18,649 results match your criteria compound antibacterial


Synergistic antibacterial activity of an active compound derived from against methicillin-resistant and its clinical isolates.

J Microbiol Biotechnol 2021 Jul 21;31(9):1-8. Epub 2021 Jul 21.

Department of Food Science and Technology, Pukyong National University, Busan 48513, Republic of Korea.

There are a growing number of reports of hospital-acquired infections caused by pathogenic bacteria, especially methicillin-resistant (MRSA). Many plant products have recently been used as a natural means of exploring antimicrobial agents against different types of human pathogenic bacteria. The aim of this research was to isolate and identify an active molecule from that has possible antibacterial activity against various clinical isolates of MRSA. Read More

View Article and Full-Text PDF

Design, Synthesis, Antibacterial Activity, and Mechanisms of Novel 1,3,4-Thiadiazole Derivatives Containing an Amide Moiety.

J Agric Food Chem 2021 Jul 28. Epub 2021 Jul 28.

State Key Laboratory Breeding Base of Green Pesticide and Agricultural Bioengineering, Key Laboratory of Green Pesticide and Agricultural Bioengineering, Ministry of Education, Guizhou University, Guiyang 550025, P.R. China.

To discover novel antibacterial agents, a series of novel 1,3,4-thiadiazole derivatives containing an amide moiety were designed and synthesized, and their antibacterial activities were tested. Compound was designed and synthesized according to the CoMFA model. Compound exhibited higher antibacterial activities against pv. Read More

View Article and Full-Text PDF

Design, synthesis, molecular docking and in silico ADMET profile of pyrano[2,3-d]pyrimidine derivatives as antimicrobial and anticancer agents.

Bioorg Chem 2021 Jul 22;115:105186. Epub 2021 Jul 22.

Department of Biochemistry, Faculty of Science, Ain Shams University, Abbassia, Cairo, Egypt.

Pyrano[2,3-d]pyrimidine derivatives were synthesized by treating cyclic compounds containing active methylene group with aldehyde and malononitrile in butanol. The behavior of pyrano[2,3-d]pyrimidine towards some electrophlies namely triethylorthoformate followed by nitrogen nucleophiles as isobutylamine, urea, phenylthiourea, p-toluidine, o-phenylenediamine, o-aminophenol, 2-amino-4-methyl-pyridine and acetic acid with the aim of obtaining some interesting non-mixed heterocyclic compounds. All synthesized compounds to some extent have shown good antimicrobial activity against different microbial strains that had been extracted by inhibiting cell wall synthesis. Read More

View Article and Full-Text PDF

EFFECTS OF KETAMINE IN METHICILLIN RESISTANT AND IN SILICO INTERACTION WITH SORTASE A.

Can J Microbiol 2021 Jul 27. Epub 2021 Jul 27.

Federal University of Ceara, 28121, Fortaleza, CE, Brazil;

Methicillin-resistant (MRSA) is one of the main human pathogens and is responsible for many diseases ranging from skin infections to more invasive infections. These infections are dangerous and expensive to treat because these strains are resistant to a large number of conventional antibiotics. Having said that, Antibacterial effect of ketamine against MRSA strains, its mechanism of action and in silico interaction with sortase A was evaluated. Read More

View Article and Full-Text PDF

Application of Dimethyl Sulfoxide as a Therapeutic Agent and Drug Vehicle for Eye Diseases.

J Ocul Pharmacol Ther 2021 Jul 26. Epub 2021 Jul 26.

Department of Oncology, National Children Hospital, Hanoi, Vietnam.

Dimethyl sulfoxide (DMSO) is an amphipathic molecule widely used as a solvent for water-insoluble substances, cryopreserving, and cell-biological therapies. It has known properties as an inducer of cellular differentiation, a free radical scavenger, and a radioprotectant. In addition, DMSO is used for its various therapeutic and pharmaceutical properties, such as anti-inflammatory, local and systemic analgesic, antibacterial, antifungal, antiviral, and membrane penetration enhancement agents. Read More

View Article and Full-Text PDF

Identification of FDA approved drugs against SARS-CoV-2 RNA dependent RNA polymerase (RdRp) and 3-chymotrypsin-like protease (3CLpro), drug repurposing approach.

