scholarly journals Antimicrobial Activity Derivatives 2H-pirano[2,3-c]piridines against Pathogens of Intestinal Yersiniosis

2021 ◽  
Vol 11 ◽  
pp. 87-92
Author(s):  
V.Yu. Ivannik ◽  
I.I. Torianyk ◽  
T.M. Moiseienko ◽  
A.I. Skliar ◽  
R.F. Yeromenko ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Chemical Structure ◽  
Statistical Data ◽  
Bactericidal Effect ◽  
Inhibitory Effect ◽  
Pyridine Derivatives ◽  
High Antimicrobial Activity ◽  
Clinical Strains ◽  
Synthetic Derivatives ◽  
Derivatives Of

Background: An important aspect in the treatment of patients with intestinal yersiniosis is the administration of effective antibiotic therapy. Performed research aimed to determine the spectrum and level of antimicrobial activity of 2H-pyrano[2,3- c]pyridine derivatives on the museum and clinical strains of gram-negative microorganisms Yersinia enterocolitica. Methodology: The object of the study was 28 synthetic derivatives of 2H-pyrano[2,3- c]pyridine. The compounds were studied according to their chemical structure. We used the method of serial dilutions in Muller-Hinton liquid nutrient medium with a museum’s and clinical strains of Y.enterocolitica. Results: Studies indicate the promise of further study of the properties of 2H- pyrono[2,3-c]pyridine to create an effective antimicrobial medicine. According to the results of studies on action of antimicrobial compounds synthesized on the basis of 2H-pyrano[2,3-с]pyridine derivatives, it was found that the MIC of compounds for all Y. enterocolitica strains was 100.0 μg/ml. The MBCC of most cultures of Yersinia (72.3 %) was 200.0 μg/ml. Compound 2{3} had a pronounced antiyersiniotic activity, the inhibitory effect of which was manifested at a concentration of 25.0 μg/ml. Retarding the growth of most Yersinia strains (95.3%) with a MIC of 50.0 μg/ml, the MIC of compounds ranged from 50.0 to 200.0 μg/ml. After statistical data processing, pyridine derivatives (compounds 2{3} and 3{5}) were identified, possessing an effective bacteriostatic and bactericidal effect on Y. enterocolitica strains. Conclusions: The results of the research showed a high antimicrobial activity of 2H- pyrano[2,3-c]pyridine derivatives. The highest activity against Y. enterocolitica was found for 2-N2-arylimino-5-hydroxy-methyl-8-methyl-2H-pyrano[2,3-c]pyridine-3-N1- aricarboxamide derivatives.

Inhibitory Effect of Retinoic Acid on Proliferation, Maturation and Tryptase Level in Human Leukemic Mast Cells (HMC-1)

2003 ◽  
Vol 16 (1) ◽  
pp. 43-47 ◽  
Author(s):  
M.G. Alexandrakis ◽  
D.S. Kyriakou ◽  
D. Seretakis ◽  
W. Boucher ◽  
R. Letourneau ◽  
...  
Keyword(s):  
Mast Cell ◽  
Retinoic Acid ◽  
Mast Cells ◽  
Allergic Inflammation ◽  
Inhibitory Effect ◽  
Control Group ◽  
Tryptase Level ◽  
Synthetic Derivatives ◽  
Derivatives Of ◽  
Inhibit Cell Proliferation

Mast cells play an important role in allergic inflammation by releasing histamine, tryptase and several inflammatory cytokines. Human leukemic mast cells (HMC-1) have been used to study mast cell mediators and their role in inflammatory mechanisms. HMC-1 contain and release several inflammatory mediators, of which the proteolytic enzyme tryptase is most characteristic. Retinoids, including retinoic acid, are naturally occurring and synthetic derivatives of vitamin A. All-trans-retinoic (ATRA) acid had been previously reported to inhibit cell proliferation, differentiation and apoptosis. In the present study, we investigated the effect of ATRA on the proliferation and secretion of tryptase in HMC-1. HMC-1 were treated with ATRA at 10-4M, 10-5M or 10-6M for 3,4 or 5 days in culture. Control HMC-1 were treated with equal amount of culture medium only. ATRA decreased the number of HMC-1 as compared to the control group. The same treatment for 3, 4 or 5 days also decreased intracellular tryptase levels. These results indicate that ATRA significantly inhibits both proliferation and growth as shown by the decreased intracellular tryptase levels in HMC-1. ATRA may be a useful agent in the treatment of mast cell proliferative disorders.

