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Antibacterial agents

Jacqueline M Zaengle-Barone, Abigail C Jackson, David M Besse, Bradford Becken, Mehreen Arshad, Patrick C Seed, Katherine J Franz
The unabated rise in bacterial resistance to conventional antibiotics, coupled with collateral damage to normal flora incurred by overuse of broad-spectrum antibiotics, necessitates the development of new antimicrobials targeted against pathogenic organisms. Here, we explore the antibacterial outcomes and mode of action of a prochelator that exploits the production of β-lactamase enzymes by drug-resistant bacteria to convert a non-toxic compound into a metal-binding antimicrobial agent directly within the microenvironment of pathogenic organisms...
March 20, 2018: ACS Infectious Diseases
Maja Cindrić, Mihaela Perić, Marijeta Kralj, Irena Martin-Kleiner, Marie-Hélène David-Cordonnier, Hana Čipčić Paljetak, Mario Matijašić, Donatella Verbanac, Grace Karminski-Zamola, Marijana Hranjec
Novel nitro (3a-3f)- and amino (4a-4f and 5a-5f)-substituted 2-benzimidazolyl and 2-benzothiazolyl benzo[b]thieno-2-carboxamides were designed and synthesized as potential antibacterial agents. The antibacterial activity of these compounds has been evaluated against Gram-positive (Staphylococcus aureus and Enterococcus faecalis) and Gram-negative bacteria (Escherichia coli and Moraxella catarrhalis). The most promising antibacterial activity was observed for the nitro- and amino-substituted benzimidazole derivatives 3a, 4a, 5a and 5b with MICs 2-8 [Formula: see text]...
March 20, 2018: Molecular Diversity
Tang Gao, Hongliang Zeng, Huan Xu, Feng Gao, Wei Li, Shengwang Zhang, Yi Liu, Guifang Luo, Mingdan Li, Dejian Jiang, Zhigao Chen, Yong Wu, Wei Wang, Wenbin Zeng
Background: Increasing bacterial infections as well as a rise in bacterial resistance call for the development of novel and safe antimicrobial agents without inducing bacterial resistance. Nanoparticles (NPs) present some advantages in treating bacterial infections and provide an alternative strategy to discover new antibiotics. Here, we report the development of novel self-assembled fluorescent organic nanoparticles ( FONs ) with excellent antibacterial efficacy and good biocompatibility. Methods: Self-assembly of 1-(12-(pyridin-1-ium-1-yl)dodecyl)-4-(1,4,5-triphenyl-1H-imidazol-2-yl)pyridin-1-ium (TPIP) in aqueous solution was investigated using dynamic light scattering (DLS) and transmission electron microscopy (TEM)...
2018: Theranostics
Kieu-Nhi Tran, Michael J Rybak
Background: Increasing utilization of vancomycin due to the high prevalence of methicillin-resistant S. aureus (MRSA) infections has lead to the emergence of vancomycin-intermediate S. aureus (VISA) and heterogeneous VISA (hVISA). In vitro data suggest the potential for potent synergy between several beta-lactams and vancomycin. The objective of this study is to evaluate the synergy between beta-lactams and vancomycin against MRSA that is vancomycin susceptible, vancomycin susceptible Staphylococcus aureus (VSSA), hVISA, and VISA...
March 19, 2018: Antimicrobial Agents and Chemotherapy
Jinshan Guo, Wei Sun, Jimin Peter Kim, Xili Lu, Qiyao Li, Min Lin, Oliver Mrowczynski, Elias B Rizk, Juange Cheng, Guoying Qian, Jian Yang
Tissue adhesives play an important role in surgery to close wounds, seal tissues, and stop bleeding, but existing adhesives are costly, cytotoxic, or bond weakly to tissue. Inspired by the water-resistant adhesion of plant-derived tannins, we herein report a new family of bioadhesives derived from a facile, one-step Michael addition of tannic acid and gelatin under oxidizing conditions and crosslinked by silver nitrate. The oxidized polyphenol groups of tannic acid enable wet tissue adhesion through catecholamine-like chemistry, while both tannic acid and silver nanoparticles reduced from silver nitrate provide antimicrobial sources inherent within the polymeric network...
March 16, 2018: Acta Biomaterialia
Shadpour Mallakpour, Soheila Mansourzadeh
The aim of this paper was to blend the polymers, poly(N-vinyl-2-pyrrolidone) (PVP) and poly(vinyl alcohol) (PVA) to produce a novel composite materials possessing the benefits of both. CuO nanoparticles (NPs) were used as a suitable filler to fabricate the blend nanocomposites (NCs) with desired properties. First, the surface of NPs, was modified with vitamin B1 (VB1 ) as a bio-safe coupling agent. Then, the blend NCs with various ratios of modified CuO (3, 5, and 7 wt%) were fabricated under ultrasonic irradiations followed by casting/solvent evaporation method...
