scholarly journals Wetting - Display Capacity of Some New Superficial Active Salefied Polyether ( =3–20) Primary Amides in Food Hygienization

2011 ◽  
Vol 68 (2) ◽  
Author(s):  
G. UIVAROSAN ◽  
C. JIANU ◽  
I. JIANU
Keyword(s):  
Food Chain ◽  
Plant Protection ◽  
Wide Spectrum ◽  
Structural Units ◽  
Ecological Agriculture ◽  
Active Compounds ◽  
New Class ◽  
Low Toxicity

Colloidal features (wetting) of conditioning auxiliaries (additives) of plant protection active principles constitute, together with toxicity, a decisive technical index in forming administering receipts in modern ecological agriculture and foodstuff processing all during the agroalimentary processing and consumption chain. In this paper we show the results of a study on a new class of superficial active compounds salefied polyether ( =3–20) primary amides. Structures have real colloidal and bacteriostatical abilities compared to a wide spectrum of microrganisms (tested in studies related to this paper). Low toxicity of polyoxyethylene chains (PEO) together with that of other structural units in provide the studied glymes with a high compatibility in relation to environment and to plant and animal organisms of the food chain.

scholarly journals Foaming Capacity of New Superficial Active Salefied Polyether ( = 3 – 20) Primary Amides in Food Hygienization

2011 ◽  
Vol 68 (2) ◽  
Author(s):  
M. SBANCA ◽  
C. JIANU ◽  
I. JIANU
Keyword(s):  
Plant Protection ◽  
Foam Stability ◽  
Wide Spectrum ◽  
Foaming Agents ◽  
New Class ◽  
Wide Range ◽  
Low Toxicity ◽  
Foaming Capacity ◽  
Water Plants ◽  
Alkaline Catalysis

.Colloidal features [foaming capacity (FC); foam stability (FS) and foam density (FD)] of conditioning auxiliaries (additives) of plant protection active principles constitute, together with toxicity, a decisive technical index in forming administering receipts in modern ecological agriculture and foodstuff processing all during the agroalimentary processing and consumption chain. In this paper we show the results of a study on a new class of superficial active compounds salefied polyether ( = 3 – 20) primary amides. As diderived glymes, they have a guided regulation capacity of the HLB balance through the change of the medium degree of oligomerisation ( ) of the polyoxyethylene chain (PEO). Can thus obtain a wide range of structures such as micellar solute, dispersion, emulsion, and foaming agents, etc., through the cyanoethylation of polyethoxylated nonylphenols with a medium degree of oligomerisation ( ) between 3 and 20 structural oxyethylene units (EO) in alkaline catalysis with monomer acrylonitrile, followed by a classical hydrogenation in heterogeneous catalysis of intermediary nitrile thus obtained, and finally partial hysrolysis and salefied with HCOOH; CH3COOH. These are biodegradable in water plants, which ensure special ecologlcal features and high compatibility within the restrictive legal ensemble of a foodstuff processing integrated in an extremely polluted environment. Structures have real bacteriostatical abilities compared to a wide spectrum of microrganisms (tested in studies related to this paper). Low toxicity of polyoxyethylene chains (PEO) together with that of other structural units in this polyether primary amides provide the studied glymes with a high compatibility in relation to environment and to plant and animal organisms of the food chain.

scholarly journals Identification of 3,4-Dihydro-2H,6H-pyrimido[1,2-c][1,3]benzothiazin-6-imine Derivatives as Novel Selective Inhibitors of Plasmodium falciparum Dihydroorotate Dehydrogenase

2021 ◽  
Vol 22 (13) ◽  
pp. 7236
Author(s):  
Endah Dwi Hartuti ◽  
Takaya Sakura ◽  
Mohammed S. O. Tagod ◽  
Eri Yoshida ◽  
Xinying Wang ◽  
...  
Keyword(s):  
Drug Target ◽  
De Novo ◽  
Dihydroorotate Dehydrogenase ◽  
Chemical Library ◽  
New Class ◽  
De Novo Biosynthesis ◽  
Starting Point ◽  
Novel Drugs ◽  
Low Toxicity ◽  
Fourth Step