Biomed Pharmacother 2021 Jun 31;138:111544. Epub 2021 Mar 31.

Institute of Biochemistry and Biophysics, Tehran University, Tehran, Iran. Electronic address:

The RNA-dependent RNA polymerase (RdRp) and 3C-like protease (3CLpro) from SARS-CoV-2 play crucial roles in the viral life cycle and are considered the most promising targets for drug discovery against SARS-CoV-2. In this study, FDA-approved drugs were screened to identify the probable anti-RdRp and 3CLpro inhibitors by molecular docking approach. The number of ligands selected from the PubChem database of NCBI for screening was 1760. Read More

View Article and Full-Text PDF

Fabrication of Versatile Pyrazole Hydrazide Derivatives Bearing a 1,3,4-Oxadiazole Core as Multipurpose Agricultural Chemicals against Plant Fungal, Oomycete, and Bacterial Diseases.

J Agric Food Chem 2021 Jul 23. Epub 2021 Jul 23.

State Key Laboratory Breeding Base of Green Pesticide and Agricultural Bioengineering, Key Laboratory of Green Pesticide and Agricultural Bioengineering, Ministry of Education, Center for R&D of Fine Chemicals of Guizhou University, Guiyang 550025, China.

Developing multipurpose agricultural chemicals is appealing in crop protection, thus eventually realizing the reduction and efficient usage of pesticides. Herein, an array of versatile pyrazole hydrazide derivatives bearing a 1,3,4-oxadiazole core were initially synthesized and biologically evaluated the antifungal, antioomycetes, and antibacterial activities. In addition, the pyrazole ring was replaced by the correlative pyrrole, thiazole, and indole scaffolds to extend the molecular diversity. Read More

View Article and Full-Text PDF

Development of ELISA formats for polymyxin B monitoring in serum of critically ill patients.

J Pharm Biomed Anal 2021 Jul 21;204:114275. Epub 2021 Jul 21.

Faculty of Medicine, M.V. Lomonosov Moscow State University, Moscow, 119991, Russia.

Treating infections in critically ill patients often requires the use of last-line antibacterial drugs such as polymyxins with a narrow therapeutic window and high toxicity. In critically ill patients, the drug pharmacokinetics changes significantly, and as a result, the antibiotic concentrations in blood and infection foci become suboptimal, which leads to therapeutic failures or toxic manifestations. For timely dosage adjustments, a competitive ELISA-based method using antibodies to polymyxin В (PMB) was developed. Read More

View Article and Full-Text PDF

Synthesis and Biological Evaluation of Fingolimod Derivatives as Antibacterial Agents.

ACS Omega 2021 Jul 9;6(28):18465-18486. Epub 2021 Jul 9.

Drug Research Program, Division of Pharmaceutical Chemistry and Technology, Faculty of Pharmacy, University of Helsinki, Viikinkaari 5 E, FI-00014 Helsinki, Finland.

We recently identified fingolimod as a potent antibiofilm compound by screening FDA-approved drugs. To study if the antibacterial activity of fingolimod could be further improved and to explore in-depth structure-activity relationships, we synthesized 28 novel fingolimod derivatives and evaluated their efficacy against grown in planktonic/single cell and biofilms. The most effective derivatives were tested on preformed biofilms and against Gram-negative bacteria and , using fingolimod as the reference compound. Read More

View Article and Full-Text PDF

Discovery of efficient inhibitors against pyruvate dehydrogenase complex component E1 with bactericidal activity using computer aided design.

Pestic Biochem Physiol 2021 Aug 9;177:104894. Epub 2021 Jun 9.