scholarly journals Synthesis and Antimicrobial Activity of a Silver-Hydroxyapatite Nanocomposite

2009 ◽  
Vol 2009 ◽  
pp. 1-6 ◽  
Author(s):  
Marcos Díaz ◽  
Flora Barba ◽  
Miriam Miranda ◽  
Francisco Guitián ◽  
Ramón Torrecillas ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Reduction Process ◽  
Bactericidal Effect ◽  
Gram Negative Bacteria ◽  
Subsequent Reduction ◽  
Visible Spectroscopy ◽  
High Antimicrobial Activity ◽  
Chemical Route ◽  
Uv Visible ◽  
High Degree

A silver-hydroxyapatite nanocomposite has been obtained by a colloidal chemical route and subsequent reduction process in H2/Ar atmosphere at350∘C. This material has been characterized by TEM, XRD, and UV-Visible spectroscopy, showing the silver nanoparticles (∼65 nm) supported onto the HA particles (∼130 nm) surface without a high degree of agglomeration. The bactericidal effect against common Gram-positive and Gram-negative bacteria has been also investigated. The results indicated a high antimicrobial activity forStaphylococcus aureus, PneumococcusandEscherichia coli,so this material can be a promising antimicrobial biomaterial for implant and reconstructive surgery applications.

scholarly journals Synthesis, Characterisation and Antimicrobial Potential of Novel N-Alkylated Pyrrole Derivatives of Chitosan

2021 ◽  
Vol 14 (4) ◽  
pp. 1730-1736
Author(s):  
Kalpana. P. R
Keyword(s):  
Antimicrobial Activity ◽  
Inhibitory Effect ◽  
Maximum Activity ◽  
Diffusion Method ◽  
Zone Of Inhibition ◽  
Pyrrole Derivatives ◽  
Structural Modifications ◽  
E Coli ◽  
Antimicrobial Potential ◽  
Derivatives Of

Chitosan, a cationic biopolymer is a major derivative of chitin. It is biocompatible, non-toxic and environ-friendly material and has broad spectrum antimicrobial activity. However, it is less effective in neutral or basic conditions due to its solubility only in acidic medium. Therefore, chemical modification with suitable groups is necessary to enhance the potency of chitosan. The present study was mainly conducted to explore the effect of structural modifications on antimicrobial potential of chitosan. N-Methyl, N-Ethyl and N-Propyl pyrrole were reacted with N-chloroacyl-6-O-triphenylmethylchitosan prepared by stepwise modification of chitosan to form N-Methyl, N-Ethyl and N-Propyl pyrrole derivatives of chitosan. Structural characterization of these pyrrole derivatives was done by IR, NMR, XRD, DSC and Elemental Analysis. The gram-negative bacterium Escherichia coli, gram-positive bacterium Staphylococcus aureus were selected for antibacterial activity and the fungus C. albicans was selected for antifungal activity by agar diffusion method and MIC method. Antimicrobial activity of the N-Methyl, N-Ethyl and N-Propyl pyrrole derivatives on E. coli, S. aureus and C. albicans showed an inhibitory effect on all the organisms. The potency of inhibition was found to be varied with the substitutions. The maximum activity was shown by N-pyrrolylpropylchitosan against E. coli (zone of inhibition 1.2±0.05cm, MIC 0.15±0.03mg/ml), S. aureus (zone of inhibition 1.4±0.03cm, MIC 0.15±0.01mg/ml), C. albicans (zone of inhibition 0.8±0.03cm, MIC 0.2±0.03mg/ml). The study also confirmed that all the three derivatives exhibited higher inhibition than that of chitosan against E. coli (zone of inhibition 0.7±0.03cm, MIC 0.09±0.02mg/ml), S. aureus (zone of inhibition 0.8±0.03cm, MIC 0.09±0.02mg/ml), C. albicans (zone of inhibition 0.6±0.03cm, MIC 0.09±0.03mg/ml). Results demonstrated that these three N-alkylpyrrole chitosan derivatives exhibited improved potency and hence can have the more applicability as antimicrobials.

scholarly journals Antimicrobial activity of antiseptics in the prevention of postoperative infectious complications