Plasmodium falciparum’s resistance to available antimalarial drugs highlights the need for the development of novel drugs. Pyrimidine de novo biosynthesis is a validated drug target for the prevention and treatment of malaria infection. P. falciparum dihydroorotate dehydrogenase (PfDHODH) catalyzes the oxidation of dihydroorotate to orotate and utilize ubiquinone as an electron acceptor in the fourth step of pyrimidine de novo biosynthesis. PfDHODH is targeted by the inhibitor DSM265, which binds to a hydrophobic pocket located at the N-terminus where ubiquinone binds, which is known to be structurally divergent from the mammalian orthologue. In this study, we screened 40,400 compounds from the Kyoto University chemical library against recombinant PfDHODH. These studies led to the identification of 3,4-dihydro-2H,6H-pyrimido[1,2-c][1,3]benzothiazin-6-imine and its derivatives as a new class of PfDHODH inhibitor. Moreover, the hit compounds identified in this study are selective for PfDHODH without inhibition of the human enzymes. Finally, this new scaffold of PfDHODH inhibitors showed growth inhibition activity against P. falciparum 3D7 with low toxicity to three human cell lines, providing a new starting point for antimalarial drug development.

2-Arylindane-1,3-diones — A New Class of Radical-active Compounds

1973 ◽  
Vol 42 (3) ◽  
pp. 214-224 ◽  
Author(s):  
V V Moiseev ◽  
I T Poluktov
Keyword(s):  
Active Compounds ◽  
New Class

S16020 pyridocarbazole derivatives display high activity to lung cancer cells

2021 ◽  
Vol 21 ◽  
Author(s):  
Gabriela Chabowska ◽  
Helena Moreira ◽  
Beata Tylińska ◽  
Ewa Barg
Keyword(s):  
Cell Viability ◽  
Anticancer Agents ◽  
Topoisomerase Ii ◽  
Wide Spectrum ◽  
A549 Cells ◽  
Biological Evaluation ◽  
Dna Intercalation ◽  
P Glycoprotein ◽  
Low Toxicity ◽  
And Migration

Background: Despite the dynamic development of medicine, globally cancer diseases remain the second leading cause of death. Therefore, there is a strong necessity to improve chemotherapy regimens and search for new anticancer agents. Pyridocarbazoles are compounds with confirmed antitumor properties based on multimodal mechanisms, i.a. DNA intercalation and topoisomerase II-DNA complex inhibition. One of them, S16020, displayed a wide spectrum of activity. Objective: The aim of the study was to investigate the antitumor potency of six S16020 derivatives, synthesized according to the SAR (structure-activity relationship) method. Methods: The biological evaluation included influence on cancer cell viability, proliferation, and migration, as well as P-glycoprotein activity. NHDF, A549, MCF-7, LoVo, and LoVo/DX cell lines were used in the study. Results: All derivatives displayed low toxicity to normal (NHDF) cells at 1 and 2 µM (≤ 20% of cell growth inhibition). The highest reduction in cell viability was noted in A549 cells which was accompanied by significant disruption of cells proliferation and motility. Compound 1 exhibited the strongest cytotoxic, antiproliferative, and antimigratory effects, higher than the reference olivacine. A significant reduction in P-glycoprotein activity was found for derivatives 6 and 1. Conclusion: S16020 derivatives could be considered as potential candidates for new anticancer drugs.

scholarly journals Synthesis and biological evaluation of triphenyl-imidazoles as a new class of antimicrobial agents

2018 ◽  
Vol 9 (4) ◽  
pp. 369-374 ◽  
Author(s):  
Anupam Anupam ◽  
Mohammed Al-Bratty ◽  
Hassan Ahmad Alhazmi ◽  
Shamim Ahmad ◽  
Supriya Maity ◽  
...  
Keyword(s):  
Antimicrobial Agents ◽  
Biological Evaluation ◽  
Fungal Strain ◽  
Dilution Method ◽  
Serum Glutamic Oxaloacetic Transaminase ◽  
Active Compounds ◽  
Lead Compounds ◽  
New Class ◽  
Diffusion Technique ◽  
Ft Ir

