Cephalosporins with 3-pyazolylpyridinium at C-3 position, which is supposed to exhibit synergic activity of ceftazidime and cefoselis, were synthesized and their antibacterial activity against gram-positive and gram-negative was inspected.

Download full-text PDF

Source
http://dx.doi.org/10.1016/s0960-894x(00)00203-1DOI Listing

Publication Analysis

Top Keywords

synthesis structure-activity
4
structure-activity relationships
4
relationships quaternary
4
quaternary ammonium
4
ammonium cephalosporins
4
cephalosporins 3-pyrazolylpyridinium
4
3-pyrazolylpyridinium derivatives
4
derivatives cephalosporins
4
cephalosporins 3-pyazolylpyridinium
4
3-pyazolylpyridinium c-3
4

Similar Publications

The emerging prevalence of antimicrobial resistance demands cutting-edge therapeutic agents to treat bacterial infections. We present a synthetic strategy to construct sequence-defined oligomers (SDOs) by using dithiocarbamate (DTC). The antibacterial activity of the synthesized library of SDOs was studied using a Gram-positive and a Gram-negative .

View Article and Find Full Text PDF

To gain further insights into the importance of the unsaturated 1,4-ketoaldehyde moiety of ophiobolin A (OpA) for the potency and selectivity observed toward cancer stem cells, several derivatives were synthesized through controlled reduction and oxidations of the unsaturated aldehyde and ketone moieties. Structure elucidation of these new OpA derivatives was achieved through detailed NMR studies and comparison to OpA and known isolated congeners possessing variations in these regions. The relative stereochemistry of the newly generated stereocenters was determined by coupling constants in conjunction with conformational analyses (DFT) of the synthetic derivatives.

View Article and Find Full Text PDF

A range of heterocyclic compounds, including Isatin (oneH-indole-2, 3-dione) and its by-products, have been shown to represent potential unit blocks in the synthesis of potential medicinal agents. Numerous studies have been carried out on isatin, its synthesis, biological uses, and its chemical composition since when it was discovered. Functionally, these isatin-containing heterocycles have demonstrated antibacterial, antidiabetic, antiviral, antitubercular, and anticancer properties, among many others.

View Article and Find Full Text PDF

Antileishmanial and Antitrypanosomal Trends of Synthetic Tetralone Derivatives.

Drug Dev Res

February 2025

Department of Pharmaceutical Chemistry, College of Pharmacy, Jouf University, Sakaka, Aljouf, Saudi Arabia.

Leishmaniasis and trypanosomiasis are parasitic diseases that are closely linked to poverty, pose significant local burdens, and are common in tropical and subtropical regions. Various synthetic tetralone derivatives were studied as potential scaffolds for antileishmanial and antitrypanosomal activities. The compounds were studied for their effectiveness against multiple kinetoplastid protozoan pathogens: Leishmania major, Leishmania mexicana, and bloodstream trypomastigotes of Trypanosoma brucei brucei.

View Article and Find Full Text PDF

Agonists of insect hormones, namely molting hormone (MH) and juvenile hormone (JH), disrupt the normal growth of insects and can be employed as insecticides that are harmless to vertebrates. In this study, a series of experiments and computational analyses were conducted to rationally design novel insect hormone agonists. Syntheses and quantitative structure-activity relationship (QSAR) analyses of two MH agonist chemotypes, imidazothiadiazoles and tetrahydroquinolines, revealed that the structural factors important for the ligand-receptor interactions are significantly different between these chemotypes.

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!