scholarly journals Phenylindolylmethyldiaminopyrimidines (PIDAPs) as Potent Antimicrobials Against Staphylococcus Aureus

2021 ◽  
Author(s):  
Margaret Deming ◽  
Alatheia King ◽  
Robert A Coover ◽  
Cale D Fahrenholtz ◽  
Aurijit Sarkar
Keyword(s):  
Staphylococcus Aureus ◽  
Structure Function ◽  
Cell Lines ◽  
Human Cell ◽  
Antimicrobial Properties ◽  
Penicillin G ◽  
Human Cell Lines ◽  
Gram Positive ◽  
Gram Negative ◽  
Dose Limiting Toxicity

We have ascertained that phenylindolylmethyldiaminopyrimidines (PIDAPs), stop the growth of USA300 MRSA at low micromolar concentrations. The controls, penicillin G and vancomycin, are able to stop the growth of MRSA at ~765 μM (256 μg/mL) and ~1.38 μM (2 μg/mL) respectively. We have also found out that PIDAPs are bactericidal at or close to the MIC. No activity was observed against Gram-negative pathogens. Other Gram-positive pathogens have not yet been tested. Based on a search through the ChEMBL database, PIDAPs are a novel class of chemicals with antimicrobial properties. A limited structure-function study suggests that the diaminopyrimidine is part of the pharmacophore. Unfortunately, we also detected potential dose-limiting toxicity on human cell lines. Further, detailed studies are needed.

scholarly journals Phenylindolylmethyldiaminopyrimidines (PIDAPs) as Potent Antimicrobials Against Staphylococcus Aureus

2021 ◽  
Author(s):  
Margaret Deming ◽  
Alatheia King ◽  
Robert A Coover ◽  
Cale D Fahrenholtz ◽  
Aurijit Sarkar
Keyword(s):  
Staphylococcus Aureus ◽  
Structure Function ◽  
Cell Lines ◽  
Human Cell ◽  
Antimicrobial Properties ◽  
Penicillin G ◽  
Human Cell Lines ◽  
Gram Positive ◽  
Gram Negative ◽  
Dose Limiting Toxicity

We have ascertained that phenylindolylmethyldiaminopyrimidines (PIDAPs), stop the growth of USA300 MRSA at low micromolar concentrations. The controls, penicillin G and vancomycin, are able to stop the growth of MRSA at ~765 μM (256 μg/mL) and ~1.38 μM (2 μg/mL) respectively. We have also found out that PIDAPs are bactericidal at or close to the MIC. No activity was observed against Gram-negative pathogens. Other Gram-positive pathogens have not yet been tested. Based on a search through the ChEMBL database, PIDAPs are a novel class of chemicals with antimicrobial properties. A limited structure-function study suggests that the diaminopyrimidine is part of the pharmacophore. Unfortunately, we also detected potential dose-limiting toxicity on human cell lines. Further, detailed studies are needed.

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.

scholarly journals Synthesis, characterization, and in vitro antimicrobial investigation of novel pyran derivatives based on 8-hydroxyquinoline

2019 ◽  
Vol 8 (1) ◽  
Author(s):  
Mohamed Rbaa ◽  
Abdelhadi Hichar ◽  
Omar Bazdi ◽  
Younes Lakhrissi ◽  
Khadija Ounine ◽  
...  
Keyword(s):  
Staphylococcus Aureus ◽  
Magnetic Resonance ◽  
Penicillin G ◽  
Diffusion Method ◽  
Bacterial Strains ◽  
Gram Positive ◽  
Gram Negative ◽  
Gram Positive Bacteria ◽  
Wide Range

Abstract Background 8-Hydroxyquinoline derivatives are known for their extensive applications in the field of analytical chemistry and separation techniques; their complexes with transition metals also exhibit antibacterial and antifungal activity. Results In the present study, we synthesized a new series of pyranoquinoline derivatives and evaluated their antibacterial activities. The structures of the synthesized compounds were characterized by Fourier transform infrared (FT-IR), hydrogen-1 nuclear magnetic resonance, carbon-13 nuclear magnetic resonance, and elemental analysis. All the prepared compounds were evaluated in vitro as antimicrobial agents against Gram-positive and Gram-negative bacterial strains (Escherichia coli (ATCC35218), Staphylococcus aureus (ATCC29213), Vibrio parahaemolyticus (ATCC17802), and Pseudomonas aeruginosa (ATCC27853)). The screening test was determined by using the standard protocol of disc diffusion method (DDM). Conclusion We have synthesized new pyranic compounds bearing an 8-hydroxyquinoline moiety on their structure. The preliminary screening results showed that all the tested compounds have a remarkable inhibitory effect on the growth of the majority of the tested bacterial strains compared to the standard antibiotic (penicillin G), and the chlorinated compound (Q1) is more active against Gram-positive bacteria than Gram-negative bacteria such as the Staphylococcus aureus strain which is the most sensitive. Gram-positive bacteria are responsible for a wide range of infectious diseases, and rising resistance in this group is causing increasing concern. Thus, this study develops novel heterocyclic compound derivatives of 8-hydroxyquinoline that have demonstrated good antibacterial activity against Gram-positive bacteria. Graphical abstract

