Four types of amide (C3; C28; C3-C28) conjugates based on 2,3-seco-18alphaH-oleanane and 2,3-secolupane mono- and dicarboxylic acids were synthesized. The range of diamide derivatives was supplemented with C3-C3' and C28-C28' dicondensed amides with two A-secotriterpene backbones educed by reacting monocarboxylic A-secoacids with biogenic amino acid lysine. Compounds with inhibitory action against herpes virus reproduction (EC50 8.7 and 4.1 McM) were found among the synthesized mono- and diamide derivatives containing an ethyl-beta-alaninate fragment. It has been ascertained that diamide with ethyl-beta-alaninate fragment combines anti-herpes virus properties and anti-HIV activity (EC50 5.1 McM). For active compounds, the maximum non-toxic concentration (MNTC)/EC50 ratios ranges from 9.7 to 40.8. The synthesized amide conjugates do not exhibit any marked cytotoxic effects against human tumor cell lines rabdomiosarcoma RD TE32, A549 lung carcinoma and melanoma MS.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1134/s1068162013020143 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Oxidative stress drives potent bactericidal activity of pyrazinamide against .
bioRxiv
December 2024
Department of Microbiology and Immunology, University of Minnesota Medical School, Minneapolis, MN 55455.
Pyrazinamide (PZA) is a critical component of tuberculosis first-line therapy due to its ability to kill both growing and non-replicating drug-tolerant populations of within the host. Recent evidence indicates that PZA acts through disruption of coenzyme A synthesis under conditions that promote cellular stress. In contrast to its bactericidal action , PZA shows weak bacteriostatic activity against in axenic culture.
View Article and Find Full Text PDFPreparation and Structural Properties of Gel Coating Films Containing Lipophilized Nanocarbon Particles Functionalized with Thixotropic Chains.
J Oleo Sci
January 2025
Graduate School of Science and Engineering, Saitama University.
Gel coating films comprising nanodiamonds organo-modified with 12-hydroxystearic (12-OHC ) and stearic acids were prepared and characterized. Because molecules with 12-OHC groups can convert solvents into thixotropic gels, Gemini-type diamide derivatives with two 12-OHC chains were also introduced as thixotropic additives into the gel coating films. Although the 12-OHC -modified nanodiamonds did not lead to solvent gelation on their own, they displayed an affinity for the thixotropic additive molecules.
View Article and Find Full Text PDFTranscriptome profiling reveals novel insights into the regulation of calcium ion and detoxification genes driving chlorantraniliprole resistance in .
Heliyon
December 2024
Interdisciplinary Graduate Program in Smart Agriculture, Kangwon National University, Chuncheon, Republic of Korea.
Since the commercialization of diamide insecticides, including chlorantraniliprole, in 2007, the overuse of diamide insecticides for over a decade has resulted in excessive chlorantraniliprole resistance in , causing continuous economic losses. While RyR target-site mutations and detoxification enzymes such as cytochrome P450 have been studied as the leading causes of resistance, previous studies, including functional research and synergistic tests, have not confirmed a clear correlation between these factors and the development of resistance. Thus, transcriptome analysis was employed to investigate alternative strategies beyond mutation(s) in RyR or metabolic factors involving detoxification pathways that allow diamide-resistance to counteract the calcium ion imbalances induced by chlorantraniliprole effectively.
View Article and Find Full Text PDFNovel Meta-Diamide Derivatives Bearing Triazole: Design, Synthesis, and Bioactivity.
Chem Biodivers
December 2024
CAC Nantong Chemical Co. Ltd, Nantong, China.
In searching for novel insecticide lead, 20 new meta-diamide compounds containing triazole were designed and synthesized regarding cyproflanilide as lead compound. All the compounds were characterized by H NMR, C NMR, and High-resolution mass spectra (HR MS). In preliminary bioassay, we found that one of the compounds: N-(cyclopropylmethyl)-N-(5-((2,6-dibromo-4-(1,2,2,2-tetrafluoro-1-(trifluoromethyl)ethyl)phenyl)carbamoyl)-2-(1H-1,2,4-triazol-1-yl)phenyl)-6-(trifluoromethyl) nicotinamide (16a) had high activity against the target organism Plutella xylostella at 1 mg/L and against the target organism Mythimna separata at 2 mg/L.
View Article and Find Full Text PDFExploring Antimalarial and Cytotoxic Activities of Hibiscus cannabinus and Corchorus capsularis Extracts Through In-Vitro and In-Silico Approaches.
Chem Biodivers
November 2024
Department of Biochemistry, Central University of Haryana, Mahendergarh, Haryana, India.
Malaria is an infectious disease, endemic to tropical and sub-tropical regions causing half a million people's deaths every year. Bioactive compounds derived from medicinal plants are used to treat malaria disease and its complications. H.
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!