospital-acquired methicillin-resistant Staphylococcus aureus (HA-MRSA), novel derivatives of ocotillol were synthesized. Methods & Results: Ocotillol derivatives with polycyclic nitrogen-containing groups were synthesized and evaluated for in vitro antibacterial activity. Compounds 36–39 exhibited potent antibacterial activity against hospital-acquired MRSA, with MIC = 8–64 μg/ml. Additionally, a combination of compound 37 and the commercially available antibiotic kanamycin showed synergistic inhibitory effects, with a fractional inhibitory concentration index of ≤0.375. Conclusion: Compound 37 has a strong inhibitory effect, and this derivative has potential for use as a pharmacological tool to explore antibacterial mechanisms.

scholarly journals Design, Synthesis and Antibacterial Activity of Coumarin-1,2,3-triazole Hybrids Obtained from Natural Furocoumarin Peucedanin

Molecules ◽  
2019 ◽  
Vol 24 (11) ◽  
pp. 2126 ◽  
Author(s):  
Alla V. Lipeeva ◽  
Danila O. Zakharov ◽  
Liubov G. Burova ◽  
Tatyana S. Frolova ◽  
Dmitry S. Baev ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
Cycloaddition Reaction ◽  
Bacterial Strains ◽  
Design Synthesis ◽  
Docking Simulations ◽  
E Coli ◽  
Antibiotic Drugs ◽  
In Vitro Antibacterial Activity ◽  
Substituted Coumarins

Synthesis of 1,2,3-triazole-substituted coumarins and also 1,2,3-triazolyl or 1,2,3-triazolylalk-1-inyl-linked coumarin-2,3-furocoumarin hybrids was performed by employing the cross-coupling and copper catalyzed azide-alkyne cycloaddition reaction approaches. The synthesized compounds were evaluated for their in vitro antibacterial activity against Staphylococcus aureus, Bacillius subtilis, Actinomyces viscosus and Escherichia coli bacterial strains. Coumarin-benzoic acid hybrids 4с, 42с and 3-((4-acetylamino-3-(methoxycarbonyl)phenyl)ethynyl)coumarin (29) showed promising activity against S. aureus strains, and the 1,2,3-triazolyloct-1-inyl linked coumarin-2,3-furocoumarin hybrid 37c was endowed with high selectivity against B. subtilis and E. coli species. The in vitro antibacterial activity of 4с, 29, 37c and 42с can potentially be compared with that of a number of modern antibiotic drugs used in the clinic, suggesting promising prospects for further research. A detailed study of the molecular interactions with the targeted protein MurB was performed using docking simulations and the obtained results are quite promising.

scholarly journals Design, Synthesis and Antibacterial Evaluation of 3-Substituted Ocotillol-Type Derivatives

Molecules ◽  
2018 ◽  
Vol 23 (12) ◽  
pp. 3320 ◽  
Author(s):  
Kai-Yi Wang ◽  
Zhi-Wen Zhou ◽  
Heng-Yuan Zhang ◽  
Yu-Cheng Cao ◽  
Jin-Yi Xu ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
Triterpenoid Saponin ◽  
Bacterial Strains ◽  
Design Synthesis ◽  
Design And Synthesis ◽  
Good Antibacterial Activity ◽  
Structure Activity ◽  
In Vitro Antibacterial Activity ◽  
Free Hydroxyl

Antibiotic resistance has become a serious global problem that threatens public health. In our previous work, we found that ocotillol-type triterpenoid saponin showed good antibacterial activity. Based on preliminary structure-activity relationship, novel serious C-3 substituted ocotillol-type derivatives 7–26 were designed and synthesized. The in vitro antibacterial activity was tested on five bacterial strains (B. subtilis 168, S. aureus RN4220, E. coli DH5α, A. baum ATCC19606 and MRSA USA300) and compared with the tests on contrast. Among these derivatives, C-3 position free hydroxyl substituted compounds 7–14, showed good antibacterial activity against Gram-positive bacteria. Furthermore, compound 22 exhibited excellent antibacterial activity with minimum inhibitory concentrations (MIC) values of 2 μg/mL against MRSA USA300 and 4 μg/mL against B. subtilis. The structure-activity relationships of all current ocotillol-type derivatives our team synthesised were summarized. In addition, the prediction of absorption, distribution, metabolism, and excretion (ADME) properties and the study of pharmacophores were also conducted. These results can provide a guide to further design and synthesis works.

ChemInform Abstract: Synthesis and in vitro Antibacterial Activity of 7-(3-Alkoxyimino-4-methyl-4-methylaminopiperidin-1-yl)fluoroquinolone Derivatives.

ChemInform ◽  
2010 ◽  
Vol 41 (30) ◽  
pp. no-no
Author(s):  
Yi-Bin Zhang ◽  
Lian-Shun Feng ◽  
Xue-Fu You ◽  
Qiang Guo ◽  
Hui-Yuan Guo ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
In Vitro Antibacterial Activity ◽  
Fluoroquinolone Derivatives

ChemInform Abstract: Synthesis and in vitro Antibacterial Activity of 7-(3-Alkoxyimino-5-amino/methylaminopiperidin-1-yl)fluoroquinolone Derivatives.

ChemInform ◽  
2011 ◽  
Vol 42 (29) ◽  
pp. no-no
Author(s):  
Yibin Zhang ◽  
Guoqing Li ◽  
Mingliang Liu ◽  
Xuefu You ◽  
Lianshun Feng ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
In Vitro Antibacterial Activity ◽  
Fluoroquinolone Derivatives
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