May 2018: Ultrasonics Sonochemistry
Sandra C Vega, Diana A Martínez, María Del S Chalá, Hernán A Vargas, Jaiver E Rosas
Multidrug resistance of pathogenic bacteria has become a public health crisis that requires the urgent design of new antibacterial drugs such as antimicrobial peptides (AMPs). Seeking to obtain new, lactoferricin B (LfcinB)-based synthetic peptides as viable early-stage candidates for future development as AMPs against clinically relevant bacteria, we designed, synthesized and screened three new cationic peptides derived from bovine LfcinB. These peptides contain at least one RRWQWR motif and differ by the copy number (monomeric, dimeric or tetrameric) and structure (linear or branched) of this motif...
2018: Frontiers in Microbiology
Happy Agarwal, Soumya Menon, S Venkat Kumar, S Rajeshkumar
A large array of diseases caused by bacterial pathogens and origination of multidrug resistance in their gene provokes the need of developing new vectors or novel drug molecules for effective drug delivery and thus, better treatment of disease. The nanoparticle has emerged as a novel drug molecule in last decade and has been used in various industrial fields like cosmetics, healthcare, agricultural, pharmaceuticals due to their high optical, electronic, medicinal properties. Use of nanoparticles as an antibacterial agent remain in current studies with metal nanoparticles like silver, gold, copper, iron and metal oxide nanoparticles like zinc oxide, copper oxide, titanium oxide and iron oxide nanoparticles...
March 15, 2018: Chemico-biological Interactions
Hari S Misra, Ganesh K Maurya, Reema Chaudhary, Chitra S Misra
Cell division and genome segregation are mutually interdependent processes, which are tightly linked with bacterial multiplication. Mechanisms underlying cell division and the cellular machinery involved are largely conserved across bacteria. Segregation of genome elements on the other hand, follows different pathways depending upon its type and the functional components encoded on these elements. Small molecules, that are known to inhibit cell division and/or resolution of intertwined circular chromosome and maintenace of DNA topology have earlier been tested as antibacterial agents...
March 2018: Microbiological Research
Patrick O Asekunowo, Rosenani A Haque, Mohd R Razali, Silas W Avicor, Mustafa F F Wajidi
A series of four benzimidazolium based nitrile-functionalized mononuclear-Ag(I)-N-heterocyclic carbene and binuclear-Ag(I)-N-heterocyclic carbene (Ag(I)-NHC) hexafluorophosphate complexes (5b-8b) were synthesized by reacting the corresponding hexafluorophosphate salts (1b-4b) with Ag2 O in acetonitrile, respectively. These compounds were characterized by1 H NMR,13 C NMR, IR, UV-visible spectroscopic techniques, elemental analyses and molar conductivity. Additionally, 8b was structurally characterized by single crystal X-ray diffraction technique...
March 13, 2018: European Journal of Medicinal Chemistry
Xianyong Feng, Peifang Wang, Jun Hou, Jin Qian, Yanhui Ao, Chao Wang
In the present work, we reported a simple method for the simultaneous phosphorus (P) doping and oxygen vacancies creation on TiO2 in a single step. The obtained P-doped TiO2 with surface oxygen vacancies (PTSOV) samples exhibited efficient photocatalytic activity for the degradation of fluoroquinolone antibacterial agent (ciprofloxacin) under visible light irradiation. The optimized sample showed a rate constant of 0.065 min-1 for degradation of ciprofloxacin (CIP) and it was about 16.2 times as high as that of TiO2 (0...
March 10, 2018: Journal of Hazardous Materials
Mohamed Abdelwahab, Nehal Salahuddin, Mohamed Gaber, Maie Mousa
Norfloxacin (NOR), a well-known antibacterial agent is also known to have potential antitumor activity. In this study, NOR was immobilized into poly(3-hydroxybutyrate/polyethylene glycol‑nickel oxide (PHB/PEG-NiO) nanocomposites using different NiO contents. The NiO nanoparticles were prepared by sol-gel method and the nanocomposites were prepared by solution cast films. Physicochemical features of nanocomposites were monitored by XRD, FTIR, SEM, TEM and TGA. PHB/PEG-5%NiO nanocomposites showed high NOR loading efficiency (60%) and a long-sustained release in comparison with other carriers...
March 13, 2018: International Journal of Biological Macromolecules
Chun-Yung Huang, Chia-Hung Kuo, Chien-Hui Wu, Ming-Wei Ku, Po-Wei Chen
Chitosan is produced by thermochemical alkaline deacetylation of chitin, but the process is usually environmentally problematic. In the present study, Illex argentinus squid pen chitin, after de-proteinization and demineralization, was pretreated with a compressional-puffing (CP) process under various puffing pressures. The CP process facilitated the increase of the crystalline index and degree of deacetylation of chitins. The CP-treated chitins were subjected to further extraction of chitosan, and four chitosan isolates (CI1-CI4) were obtained...
July 15, 2018: Food Chemistry
Menglong Liu, Danfeng He, Tao Yang, Wei Liu, Li Mao, Yang Zhu, Jun Wu, Gaoxing Luo, Jun Deng
BACKGROUND: Silver and photothermal therapy (PTT) have been widely used for eradicating the drug-resistant bacteria. However, the risks of excess of silver for humans and the low efficiency of PTT still limit their in vivo therapeutic application. Integration of two distinctive bactericides into one entity is a promising platform to improve the efficiency of antimicrobial agents. RESULTS: In this study, a chemo-photothermal therapeutic platform based on polydopamine (PDA)-coated gold nanorods (GNRs) was developed...