2021 ◽  
pp. 33-36
Author(s):  
N. A. Bagnyuk ◽  
O. A. Nazarchuk ◽  
Y. M. Babina ◽  
R. M. Chornopyshchuk ◽  
A. V. Kulyk
Keyword(s):  
Staphylococcus Aureus ◽  
Antimicrobial Activity ◽  
Antimicrobial Properties ◽  
Bactericidal Effect ◽  
Infectious Complications ◽  
Antimicrobial Efficacy ◽  
Gram Positive ◽  
Gram Negative ◽  
Clinical Strains ◽  
Enterococcus Spp

Recently, among hospital strains of microorganisms, an increase in the number of antiseptic-resistant strains of opportunistic pathogens has been registered, which significantly affects the effectiveness of these drugs. It is important to study their antimicrobial efficacy to justify rational use. The aim is to conduct a comparative study of the antimicrobial efficacy of antiseptics of decamethoxine, chlorhexidine, polyhexanide. During study we examined the antimicrobial activity against 186 clinical strains of microorganisms (Acinetobacter baumannii, Staphylococcus aureus, Pseudomonas aeruginosa, Enterococcus spp., Enterobacter spp.) isolated from patients with infectious complications in the postoperative period. The minimum inhibitory (MIC) and bactericidal concentrations (MBC) of 0.02 % and 0.1 % decamethoxine, 0.05 % chlorhexidine bigluconate, 0.1 % polyhexanide were determined; antimicrobial efficacy of drugs was evaluated by the index of antiseptic activity by conventional methods. The study found high antimicrobial properties of decamethoxine, chlorhexidine, which had a high bactericidal effect on clinical strains of S. aureus, Enterococcus spp., Enterobacter spp. Proved the benefits of antimicrobial activity of the drug based on decamethoxine (p<0.001). The polyhexanide has pronounced antimicrobial properties against A. baumannii, bacteria of the family Enterobactericae, P. aeruginosa. Thus, the leading gram-positive (Staphylococcus aureus, enterococci) and gram-negative pathogens (enterobacteria, acinetobacteria, pseudomonads) are sensitive to polyhexanide, chlorhexidine and the domestic drug decamethoxin, with a probable advantage of the antimicrobial properties of the latter over all gram-positive and most gram-negative microorganisms.

The analysis of sensitivity of Escherichia clinical strains, isolated from ill children to antibiotics, antiseptics

2013 ◽  
Vol 4 (4) ◽  
pp. 23-27
Author(s):  
Gordiy Kondratyevich Paliy ◽  
Oleksandr Adamovych Nazarchuk ◽  
Dmitri Vladimirovich Paliy ◽  
Sergey Adamovych Nazarchuk ◽  
Oksana Olegovna Gonchar ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
High Sensitivity ◽  
High Antimicrobial Activity ◽  
Clinical Strains ◽  
E Coli ◽  
Amoxicillin Clavulanate ◽  
Low Sensitivity

In the research the results of the study of sensitivity of Escherichia clinical strains (E. coli n 110) to antibiotics, antiseptics are presented. The Escherichia were isolated from ill children. According to the data of the research, we found high sensitivity of E. coli to combined penicillin antibiotics (amoxicillin/clavulanate, piperacyllin/tazobactam), cefalosporines (ceftriaxone, cefepime); meropenem; fluoroquilones (gatifloxacine, levofloxacine). The Escherichia had low sensitivity to amoxicillin/sulbactam, streptomycine, kanamycine, cefazoline, cefamandol, cefuroxime. High antimicrobial activity of decasan, miramistin with superiority of decasan according to E. coli, was proven.

scholarly journals In silico and in vivo anti-malarial investigation on [(5-nitroheteroaryl-2-yl) methylidene] hydrazinyl hetroaryl derivatives

2020 ◽  
Author(s):  
Azar Tahghighi ◽  
Seyed-Mahdi Mohamadi-Zarch1 ◽  
Hamze Rahimi ◽  
Mahya Marashiyan ◽  
Naseh Maleki-Ravasan ◽  
...  
Keyword(s):  
Plasmodium Falciparum ◽  
Liver Toxicity ◽  
Inhibitory Effect ◽  
Docking Studies ◽  
Molecular Binding ◽  
Effective Drugs ◽  
Synthetic Derivatives ◽  
Derivatives Of