Newer triphenyl-imidazole derivatives (4a-h) were synthesized in good yields by the reaction of benzil and substituted benzaldehydes in equimolar quantities and refluxing the product with acetyl chloride thereafter. Structures were confirmed by using FT-IR, 1H NMR and 13C NMR spectroscopic methods. All the synthesized compounds were tested for their antimicrobial activity using agar diffusion technique against Gram positive (Staphhylococcus aureus and Bacillus subtilis), Gram negative (Escherichia coli and Pseudomonas aureginosa) as well as Fungal strain (Candida albicans). Interestingly compounds 4a, 4b, 4f and 4h showed significant antibacterial activity, whereas compound 4b was found to have remarkable activity against the fungal strain. The Minimum Inhibitory Concentration (MIC) and Minimum Bactericidal Concentration (MBC) of most active compounds were determined by broth dilution method and compound 4b emerged to have potent activities against most of the strains having MIC in the range of 25-200 µg/mL. To check the possible toxicities of the most active compounds, they were orally administered in rats and the concentration of liver enzymes serum glutamic-oxaloacetic transaminase (SGOT), serum glutamic pyruvic transaminase (SGPT) and alkaline phosphatase (ALKP) were determined. Compound 4h showed significant increase in the enzymes level depicting the hepatotoxicity. The structure-activity relationship studies showed the importance of electron withdrawing groups at the distant phenyl ring at ortho and para positions as the compounds having chloro or nitro at these positions tend to be more active than the compounds with electron releasing groups such as methoxy. These compounds may act as lead compounds for further studies and appropriate modification in their structure may lead to agents having high efficacy with lesser toxicity.

scholarly journals Non-Toxic Virucidal Macromolecules Show High Efficacy Against Influenza Virus Ex Vivo and In Vivo

2020 ◽  
Author(s):  
Ozgun Kocabiyik ◽  
Valeria Cagno ◽  
Paulo Jacob Silva ◽  
Yong Zhu ◽  
Laura Sedano ◽  
...  
Keyword(s):  
Broad Spectrum ◽  
Viral Infections ◽  
Ex Vivo ◽  
Public Health Problem ◽  
Major Public Health Problem ◽  
New Class ◽  
Influenza Strain ◽  
Low Toxicity

AbstractInfluenza is one of the most widespread viral infections worldwide and represents a major public health problem. The risk that one of the next pandemics is caused by an influenza strain is very high. It is very important to develop broad-spectrum influenza antivirals to be ready for any possible vaccine shortcomings. Anti-influenza drugs are available but they are far from ideal. Arguably, an ideal antiviral should target conserved viral domains and be virucidal, i.e. irreversibly inhibit viral infectivity. Here, we describe a new class of broad-spectrum anti-influenza macromolecules that meets these criteria and displays exceedingly low toxicity. These compounds are based on a cyclodextrin core modified on its primary face with long hydrophobic linkers terminated in 6’sialyl-N-acetyllactosamine (6’SLN) or 3’SLN. SLN enables nanomolar inhibition of the viruses while the hydrophobic linkers confer irreversibility to the inhibition. The combination of these two properties allows for efficacy in vitro against several human or avian influenza strains, as well as against a 2009 pandemic influenza strain ex vivo. Importantly, we show that, in mice, the compounds provide therapeutic efficacy when administered 24h post-infection allowing 90% survival as opposed to no survival for the placebo and oseltamivir..

scholarly journals Commercial AHAS-inhibiting herbicides are promising drug leads for the treatment of human fungal pathogenic infections

2018 ◽  
Vol 115 (41) ◽  
pp. E9649-E9658 ◽  
Author(s):  
Mario D. Garcia ◽  
Sheena M. H. Chua ◽  
Yu-Shang Low ◽  
Yu-Ting Lee ◽  
Kylie Agnew-Francis ◽  
...  
Keyword(s):  
Candida Albicans ◽  
Antifungal Drug ◽  
New Drugs ◽  
Acetohydroxyacid Synthase ◽  
Drug Candidates ◽  
New Class ◽  
Branched Chain Amino Acid ◽  
Low Toxicity ◽  
Chlorimuron Ethyl ◽  
Branched Chain

