Design, synthesis, in-silico studies and biological screening of quinazolinone analogues as potential antibacterial agents against MRSA.

Design, synthesis, in-silico studies and biological screening of quinazolinone analogues as potential antibacterial agents against MRSA. Bioorg Med Chem. 2019 May 10;: Authors: Qureshi SI, Chaudhari HK Abstract Type or The emergence of resistance to antibiotic has developed a complicated situation in the treatment of bacterial infections. Considering the antimicrobial resistance phenomenon as one of the greatest challenge of medicinal chemists for search of better anti-bacterial agents, which have potential narrow spectrum activity with low development of resistance potential and low toxicity to host. Cross-linking of peptidoglycan is a key step catalyze by Penicillin binding protein (PBP) to maintain integrity of cell wall in bacterial cell. However, these Penicillin binding protein (PBP) has developed resistance in methicillin-resistant Staphylococcus aureus (MRSA) due to acquisition of additional PBP2a. Various Quinazolinone analogues are reported in literature as potential anti-bacterial agents against MRSA. In present study new quinazolinone analogues has been designed, guided by molecular docking, In-silico and MM-GBSA study. Newly designed molecules have been synthesized by medicinal chemistry route and their characterization was done by using IR, NMR, &HR-MS techniques. Biological evaluation of synthesized compounds has been done on wild type Gram-negative (Escherichia coli), Gram-positive (Staphylococcus aureus) and resistant MRSA bacterial ...
Source: Bioorganic and Medicinal Chemistry - Category: Chemistry Authors: Tags: Bioorg Med Chem Source Type: research

Related Links:

Application of Antimicrobial Peptides of the Innate Immune System in Combination With Conventional Antibiotics—A Novel Way to Combat Antibiotic Resistance? Maria S. Zharkova1, Dmitriy S. Orlov1, Olga Yu. Golubeva2, Oleg B. Chakchir3, Igor E. Eliseev3, Tatyana M. Grinchuk4 and Olga V. Shamova1* 1Laboratory of Design and Synthesis of Biologically Active Peptides, Department of General Pathology and Pathophysiology, FSBSI Institute of Experimental Medicine, Saint Petersburg, Russia 2Laboratory of Nanostructures Research, Institute of Silicate Chemistry of the Russian Academy of Sciences, Saint Petersburg, Russia ...
Source: Frontiers in cellular and infection microbiology - Category: Microbiology Source Type: research
Conclusion The results of our study demonstrate that robenidine is not suitable as a sole antimicrobial agent for the treatment of Gram-negative pathogen infections due to the lack of activity against the majority of Gram-negative isolates except for A. baumannii and A. calcoaceticus. However, we demonstrated in vitro efficacy against all selected Gram-negative organisms when robenidine was tested in combination with EDTA or PMBN, including against multidrug-resistant strains. Therefore, robenidine may be an appropriate candidate as a component of a combination preparation for the treatment of otitis externa in dogs. This...
Source: Frontiers in Microbiology - Category: Microbiology Source Type: research
Conclusion This study confirms the in vitro antibacterial activity of BIOCITRO® against Gram-negative and Gram-positive bacteria. For most of the strains, the product reached the bactericidal effect at the same concentration of the bacteriostatic effect and maximum difference between MIC and MBC was two dilution steps. The less susceptible species of the study were S. enterica ssp. enterica and E. coli with MBC90 values of 256 and 128 μg/mL, respectively, while the most susceptible was C. perfringens with MBC90 of 16 μg/mL. After short exposition time to the product, the significant effect over the viability of ...
Source: Frontiers in Microbiology - Category: Microbiology Source Type: research
Raquel Ferrer-Espada1,2, Xiaojing Liu1,2, Xueping Sharon Goh1,2 and Tianhong Dai1,2* 1Wellman Center for Photomedicine, Massachusetts General Hospital, Harvard Medical School, Boston, MA, United States 2Vaccine &Immunotherapy Center, Massachusetts General Hospital, Harvard Medical School, Boston, MA, United States Polymicrobial biofilms, in which mixed microbial species are present, play a significant role in persistent infections. Furthermore, polymicrobial biofilms promote antibiotic resistance by allowing interspecies transfer of antibiotic resistance genes. In the present study, we investigated the effec...
Source: Frontiers in Microbiology - Category: Microbiology Source Type: research
Publication date: Available online 20 February 2019Source: Journal of Microbiological MethodsAuthor(s): Syed Baker, Svetlana V. Prudnikova, Anna A. Shumilova, Olga V. Perianova, Sergey M. Zharkov, Andrey KuzminAbstractThe present study describes the synthesis of silver and zinc oxide nanobactericides from the phytogenic source Bupleurum aureum. The synthesized nanobactericides were characterized and evaluated for bio-functionalization onto bacterial cellulose membrane which was synthesized by Komagataeibacterxylinus B-12068 culture strain. The synthesis of nanobacterides were initially confirmed using UV–Visible spec...
Source: Journal of Microbiological Methods - Category: Microbiology Source Type: research
Publication date: Available online 17 November 2018Source: Journal of Global Antimicrobial ResistanceAuthor(s): Helio S. Sader, Jennifer M. Streit, Cecilia G. Carvalhaes, Michael D. Huband, Michael A. PfallerAbstractBackgroundCeftaroline fosamil is approved for the treatment of acute bacterial skin and skin structure infections (ABSSSI), including those caused by methicillin-resistant Staphylococcus aureus (MRSA). We evaluated the frequency and antimicrobial susceptibility of organisms isolated from patients hospitalised with community-acquired (CA) SSSI in Europe (EUR), the Asia-Pacific region (APAC), and Latin America (L...
Source: Journal of Global Antimicrobial Resistance - Category: Infectious Diseases Source Type: research
ConclusionThis study shows low resistance to meropenem and tigecycline among the Enterobacteriaceae, and continued activity of linezolid, vancomycin and tigecycline against Gram-positive organisms. However, antimicrobial resistance continues to be problematic in Eastern Europe and requires continued surveillance.
Source: Journal of Global Antimicrobial Resistance - Category: Infectious Diseases Source Type: research
Publication date: Available online 27 October 2018Source: Inorganica Chimica ActaAuthor(s): Cillian O'Beirne, Nada F. Alhamad, Qinxi Ma, Helge Müller-Bunz, Kevin Kavanagh, Geraldine Butler, Xiangming Zhu, Matthias TackeAbstractThe rising threat of Antimicrobial Resistance (AMR) requires a novel approach to the treatment of infectious diseases. Covalently bonded silver, which has known antibacterial and antifungal properties and multiple mechanisms of action, may provide a treatment strategy when used alone or in combination with already known antimicrobial compounds. Here we describe the synthesis of eight novel silve...
Source: Inorganica Chimica Acta - Category: Chemistry Source Type: research
AbstractBackgroundTreatment and prevention of wound infection continues to be a challenging issue in clinical settings of Nepal especially in the context of globally growing problem of antimicrobial resistance. Study on opportunistic pathogens and sensitivity to commonly prescribed local antimicrobial agents are cardinal to reduce the disease burden of wound infections. The aim of this study was to determine the prevalence and antimicrobial susceptibility pattern of methicillin resistantStaphylococcus aureus (MRSA) and extended spectrum β-lactamase (ESBL) producing bacteria from wound infections of patients at a terti...
Source: Antimicrobial Resistance and Infection Control - Category: Infectious Diseases Source Type: research
ConclusionsHigh bacterial contamination of frequently touched objects with variety of potential pathogens and normal flora was detected.S. aureus was the most common bacterial isolate. Biofilm forming ability offers additional survival advantage to the organisms on these objects. Present study highlights the need of improved hand hygiene among healthcare workers and regular cleaning/disinfection of sites of frequent public contact.
Source: Antimicrobial Resistance and Infection Control - Category: Infectious Diseases Source Type: research
More News: Antimicrobial Resistance | Chemistry | Gastroenteritis | Infectious Diseases | Linezolid | Molecular Biology | MRSA | Penicillin | Science | Staphylococcus Aureus | Study | Superbugs | Toxicology | Zyvox