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      Synthesis, antimicrobial and in vitro antitumor activities of a series of 1,2,3-thiadiazole and 1,2,3-selenadiazole derivatives

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          Abstract

          Three derivatives of substituted 1,2,3-thia- or 1,2,3-selenadiazole (4a–c) were prepared and characterized by different chemical techniques. These compounds were evaluated for their antimicrobial and antitumor activities. Compounds 4a (propenoxide derivative), 4b (carbaldehyde derivative), and 4c (benzene derivative) were active against the yeast-like fungi Candida albicans. Compound 4a was active against gram-negative Escherichia coli, and compound 4c was active against the gram-positive Staphylococcus aureus. For the antitumor activity, both compounds 4b and 4c were active against all tested tumor cell lines, namely, SW480, HCT116, C32, MV3, HMT3522, and MCF-7. The activity of compound 4c was greater than that of compound 4b and more than that of the reference antitumor 5-flourouracil against the SW480, HCT116, and MCF-7 tumor cell lines. In conclusion, a number of the prepared 1,2,3-thia- or 1,2,3-selenadiazole compounds showed promising antifungal, antibacterial, and in vitro antitumor activities. Further investigations are required to explore the mechanism by which active compound are inducing their cytotoxicity.

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          Most cited references 23

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          Antibiotic Discovery: Combatting Bacterial Resistance in Cells and in Biofilm Communities

          Bacterial resistance is a rapidly escalating threat to public health as our arsenal of effective antibiotics dwindles. Therefore, there is an urgent need for new antibiotics. Drug discovery has historically focused on bacteria growing in planktonic cultures. Many antibiotics were originally developed to target individual bacterial cells, being assessed in vitro against microorganisms in a planktonic mode of life. However, towards the end of the 20th century it became clear that many bacteria live as complex communities called biofilms in their natural habitat, and this includes habitats within a human host. The biofilm mode of life provides advantages to microorganisms, such as enhanced resistance towards environmental stresses, including antibiotic challenge. The community level resistance provided by biofilms is distinct from resistance mechanisms that operate at a cellular level, and cannot be overlooked in the development of novel strategies to combat infectious diseases. The review compares mechanisms of antibiotic resistance at cellular and community levels in the light of past and present antibiotic discovery efforts. Future perspectives on novel strategies for treatment of biofilm-related infectious diseases are explored.
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            Carbapenemase-producing Enterobacteriaceae: overview of a major public health challenge.

            Bacterial resistance to antibiotics has become a major source of concern for public health. Enterobacteriaceae are among the most common human pathogens, causing community-acquired as well as hospital-acquired infections. Carbapenem-resistant Enterobacteriaceae have been increasingly reported worldwide since their first identification more than 20 years ago. Three main classes of carbapenemases have been identified: Ambler class A beta-lactamase (KPC), class B (metallo-enzymes), and class D (OXA-48 type). Klebsiella pneumoniae carbapenemases (KPC) was first reported in the United States in the late 1990s and since then worldwide, with a marked endemicity in the United States, Greece, and now Italy. Carbapenemase NDM-1 (New Delhi metallo-beta-lactamase-1) is one of the most recently reported metallo-enzymes. It has spread widely in the Indian sub-continent and now worldwide. Carbapenemases of the oxacillinase-48 type (OXA-48) have been identified mostly in Mediterranean and southern European countries with a rapid spread. An early and quick identification of carbapenemase-producing infected patients, but also of carriers, is mandatory to prevent the spread of these highly resistant pathogens. The early identification of carriers and implementing of cohorting strategies is the only means to prevent nosocomial outbreaks caused by carbapenemase, with very few, if any, therapeutic options. Copyright © 2013 Elsevier Masson SAS. All rights reserved.
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              Evolution of antimicrobial resistance among Enterobacteriaceae (focus on extended spectrum β-lactamases and carbapenemases).

              Bacteria within the family Enterobacteriaceae are important pathogens in nosocomial and community settings. Over the past two decades, antimicrobial resistance among Enterobacteriaceae dramatically escalated worldwide. The authors review the mechanisms of antimicrobial resistance among Enterobacteriaceae, epidemiology and global spread of resistance elements and discuss therapeutic options. An exhaustive search for literature relating to Enterobacteriaceae was performed using PubMed, using the following key words: Enterobacteriaceae; Klebsiella pneumoniae; Escherichia coli; antimicrobial resistance; plasmids; global epidemiology; carbapenemases (CPEs); extended spectrum β-lactamases (ESBLs) and multidrug resistance (MDR). Enterobacteriaceae are inhabitants of intestinal flora and spread easily among humans (via hand carriage, contaminated food or water or environmental sources). Antimicrobial resistance may develop via plasmids, transposons or other mobile resistance elements. Mutations conferring resistance typically increase over time; the rate of increase is amplified by selection pressure from antibiotic use. Factors that enhance spread of antimicrobial resistance include: crowding; lack of hygiene; overuse and over-the-counter use of antibiotics; tourism; refugees and international travel. Clonal spread of resistant organisms among hospitals, geographic regions and continents has globally fueled the explosive rise in resistance. The emergence and widespread dissemination of MDR clones containing novel resistance elements (particularly ESBLs and CPEs) has greatly limited therapeutic options. In some cases, infections due to MDR Enterobacteriaceae are untreatable with existing antimicrobial agents. The authors discuss current and future therapeutic options for difficult-to-treat infections due to these organisms.
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                Author and article information

                Journal
                Drug Des Devel Ther
                Drug Des Devel Ther
                Drug Design, Development and Therapy
                Drug Design, Development and Therapy
                Dove Medical Press
                1177-8881
                2015
                16 July 2015
                : 9
                : 3645-3652
                Affiliations
                [1 ]Department of Clinical Pharmacy, Faculty of Pharmacy, Jordan University of Science and Technology, Irbid, Jordan
                [2 ]Faculty of Pharmaceutical Sciences, Hashemite University, Zarqa, Jordan
                [3 ]Department of Applied Chemical Sciences, Jordan University of Science and Technology, Irbid, Jordan
                [4 ]Department of Applied Biological Sciences, Faculty of Science and Arts, Jordan University of Science and Technology, Irbid, Jordan
                [5 ]Department of Medicinal Chemistry and Pharmacognosy, Faculty of Pharmacy, Jordan University of Science and Technology, Irbid, Jordan
                Author notes
                Correspondence: Nizar M Mhaidat, Department of Clinical Pharmacy, Faculty of Pharmacy, Jordan University of Science and Technology, PO Box 3030, Irbid, 22110, Jordan, Tel +962 2 720 1000, ext 23542, Fax +962 2 720 1075, Email nizarm@ 123456just.edu.jo
                Article
                dddt-9-3645
                10.2147/DDDT.S86054
                4540747
                © 2015 Mhaidat et al. This work is published by Dove Medical Press Limited, and licensed under Creative Commons Attribution – Non Commercial (unported, v3.0) License

                The full terms of the License are available at http://creativecommons.org/licenses/by-nc/3.0/. Non-commercial uses of the work are permitted without any further permission from Dove Medical Press Limited, provided the work is properly attributed.

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                Original Research

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