The antimicrobial activity of 3-methyl-5-isopropyl (or ethyl) 6-methyl-4-nitrophenyl-1,4-dihydropyridine-3,5-dicarboxylate derivatives was evaluated. Prokaryotes (bacteria) appeared to be more sensitive to their antimicrobial activity than were eukaryotes (filamentous fungi). The best antibacterial activity was shown by derivative 33, which was able to inhibit the growth of Mycobacterium smegmatis (MIC33 = 9 μg.ml(-1)), Staphylococcus aureus (MIC33 = 25 μg.ml(-1)), and Escherichia coli (MIC33 = 100 μg.ml(-1)). In addition, derivative 4 demonstrated its antibacterial power on the acid-fast bacterial species M. smegmatis and on Gram-positive S. aureus. Focusing on the structure-activity relationship, it appears that the increase in the substituent bulk at the C2 position improved the antibacterial activity of the set of compounds studied. Derivatives 33 and 4, carrying 2-cyano-3-oxo-3-phenylprop-1-en-1-yl and allyliminomethyl groups, respectively, showed significantly higher inhibition activities on all tested microorganisms in comparison with the rest of the derivatives. This enhancement was also in good correlation with different log P values (lipophilicity parameter).
Download full-text PDF |
Source |
|---|---|
| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4065119 | PMC |
| http://dx.doi.org/10.3797/scipharm.1311-04 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Efficacy and safety of SHEN26, a novel oral small molecular RdRp inhibitor for COVID-19 treatment: a multicenter, randomized, double-blinded, placebo-controlled, phase II clinical trial.
Virol J
January 2025
Medi-X Pingshan, Southern University of Science and Technology, Shenzhen, Guangdong, 518118, China.
Background: SHEN26 (ATV014) is an oral RNA-dependent RNA polymerase (RdRp) inhibitor with potential anti-SARS-CoV-2 activity. Safety, tolerability, and pharmacokinetic characteristics were verified in a Phase I study. This phase II study aimed to verify the efficacy and safety of SHEN26 in COVID-19 patients.
View Article and Find Full Text PDFEvaluating programmatic reactive focal drug administration impact on malaria incidence in northern Senegal: an interrupted time series analysis.
Malar J
January 2025
PATH, 2201 Westlake Ave Ste 200, Seattle, WA, 98121, USA.
Background: The World Health Organization conditionally recommends reactive drug administration to reduce malaria transmission in settings approaching elimination. However, few studies have evaluated the impact of reactive focal drug administration (rFDA) in sub-Saharan Africa, and none have evaluated it under programmatic conditions. In 2016, Senegal's national malaria control programme introduced rFDA, the presumptive treatment of compound members of a person with confirmed malaria, and reactive mass focal drug administration (rMFDA), an expanded effort including neighbouring compounds during an outbreak, in 10 low transmission districts in the north of the country.
View Article and Find Full Text PDFNon-thermal atmospheric plasma treatments enhance the growth, photosynthesis, metabolite accumulation, and nutritional value of geranium (Pelargonium graveolens L'Herit) leaves.
BMC Plant Biol
January 2025
Department of Integrative Agriculture, College of Agriculture and Veterinary Medicine, United Arab Emirates University, P.O. Box 15551, Al Ain, Abu Dhabi, United Arab Emirates.
This study investigated the effects of non-thermal atmospheric plasma (NTAP) treatment on the growth, chemical composition, and biological activity of geranium (Pelargonium graveolens L'Herit) leaves. NTAP was applied at a frequency of 13.56 MHz, exposure time of 15 s, discharge temperature of 25 °C, and power levels (T1 = 50, T2 = 80, and T3 = 120 W).
View Article and Find Full Text PDFHospital attendance, malaria prevalence and self-medication with an antimalarial drug before and after the start of COVID-19 pandemic in a sentinel site for malaria surveillance in Gabon.
Malar J
January 2025
Department of Parasitology-Mycology and Tropical Medicine, Université Des Sciences de La Santé de Libreville, BP 4009, Libreville, Gabon.
Background: The negative impact of COVID-19 pandemic on healthcare service utilization has been reported in several countries. In Gabon, data on the preparedness for future pandemic are lacking. The aim of the present study was to assess the trends of hospital attendance, malaria and self-medication prevalences as well as ITN use before and during Covid-19 first epidemic waves in a paediatric wards of a sentinel site for malaria surveillance, in Libreville, Gabon.
View Article and Find Full Text PDFRemoval of Antibiotics in Breeding Wastewater Tailwater Using Microalgae-Based Process.
Bull Environ Contam Toxicol
January 2025
Key Laboratory of Three Gorges Reservoir Region's Eco-Environment, Ministry of Education, Chongqing University, Chongqing, 400045, China.
Ciprofloxacin (CIP) and oxytetracycline (OTC) are commonly detected antibiotic species in breeding wastewater, and microalgae-based antibiotic treatment technology is an environmentally friendly and cost-effective method for its removal. This study evaluated the effects of CIP and OTC on Scenedesmus sp. in the breeding wastewater tailwater and the removal mechanisms of antibiotics.
View Article and Find Full Text PDFWant 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!