Investigations of the influence of microgravity on the state of human cell lines

2004 ◽  
Vol 10 (5-6) ◽  
pp. 226-228
Author(s):  
L.M. Nosach ◽  
◽  
O.Yu. Povnitsa ◽  
V.L. Zhovnovata ◽  
◽  
...  
Keyword(s):  
Cell Lines ◽  
Human Cell ◽  
The State ◽  
Human Cell Lines

scholarly journals 1554. Epidemiology of Adult Bacterial Hand Infections at Two Urban Hospitals

2020 ◽  
Vol 7 (Supplement_1) ◽  
pp. S777-S778
Author(s):  
Arsheena Yassin ◽  
Christine Stavropoulos ◽  
Krystina L Woods ◽  
Jiashan Xu ◽  
Justin Carale ◽  
...  
Keyword(s):  
New York ◽  
Staphylococcus Aureus ◽  
Antibiotic Regimen ◽  
Gram Positive ◽  
Gram Negative ◽  
Streptococcus Species ◽  
Urban Hospitals ◽  
Haemophilus Parainfluenzae ◽  
Empiric Antibiotic ◽  
Gram Negative Organisms

Abstract Background Hand infections represent a major source of morbidity, which can result in hand stiffness and amputation. Early appropriate empiric antibiotic regimen may reduce the associated morbidity, hence the importance to examine local epidemiology. The aim of this study was to define the current epidemiology of adult hand infections at two urban hospitals in New York City. Methods We performed a double center, retrospective study of adult patients hospitalized from March 2018 to May 2020. Patients with positive cultures associated with the hand infections were included. Retrospectively, 100 patients were reviewed. Data on baseline demographic, clinical, surgical, microbiology, and treatment parameters were collected. Results Of the 100 patients, 76% were male, with median age of 47.5 years (35, 58.25) and average C-reactive protein (CRP) of 50.66 mg/L (± 64.64) on admission (see Table 1). Previous hospitalization within 1 year (38%), previous surgical procedures (39%) and recent IV medication use (26%) were common. 130 bacterial isolates were identified (see Table 2). The most frequent organisms were Gram-positive, with Methicillin susceptible Staphylococcus aureus (MSSA, 25.38%), Streptococcus species (20.08%), and Methicillin resistant Staphylococcus aureus (MRSA, 15.38%) being the most common. Gram-negative organisms were infrequent, with Haemophilus parainfluenzae (3.85%), Enterobacter cloacae (3.85) and Pseudomonas aeruginosa (3.08%) being the most prevalent. Of the 100 patients, 27% had polymicrobial infections, associated with trauma (6%), illicit IV use (6%) and unknown (7%) etiologies. Table 1: Baseline demographics and co-morbid conditions Table 2: Types and numbers of organisms in relation to etiologies Conclusion Within our population, the most common organisms associated with hand infections were Gram-positive, with Staphylococcus aureus and Streptococcus species being the most prevalent. Gram-negative pathogens were infrequently isolated. The results within this study can provide guidance to clinicians on assessing the appropriate empiric antibiotic regimen in patients with hand infections, and can serve as a basis for further studies identifying risk factors associated with isolation of organisms associated with hand infections. Disclosures All Authors: No reported disclosures

scholarly journals Dicalcin suppresses in vitro trophoblast attachment in human cell lines

2021 ◽  
Vol 570 ◽  
pp. 206-213
Author(s):  
Ryohei Saito ◽  
Hiromasa Satoh ◽  
Kayo Aoba ◽  
Hajime Hirasawa ◽  
Naofumi Miwa
Keyword(s):  
Cell Lines ◽  
Human Cell ◽  
Human Cell Lines
Sign in / Sign up

Export Citation Format

Share Document