Abstract Background Today, the resistance to Plasmodium falciparum against common anti-malarial drugs has attracted the attention towards the alternative and effective drugs. Synthetic derivatives of [(5-nitroieroaryl-2-yl) methylidene] hydrazineyl heteroaryl showed in vitro anti-plasmodial activity. The aim of this study was to evaluate the molecular binding and antiplasmid activity of in vivo synthetic compounds.Methods: The molecular docking was used to study the binding of compounds to heme and Plasmodium falciparum lactate dehydrogenase (PfLDH). Acute toxicity of the synthetic compounds was evaluated based on modified up & down method. Anti-plasmodial activity of the compounds was conducted by two standard methods of Peter and Rane’s tests via chloroquine-sensitive Plasmodium berghei . Also, the toxicity of mice’s internal organs was evaluated on day 7 in addition to the histopathology of their liver.Results The docking studies showed that active site of PfLDH had at least four common residues including Ala98, Ile54, Gly29 and Tyr97 to bind the compounds with the affinity ranging from -8.0 to -8.4 Kcal/mol. The mode of binding of ligands to heme revealed effective binding affinity ranging from -5.1 to -5.5 Kcal/mol. Compound 2 showed the highest % suppression of parasitemia (99.09%) at the dose of 125mg/kg/day in Peter’s tests. Compound 3 with 79.42% suppression was the best compounds in Rane’s test at the lowest dose (31.25 mg/kg/day). The histopathology of the mice’s livers did not reveal the focal necrosis of hepatocytes in the studied compounds.Conclusions The docking studies verified Pf LDH inhibition and the inhibitory effect on the hemozoin formation for the studied compounds. Accordingly, some compounds may provide new achievements for the development of antimalarial drugs without liver toxicity, although further studies are required to optimize their anti-plasmodial activity.

Sulfonamides and Sulphonyl Ester of Quinolines as Non-Acidic, Non- Steroidal, Anti-inflammatory Agents

2020 ◽  
Vol 17 ◽  
Author(s):  
Bilquees Bano ◽  
Kanwal ◽  
Khalid Mohammed Khan ◽  
Almas Jabeen ◽  
Aisha Faheem ◽  
...  
Keyword(s):  
Heterocyclic Compounds ◽  
Biological Activities ◽  
Inhibitory Effect ◽  
Inflammatory Activity ◽  
Spectroscopic Techniques ◽  
Wide Range ◽  
Anti Inflammatory ◽  
Hydroxy Quinoline ◽  
Synthetic Derivatives ◽  
Derivatives Of

Background:: Quinolines are important class of heterocyclic compounds possessing wide range of biological activities. Previously, we had identified Schiff bases of quinoline as potential anti-inflammatory agents, thus the current work is the continuation of our previous study. Objective:: In the current study 3-, 5-, and 8-sulfonamide and 8-sulfonate derivatives of quinoline (1-50) were synthesized and their antiinflammatory potential was evaluated. These synthetic analogs were evaluated for their anti-inflammatory activity via ROS (Reactive oxygen species) inhibitory effect produced from phagocytes from human whole blood. Methods:: The sulfonamide and sulfonate derivatives of quinoline were synthesized via treating 5-, 3-, 8-amino, and 8-hydroxy quinoline with different substituted sulfonyl chlorides in pyridine. The synthetic molecules were characterized using various spectroscopic techniques and screened for their anti-inflammatory potential. Results and Discussion:: Among the synthetic derivatives 1-50, six compounds showed good to moderate anti-inflammatory activity. Compounds 47 (IC50 = 2.9 ± 0.5 μg/mL), 36 (IC50 = 3.2 ± 0.2 μg/mL), and 24 (IC50 = 6.7 ± 0.3 μg/mL) exhibited enhanced activity as compared to the standard ibuprofen (IC50 = 11.2 ± 1.9 μg/mL). Compounds 20 (IC50 = 25.5 ± 0.7 μg/mL), 50 (IC50 = 42.9 ± 5.6 μg/mL), and 8 (IC50 = 53.9 ± 3.1 μg/mL) were moderately active, however, rest of the compounds were found to be inactive. Conclusion:: The sulfonamide and sulfonate derivatives of quinoline were found to have promising anti-inflammatory activity. Further studies on the modification of these molecules may leads to the discovery of new and potential anti-inflammatory agents.

scholarly journals The Impact of Alkaloids Structures from NaturalCompounds on Public Health