Key Laboratory of Pesticide and Chemical Biology of Ministry of Education, College of Chemistry, Central China Normal University, 152 Luoyu Road, Wuhan 430079, PR China. Electronic address:

Computer aided optimization of lead compounds is of great significance to the design and discovery of new agrochemicals. A series of 2,6-dimethyl-4-aminopyrimidine acylhydrazones 6 was rationally designed as pyruvate dehydrogenase complex component E1 (PDHc-E1) inhibitors using computer aided drug design. Compounds in series 6 showed excellent inhibitory activity against Escherichia coli PDHc-E1, which was considerably higher than that of the lead compound A2. Read More

View Article and Full-Text PDF

Immobilizing Bactericides on Dental Resins via Electron Beam Irradiation.

J Dent Res 2021 Jul 23:220345211026569. Epub 2021 Jul 23.

Department of Biomaterials Science, Graduate School of Dentistry, Osaka University, Suita, Japan.

Polymerizable bactericides, such as quaternary ammonium compound-based monomers, have been intensively studied as candidates for immobilizing antibacterial components on dental resin. However, they predominantly exhibit a bacteriostatic behavior, rather than bactericidal, as the immobilized components are left with insufficient molecular movement to disrupt the bacterial surface structure through contact-mediated action. In this study, we developed a novel strategy to increase the density of the immobilized bactericide and enhance its antibacterial/antibiofilm properties by combining a surface-grafting technique with electron beam irradiation. Read More

View Article and Full-Text PDF

Synthesis, Antibacterial and Antifungal Activity of New 3-Aryl-5-pyrrolo[1,2-]imidazole and 5-Imidazo[1,2-]azepine Quaternary Salts.

Molecules 2021 Jul 13;26(14). Epub 2021 Jul 13.

Institute of Pharmacology and Toxicology, Antona Tsedika 14, 03057 Kyiv, Ukraine.

A series of novel 3-aryl-5-pyrrolo[1,2-]imidazole and 5-imidazo[1,2-]azepine quaternary salts were synthesized in 58-85% yields via the reaction of 3-aryl-6, 7-dihydro-5-pyrrolo[1,2-]imidazoles or 3-aryl-6,7,8,9-tetrahydro-5-imidazo[1,2-]azepines and various alkylating reagents. All compounds were characterized by H NMR, C NMR, and LC-MS. The conducted screening studies of the in vitro antimicrobial activity of the new quaternary salts derivatives established that 15 of the 18 newly synthesized compounds show antibacterial and antifungal activity. Read More

View Article and Full-Text PDF

Enhancement of Biological and Pharmacological Properties of an Encapsulated Polyphenol: Curcumin.

Molecules 2021 Jul 13;26(14). Epub 2021 Jul 13.

Division of Pharmaceutics, Faculty of Pharmacy, Rhodes University, Makhanda 6140, South Africa.

There is a dearth of natural remedies available for the treatment of an increasing number of diseases facing mankind. Natural products may provide an opportunity to produce formulations and therapeutic solutions to address this shortage. Curcumin (CUR), diferuloylmethane; I,7-bis-(4-hydroxy-3-methoxyphenyl)-1,6-heptadiene-3,5-dione is the major pigment in turmeric powder which has been reported to exhibit a number of health benefits including, antibacterial, antiviral, anti-cancer, anti-inflammatory and anti-oxidant properties. Read More

View Article and Full-Text PDF

Aspochalasin H1: A New Cyclic Aspochalasin from Hawaiian Plant-Associated Endophytic Fungus sp. FT1307.

Molecules 2021 Jul 12;26(14). Epub 2021 Jul 12.

Department of Pharmaceutical Sciences, Daniel K. Inouye College of Pharmacy, University of Hawai'i at Hilo, Hilo, HI 96720, USA.

is one of the most diverse genera, and it is chemically profound and known to produce many biologically active secondary metabolites. In the present study, a new aspochalasin H1 (), together with nine known compounds (-), were isolated from a Hawaiian plant-associated endophytic fungus sp. FT1307. Read More

View Article and Full-Text PDF

New Broth Macrodilution Volatilization Method for Antibacterial Susceptibility Testing of Volatile Agents and Evaluation of Their Toxicity Using Modified MTT Assay In Vitro.