March 16, 2018: Journal of Nanobiotechnology
Bhupesh Bagga, Savitri Sharma, Sai Jeevan Madhuri Guda, Ritu Nagpal, Joveeta Joseph, Kodiganti Manjulatha, Ashik Mohamed, Prashant Garg
BACKGROUND: Pythium insidiosum is a parafungus that causes keratitis resembling fungal keratitis. This study compares outcome in a large cohort of patients with P insidiosum keratitis treated with antifungal drugs, to a pilot group treated with antibacterial antibiotics. METHODS: Between January 2014 and December 2016, 114 patients with culture positive P insidiosum keratitis were included in the study. A subset of culture isolates was tested in vitro for response to nine antibacterial antibiotics by disc diffusion and E test...
March 15, 2018: British Journal of Ophthalmology
Nermeen M Abu-Elala, Huda O AbuBakr, Marwa S Khattab, Samah H Mohamed, Maha A El-Hady, Rehab A Ghandour, Rania E Morsi
Despite the potential antimicrobial and water purification benefits of chitosan-based nanocomposites, there are growing concerns regarding the hazards of leached nanoparticles (NPs) to the in-contact circumference. The antibacterial performance of the nanocomposites of chitosan with silver and copper NPs and carbon nanotubes was assessed with an emphasis on their impact on fish health. The minimal inhibitory concentrations of each preparation and the growth curves of Aeromonas hydrophila exposed to different nanocomposites were measured...
March 12, 2018: International Journal of Biological Macromolecules
Amarjeet Singh, Bhavana Sharma, Renu Deswal
In the present study, we report perhaps for the first time the use of novel varieties of Brassica oleracea var. botrytis and Raphanus sativus as potential bioreductant, to synthesize highly stable silver nanoparticles (AgNPs, no aggregation observed for six months), which is a significant finding as plant extract-directed AgNPs are intrinsically unstable and tend to aggregate. The reduction of Ag+ to Ag0 nanostructures was confirmed using UVVis spectroscopy showing SPR spectra at 400-435 nm. Nanosight and transmission electron microscope (TEM) analysis showed monodisperse spherical AgNPs (4-18 nm)...
May 2018: Journal of Trace Elements in Medicine and Biology
Rajendra H Patil, Firoz A Kalam Khan, Kaivalya Jadhav, Manoj Damale, Siddique Akber Ansari, Hamad M Alkahtani, Azmat Ali Khan, Shantanu D Shinde, Rajesh Patil, Jaiprakash N Sangshetti
We report the synthesis of some new piperazine-sulphonamide linked Schiff bases as fungal biofilm inhibitors with antibacterial and antifungal potential. The biofilm inhibition result of Candida albicans proposed that the compounds 6b (IC50  = 32.1 μM) and 6j (IC50  = 31.4 μM) showed higher inhibitory activity than the standard fluconazole (IC50  = 40 μM). Compound 6d (MIC = 26.1 μg/mL) with a chloro group at the para position was found to be the most active antibacterial agent of the series against Bacillus subtilis when compared with the standard ciprofloxacin (MIC = 50 μg/mL)...
March 15, 2018: Archiv der Pharmazie
Amit Shivajirao Waghmare, Shivaji Sandu Pandit, Dayanand M Suryawanshi
AIM AND OBJECTIVE: 4H-pyran is one of the most well-known groups of synthetic heterocyclic compounds and it has attracted considerable attention of chemists in recent years because of their extensive range of biological and pharmaceutical activities. These compounds are used as antibacterial, anticancer agents, anti-coagulants, spasmolytics and anti-anaphylactic. 4H-pyran derivatives are utilized in cosmetics, pigments, biodegradable agrochemicals as well as photoactive materials. In addition, 4H-pyrans are also helpful as cognitive enhancers for the treatment of neuro degenerative diseases, including Alzheimer's disease, as well as for the treatment of schizophrenia and myoclonus...
March 14, 2018: Combinatorial Chemistry & High Throughput Screening
Assem Barakat, Abdullah M Al-Majid, Bander M Al-Qahtany, M Ali, Mohamed Teleb, Mohamed H Al-Agamy, Sehrish Naz, Zaheer Ul-Haq
BACKGROUND: Design and synthesis of pyrazole-dimedone derivatives were described by one-pot multicomponent reaction as new antimicrobial agents. These new molecular framework were synthesized in high yields with a broad substrate scope under benign conditions mediated by diethylamine (NHEt2 ). The molecular structures of the synthesized compounds were assigned based on different spectroscopic techniques (1 H-NMR,13 C-NMR, IR, MS, and CHN). RESULTS: The synthesized compounds were evaluated for their antibacterial and antifungal activities against S...
March 14, 2018: Chemistry Central Journal
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