2015 ◽  
Vol 5 (1) ◽  
pp. 34 ◽  
Author(s):  
Emin Cadar ◽  
Aneta Tomescu ◽  
Cristina Luiza Erimia ◽  
Alef Mustafa ◽  
Rodica Sîrbu
Keyword(s):  
Public Health ◽  
Human Health ◽  
Chemical Structure ◽  
Indole Derivatives ◽  
Pyridine Derivatives ◽  
Plant Origin ◽  
Basic Character ◽  
The Impact ◽  
Derivatives Of ◽  
Tryptophan Derivatives

Alkaloids are organic heterocycle substances with nitrogen, of plant origin, with basic character, arising from the secondary metabolism of plants, which give characteristic reactions and exert an effect on animal bodies, most often of a toxic nature. Alkaloids have at least one atom of heterocycle nitrogen, in which case it is often tertiary, less frequently quaternary. The heterocycles can condense among themselves or with other cycles in such a way that alkaloid molecules may become poly- or macro-cycles. Alkaloids are classified on both the criterion of chemical structure, as well as based on their origin. Thus, the known alkaloids are divided into the following categories: derivatives of pyridine, derivatives of pyrolidine, derivatives of tryptophan, derivatives of quinolone and izoquinolone, derivatives of phenetylamine, indole derivatives, derivatives of purine, terpenes, and derivatives of betaine with quaternary nitrogen.This work presents the structures, location in natural compounds, as well as data pertaining to the extraction, identification, metering, and purification for various compounds, such as coniine, nicotine, atropine and cocaine, morphine and codeine, quinine, papaverine, strychnine, and caffeine.The effects these substances have on human health are highlighted.

Synthetic derivatives of pulchrol: An antiparasitic natural product

Planta Medica ◽  
2016 ◽  
Vol 81 (S 01) ◽  
pp. S1-S381
Author(s):  
P Terrazas ◽  
O Sterner
Keyword(s):  
Natural Product ◽  
Synthetic Derivatives ◽  
Derivatives Of

Effects of Prostaglandins, Derivatives of Cyclic 3':5'-AMP, Theophylline, Cholinergic Agents and Colchicine on Clot Retraction in Dilute Platelet-Rich Plasma and Gel-Separated Platelet Test Systems

1977 ◽  
Vol 38 (02) ◽  
pp. 0420-0428 ◽  
Author(s):  
J. L Moake ◽  
P. L Cimo ◽  
K Widmer ◽  
D. M Peterson ◽  
J. R Gum
Keyword(s):  
Platelet Rich Plasma ◽  
Inhibitory Effect ◽  
Fibrin Clot ◽  
Serotonin Release ◽  
Dibutyryl Camp ◽  
Clot Retraction ◽  
Dilute Suspensions ◽  
Cholinergic Agents ◽  
Camp Levels ◽  
Derivatives Of

SummaryIn dilute suspensions of platelet-rich plasma (PRP) or gel-separated platelets (GSP), dibutyryl-cAMP (DBcAMP) and monobutyryl-cAMP inhibited platelet-mediated fibrin clot retraction in concentrations of 2–3 × 10–6M, with complete inhibition at 1–3 × 10–4M. Prostaglandin E1 (PGE1), which inhibited fibrin clot retraction in concentrations greater than 1.5–3 × 10–8M, was a more effective inhibitor than either PGE2 or PGF2α. In the presence of theophylline (10–4M), concentrations of DBcAMP, PGE1 PGE2 and PGF2α necessary to inhibit fibrin clot retraction were reduced 50-fold for DBcAMP and 2.5 to 20-fold for the prostaglandins. In dilute PRP or GSP, inhibition of fibrin clot retraction does not result from inhibition of thrombin-induced platelet aggregation. Thus, compounds which increase platelet cAMP levels result in the inhibition of platelet-mediated fibrin clot retraction, and this inhibitory effect may be mediated, at least in part, through suppression of platelet contractility. Cyclic GMP, dibutyryl-cGMP and carbamylcholine-Cl (which stimulates guanylate cyclase) did not influence fibrin clot retraction, and did not prevent inhibition of fibrin clot retraction by DBcAMP and PGE?. Colchicine, in concentrations known to disrupt platelet microtubules (2.5 × 10–6M to 2.5 x 10–3M), had little inhibitory effect on either fibrin clot retraction or platelet (3H)-serotonin release.

Sign in / Sign up

Export Citation Format

Share Document