Molecules 2021 Jul 9;26(14). Epub 2021 Jul 9.

Department of Crop Sciences and Agroforestry, Faculty of Tropical AgriSciences, Czech University of Life Sciences Prague, 16500 Prague, Czech Republic.

In this study, a new broth macrodilution volatilization method for the simple and rapid determination of the antibacterial effect of volatile agents simultaneously in the liquid and vapor phase was designed with the aim to assess their therapeutic potential for the development of new inhalation preparations. The antibacterial activity of plant volatiles (β-thujaplicin, thymohydroquinone, thymoquinone) was evaluated against bacteria associated with respiratory infections (, , , ) and their cytotoxicity was determined using a modified thiazolyl blue tetrazolium bromide assay against normal lung fibroblasts. Thymohydroquinone and thymoquinone possessed the highest antibacterial activity against , with minimum inhibitory concentrations of 4 and 8 µg/mL in the liquid and vapor phases, respectively. Read More

View Article and Full-Text PDF

Copper(II) complexes based on thiosemicarbazone ligand: Preparation, crystal structure, Hirshfeld surface, energy framework, antiMycobacterium activity, in silico and molecular docking studies.

J Inorg Biochem 2021 Jul 15;223:111543. Epub 2021 Jul 15.

Institute of Chemistry, Federal University of Uberlândia, 38400-902 Uberlândia, MG, Brazil. Electronic address:

Considering the promising previous results on the remarkable activity exhibited by cobalt(III) and manganese(II) thiosemicarbazone compounds as antibacterial agents, the present study aimed to prepare and then evaluate the antibacterial activity of two different types of Cu(II) complexes based on a 2-acetylpyridine-N(4)-methyl-thiosemicarbazone ligand (Hatc-Me), a monomer complex [CuCl(atc-Me)] and a novel dinuclear complex [{Cu(μ-atc-Me)}μ-SO]. The compounds were characterized by infrared spectra, ultraviolet visible and CHN elemental analysis. In addition, the crystalline structures of the complexes were determined by single-crystal X-ray diffraction. Read More

View Article and Full-Text PDF

Gallic acid mitigates LPS-induced inflammatory response via suppressing NF-κB signalling pathway in IPEC-J2 cells.

J Anim Physiol Anim Nutr (Berl) 2021 Jul 20. Epub 2021 Jul 20.

Key Laboratory of Feed Biotechnology of Ministry of Agriculture and Rural Affairs, Institute of Feed Research, Chinese Academy of Agricultural Sciences, Beijing, China.

Gallic acid is a phenolic compound that exhibits antibacterial, antioxidative and anti-inflammatory functions. In a previous study, we found that dietary supplementation with gallic acid decreased incidence of diarrhoea and protected intestinal integrity in weaning piglets. However, the underlying mechanism remains unclear. Read More

View Article and Full-Text PDF

Determination of antimicrobial and antimutagenic properties of some Schiff bases.

An Acad Bras Cienc 2021 19;93(3):e20191432. Epub 2021 Jul 19.

Atatürk University, Faculty of Science, Department of Biology, Erzurum, Turkey.

In this study, we aimed to investigate for the first time antimicrobial and antimutagenic activities new two Schiff bases, obtained from a primary amine (p-toluidine, o-toluidine) and an aldehyde (Helicin). Synthesized compounds characterized with elemental analysis, fourier transform infrared spectroscopy, ultraviolet-visible spectrophotometry. 1H-13C nuclear magnetic resonance spectroscopy. Read More

View Article and Full-Text PDF

Clinical efficacy of grape seed extract as an adjuvant to scaling and root planing in treatment of periodontal pockets.

J Biol Regul Homeost Agents 2021 Mar-Apr;35(2 Suppl. 1):89-96

Department of Biomedical, Surgical and Dental Sciences, Università degli Studi di Milano, Milan, Italy.

