Design, synthesis and evaluation of hybrid of tetrahydrocarbazole with 2,4-diaminopyrimidine scaffold as antibacterial agents.

Eur J Med Chem

Shanghai Key Laboratory of Regulatory Biology, The Institute of Biomedical Sciences and School of Life Sciences, East China Normal University, Shanghai, 200241, China. Electronic address:

Published: January 2019

AI Article Synopsis

  • * Researchers combined a 2,4-diaminopyrimidine structure with the tetrahydrocarbazole to make new hybrid compounds, which were also evaluated for antibacterial activity.
  • * The most effective hybrid compound, identified as 12c, displayed strong antibacterial effects with low minimum inhibitory concentration (MIC) values against both S. aureus Newman and E. coli AB1157, as well as against multiple drug-resistant S. aureus strains.

Article Abstract

Several 6-substituted tetrahydrocarbazole derivatives were designed, synthesized and evaluated for the antibacterial activities against Staphylococcus aureus Newman strain. Subsequently, 2,4-diaminopyrimidine scaffold was merged with the tetrahydrocarbazole unit to generate a series of novel hybrid derivatives and the antibacterial activities were also investigated. Among these novel hybrids, compound 12c showed the most potent activity with a MIC of 0.39-0.78 μg/mL against S. aureus Newman and Escherichia coli AB1157 strain. In addition, compound 12c exhibited low MIC values against a panel of multidrug-resistant strains of S. aureus.

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.ejmech.2018.11.016DOI Listing

Publication Analysis

Top Keywords

24-diaminopyrimidine scaffold
8
antibacterial activities
8
compound 12c
8
design synthesis
4
synthesis evaluation
4
evaluation hybrid
4
hybrid tetrahydrocarbazole
4
tetrahydrocarbazole 24-diaminopyrimidine
4
scaffold antibacterial
4
antibacterial agents
4

Similar Publications

Rotator cuff tears are the most common conditions in sports medicine and attract increasing attention. Scar tissue healing at the tendon-bone interface results in a high rate of retears, making it a major challenge to enhance the healing of the rotator cuff tendon-bone interface. Biomaterials currently employed for tendon-bone healing in rotator cuff tears still exhibit limited efficacy.

View Article and Find Full Text PDF

CASK, a MAGUK family scaffold protein, regulates gene expression as a transcription co-activator in neurons. However, the mechanism of CASK nucleus translocation and the regulatory function of CASK in myeloid cells remains unclear. Here, we investigated its role in H5N1-infected macrophages.

View Article and Find Full Text PDF

Bolstered bone regeneration by multiscale customized magnesium scaffolds with hierarchical structures and tempered degradation.

Bioact Mater

April 2025

Department of Orthopedic Surgery, State Key Laboratory of Complex Severe and Rare Diseases, Peking Union Medical College Hospital, Chinese Academy of Medical Science and Peking Union Medical College, Beijing 100730, China.

Addressing irregular bone defects is a formidable clinical challenge, as traditional scaffolds frequently fail to meet the complex requirements of bone regeneration, resulting in suboptimal healing. This study introduces a novel 3D-printed magnesium scaffold with hierarchical structure (macro-, meso-, and nano-scales) and tempered degradation (microscale), intricately customized at multiple scales to bolster bone regeneration according to patient-specific needs. For the hierarchical structure, at the macroscale, it can feature anatomic geometries for seamless integration with the bone defect; The mesoscale pores are devised with optimized curvature and size, providing an adequate mechanical response as well as promoting cellular proliferation and vascularization, essential for natural bone mimicry; The nanoscale textured surface is enriched with a layered double hydroxide membrane, augmenting bioactivity and osteointegration.

View Article and Find Full Text PDF

Developing scaffolds supporting functional cell attachment and tissue growth is critical in basic cell research, tissue engineering, and regenerative medicine approaches. Though poly(ethylene glycol) (PEG) and its derivatives are attractive for hydrogels and scaffold fabrication, they often require bioactive modifications due to their bioinert nature. In this work, biomimetic synthesized conductive polypyrrole-poly(3,4-ethylenedioxythiophene) copolymer doped with poly(styrenesulfonate) (PPy-PEDOT:PSS) was used as a biocompatible coating for poly(ethylene glycol) diacrylate (PEGDA) hydrogel to support neuronal and muscle cells' attachment, activity, and differentiation.

View Article and Find Full Text PDF

The Pacific banana slug, Ariolimax columbianus, is endemic to the forests of the Pacific Northern West. Found throughout coastal foothills and mountains of California, the hermaphroditic molluscs Ariolimax spp. are niche-constrained, hyper-localized, and phenotypically diverse.

View Article and Find Full Text PDF

Want AI Summaries of new PubMed Abstracts delivered to your In-box?

Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!