The increased prevalence of drug-resistant human pathogenic fungal diseases poses a major threat to global human health. Thus, new drugs are urgently required to combat these infections. Here, we demonstrate that acetohydroxyacid synthase (AHAS), the first enzyme in the branched-chain amino acid biosynthesis pathway, is a promising new target for antifungal drug discovery. First, we show that several AHAS inhibitors developed as commercial herbicides are powerful accumulative inhibitors of Candida albicans AHAS (Ki values as low as 800 pM) and have determined high-resolution crystal structures of this enzyme in complex with several of these herbicides. In addition, we have demonstrated that chlorimuron ethyl (CE), a member of the sulfonylurea herbicide family, has potent antifungal activity against five different Candida species and Cryptococcus neoformans (with minimum inhibitory concentration, 50% values as low as 7 nM). Furthermore, in these assays, we have shown CE and itraconazole (a P450 inhibitor) can act synergistically to further improve potency. Finally, we show in Candida albicans-infected mice that CE is highly effective in clearing pathogenic fungal burden in the lungs, liver, and spleen, thus reducing overall mortality rates. Therefore, in view of their low toxicity to human cells, AHAS inhibitors represent a new class of antifungal drug candidates.

scholarly journals Targeted Molecular Imaging Using Aptamers in Cancer

2018 ◽  
Vol 11 (3) ◽  
pp. 71 ◽  
Author(s):  
Sorah Yoon ◽  
John Rossi
Keyword(s):  
Wide Spectrum ◽  
Rna Aptamers ◽  
Tissue Imaging ◽  
Live Cells ◽  
Target Cells ◽  
New Class ◽  
Non Invasive ◽  
Resolution Imaging ◽  
Tissue Specimens

Imaging is not only seeing, but also believing. For targeted imaging modalities, nucleic acid aptamers have features such as superior recognition of structural epitopes and quick uptake in target cells. This explains the emergence of an evolved new class of aptamers into a wide spectrum of imaging applications over the last decade. Genetically encoded biosensors tagged with fluorescent RNA aptamers have been developed as intracellular imaging tools to understand cellular signaling and physiology in live cells. Cancer-specific aptamers labeled with fluorescence have been used for assessment of clinical tissue specimens. Aptamers conjugated with gold nanoparticles have been employed to develop innovative mass spectrometry tissue imaging. Also, use of chemically conjugated cancer-specific aptamers as probes for non-invasive and high-resolution imaging has been transformative for in vivo imaging in multiple cancers.

scholarly journals Aptamers Chemistry: Chemical Modifications and Conjugation Strategies

Molecules ◽  
2019 ◽  
Vol 25 (1) ◽  
pp. 3 ◽  
Author(s):  
Fadwa Odeh ◽  
Hamdi Nsairat ◽  
Walhan Alshaer ◽  
Mohammad A. Ismail ◽  
Ezaldeen Esawi ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Drug Delivery Systems ◽  
Delivery Systems ◽  
Pharmacological Properties ◽  
Chemical Modifications ◽  
New Class ◽  
Advantages And Disadvantages ◽  
Dna Oligonucleotides ◽  
Low Toxicity ◽  
Group Diversity

Soon after they were first described in 1990, aptamers were largely recognized as a new class of biological ligands that can rival antibodies in various analytical, diagnostic, and therapeutic applications. Aptamers are short single-stranded RNA or DNA oligonucleotides capable of folding into complex 3D structures, enabling them to bind to a large variety of targets ranging from small ions to an entire organism. Their high binding specificity and affinity make them comparable to antibodies, but they are superior regarding a longer shelf life, simple production and chemical modification, in addition to low toxicity and immunogenicity. In the past three decades, aptamers have been used in a plethora of therapeutics and drug delivery systems that involve innovative delivery mechanisms and carrying various types of drug cargos. However, the successful translation of aptamer research from bench to bedside has been challenged by several limitations that slow down the realization of promising aptamer applications as therapeutics at the clinical level. The main limitations include the susceptibility to degradation by nucleases, fast renal clearance, low thermal stability, and the limited functional group diversity. The solution to overcome such limitations lies in the chemistry of aptamers. The current review will focus on the recent arts of aptamer chemistry that have been evolved to refine the pharmacological properties of aptamers. Moreover, this review will analyze the advantages and disadvantages of such chemical modifications and how they impact the pharmacological properties of aptamers. Finally, this review will summarize the conjugation strategies of aptamers to nanocarriers for developing targeted drug delivery systems.

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