Grape seed extract (GSE), a naturally producing polyphenolic compound, is found to be a potent hostmodulatory agent and considered for management of periodontal disease. Its anti-bacterial, antioxidant, and anti-inflammatory property may aid in achieving periodontal health. To assess the clinical efficacy of GSE in adjunct to scaling and root planing (SRP) in healing of periodontal pockets. Read More

View Article and Full-Text PDF

Exploration of the Antimicrobial Effects of Benzothiazolylthiazolidin-4-One and In Silico Mechanistic Investigation.

Molecules 2021 Jul 2;26(13). Epub 2021 Jul 2.

Department of Chemistry, College of Science, Imam Abdulrahman Bin Faisal University, Dammam 31441, Saudi Arabia.

Background: Infectious diseases still affect large populations causing significant morbidity and mortality. Bacterial and fungal infections for centuries were the main factors of death and disability of millions of humans. Despite the progress in the control of infectious diseases, the appearance of resistance of microbes to existing drugs creates the need for the development of new effective antimicrobial agents. Read More

View Article and Full-Text PDF

Structure-guided microbial targeting of antistaphylococcal prodrugs.

Elife 2021 Jul 19;10. Epub 2021 Jul 19.

Department of Pediatrics, Washington University School of Medicine, St. Louis, United States.

Carboxy ester prodrugs are widely employed to increase oral absorption and potency of phosphonate antibiotics. Prodrugging can mask problematic chemical features that prevent cellular uptake and may enable tissue-specific compound delivery. However, many carboxy ester promoieties are rapidly hydrolyzed by serum esterases, limiting their therapeutic potential. Read More

View Article and Full-Text PDF

Development of antibacterial compounds that constrain evolutionary pathways to resistance.

Elife 2021 Jul 19;10. Epub 2021 Jul 19.

Department of Chemistry and Chemical Biology, Harvard University, Cambridge, United States.

Antibiotic resistance is a worldwide challenge. A potential approach to block resistance is to simultaneously inhibit WT and known escape variants of the target bacterial protein. Here we applied an integrated computational and experimental approach to discover compounds that inhibit both WT and trimethoprim (TMP) resistant mutants of dihydrofolate reductase (DHFR). Read More

View Article and Full-Text PDF

Metabolite Profiling of Malaysian Reveals Eplerenone as Novel Antibacterial Compound for Drug Repurposing Against MDR Bacteria.

Front Microbiol 2021 30;12:653562. Epub 2021 Jun 30.

Department of Biological Sciences, Sunway University, Petaling Jaya, Malaysia.

With a continuous threat of antimicrobial resistance on human health worldwide, efforts for new alternatives are ongoing for the management of bacterial infectious diseases. Natural products of land and sea, being conceived to be having fewer side effects, pose themselves as a welcome relief. In this respect, we have taken a scaffolded approach to unearthing the almost unexplored chemical constituents of Malaysian red seaweed, . Read More

View Article and Full-Text PDF

Synthetic cajaninstilbene acid derivatives eradicate methicillin-resistant Staphylococcus aureus persisters and biofilms.

Eur J Med Chem 2021 Jul 10;224:113691. Epub 2021 Jul 10.

College of Pharmacy, Jinan University, Guangzhou, 510632, PR China. Electronic address:

The Staphylococcus aureus can switch to a transient genotype-invariant dormancy, known as a persister, to survive treatment with high doses of antibiotics. This transient persister is an important reason underlying its resistance. There is an urgent need to find new antibacterial agents capable of eradicating methicillin-resistant S. Read More

View Article and Full-Text PDF

Preparation of new spiropyrazole, pyrazole and hydantoin derivatives and investigation of their antioxidant and antibacterial activities.

Chem Biodivers 2021 Jul 17. Epub 2021 Jul 17.

University of Mazandaran, Organic Chemistry, air way, Babolsar, IRAN (ISLAMIC REPUBLIC OF).

In this study, the synthesis of new spiropyrazoles, pyrazole and hydantoin hetercycles is reported by three compounent reactions of parabanic acids, hydrazine derivatives, and phenacyl bromides in the presence of triphenylphosphine as a nucleophile and triethylamine as a base in good to high yields (69-91%). Evaluation of the synthesized compounds revealed a good to excellent antioxidant activities (37.6-96. Read More

View Article and Full-Text PDF

Alstoscholarisine K, an Antimicrobial Indole from Gall-Induced Leaves of .

Org Lett 2021 Jul 16. Epub 2021 Jul 16.

State Key Laboratory of Phytochemistry and Plant Resources in West China, Kunming Institute of Botany, Chinese Academy of Sciences, Kunming 650201, P. R. China.

Alstoscholarisine K, an indole alkaloid with eight chiral carbons and featuring a novel 6/5/6/6/6/6/6/5 octacyclic architecture, was found to be specific to the gall-infected leaves of . Its structure was elucidated by spectroscopy, computational analysis, and single-crystal X-ray diffraction. The unusual highly fused cage-like pyrrolo[1,2-]pyrimidine structure with an additional -CN unit is possibly derived from a combination of monoterpenoid indole and polyamine pathways. Read More

View Article and Full-Text PDF

Role of nitazoxanide as a repurposed drug in the treatment and management of various diseases.

Drugs Today (Barc) 2021 Jul;57(7):455-473

Department of Pharmaceutical Technology, Meerut Institute of Engineering and Technology, Meerut, Uttar Pradesh, India.

Nitazoxanide (NTZ) is an orally active drug with significant postmarketing experience including more than 75 million adults and children. Presently, this drug is widely used for a number of infectious conditions and diseases. It has a wide range of applications such as antiprotozoal, anthelmintic and antiviral against various types of Gram-positive and Gram-negative bacteria, parasites and certain viruses. Read More

View Article and Full-Text PDF

Bioinorganic Synthesis of Polyrhodanine Stabilized FeO/Graphene Oxide in Microbial Supernatant Media for Anticancer and Antibacterial Applications.

Bioinorg Chem Appl 2021 25;2021:9972664. Epub 2021 Jun 25.

Department of Chemical Engineering, University of Mohaghegh Ardabili (UMA), Ardabil, Iran.

Polyrhodanines have been broadly utilized in diverse fields due to their attractive features. The effect of polyrhodanine- (PR-) based materials on human cells can be considered a controversial matter, while many contradictions exist. In this study, we focused on the synthesis of polyrhodanine/FeO modified by graphene oxide and the effect of kombucha (Ko) supernatant on results. Read More

View Article and Full-Text PDF

Antibacterial and antioxidant activities of a novel enol ether nor-sesquiterpene isolated from Myrtus nivellei Batt. & Trab.

Fitoterapia 2021 Jul 10;153:104987. Epub 2021 Jul 10.

Laboratoire de Pharmacognosie, Université de Picardie Jules Verne, Université de Liège, Univ. Lille, Junia, UMRT 1158 BioEcoAgro - Métabolites spécialisés d'origine végétale, F-80000 Amiens, France.

Myrtus nivellei is a plant traditionally used to treat diseases including infection of microbial origin. Several M. nivellei Batt. Read More

View Article and Full-Text PDF

Design, Synthesis and Antimicrobial Evaluation of Novel Benzimidazole-incorporated Naphthalimide Derivatives As Salmonella typhimurium DNA Intercalators, and Combination Researches.

Med Chem 2021 Jul 11. Epub 2021 Jul 11.

Institute of Bioorganic & Medicinal Chemistry, School of Chemistry and Chemical Engineering, Southwest University, Chongqing 400715, China.

Objective: A series of novel benzimidazole-incorporated naphthalimide derivatives were designed and prepared to overcome the increasing antibiotic resistance.

Method: The target novel benzimidazole-incorporated naphthalimide derivatives were synthesized from commercial 4-bromo-1,8-naphthalic anhydride and o-phenylene diamine by aminolysis, N-alkylation, and so on. The antimicrobial activity of the synthesized compounds was evaluated in vitro by a two-fold serial dilution technique. Read More

View Article and Full-Text PDF