Dual Action-Based Approaches to Antibacterial Agents

Bremner, John B.; Ambrus, Joseph I.; Samosorn, Siritron

doi:10.2174/092986707780831168

Cited by 80 publications

(57 citation statements)

References 40 publications

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“…treatment, resistance has been the main and a greater challenge for scientists and pharmaceutical and biotechnology companies (Bremner et al, 2007;Kaufman, 2011). Altogether, these results revealed the importance of the specialist to perform the prescription of an antifungal agent and the urgent need for new options of treatment, including different approaches and molecules from different origins and mechanisms of action.…”

Section: (B) Ribose-5-phosphate Isomerase B From the Pathogenic Fungusmentioning

confidence: 99%

Mycoses and Antifungals: reviewing the basis of a current problem that still is a biotechnological target for marine products

et al. 2014

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Currently, the limited number of antifungals available for treating fungal infections, the increased multiresistance, and the adverse effects are the major obstacles for fungal infection therapy. Additionally, the recent emergence of opportunistic fungus infections reinforced the requirement for discovering novel antifungal agents. Herein we reviewed the main topics about fungi and its related infections, the antifungals available, their mechanism of action and resistance profile. In this work, we pointed fungi as a biotechnological target for finding new options in alternative sources such as marine products with new mechanisms of action to allow treating these dangerous infections.

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Section: (B) Ribose-5-phosphate Isomerase B From the Pathogenic Fungusmentioning

confidence: 99%

Mycoses and Antifungals: reviewing the basis of a current problem that still is a biotechnological target for marine products

et al. 2014

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“…Furthermore, as it is stated that the antitumor efficacy of many chemotherapeutic agents in many occasions is correlated with antibiotic properties (Sievert et al, 2002;Bremner et al, 2007), new approaches to promote anti-proliferation and apoptosis in cancer cells along with enhancing the antibiotic activity could lead to the development of dual/multiple targets (Hubschwerlen et al, 2003). In addition, these new agents may overcome tumor resistance.…”

Section: Introductionmentioning

confidence: 99%

One-pot three-component synthesis of peptidomimics for investigation of antibacterial and antineoplastic properties

Abdou

Bekheit

2018

Arabian Journal of Chemistry

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The a-hydroxyphosphonate generated from dialkyl phosphites and 1-phenyl-1H-pyrazole-4-carbaldehyde derivative was, in situ, trapped by isothiocyanates, isocyanates or acetic anhydride to produce dialkyl phosphorylmethyl-carbamothioates, -carbamates and/or -methyl acetates in good yields. The reactions were carried out in tetrahydrofuran (THF) in one step at room temperature, using K 2 CO 3 catalyst. Antimicrobial and antineoplastic activities of the synthesized compounds were estimated. The results showed that all new compounds cause moderate to good antibiotic activities. However, phosphorylmethylcarbamothioates exhibited the highest growth inhibition. Furthermore, selected nine new synthesized compounds were evaluated for anticancer activity against eight human tumor cell lines (MCF7, MDA-MB-435, BT-549, IGROVI, SK-OV-3, PX-3, PU-145, and HEPG2). The majority of these compounds revealed moderate to potent activity against MCF7, PU-145, and HEPG2. Among them, two of the phosphorylmethylcarbamo thioates showed excellent broad spectrum of anticancer activity with IC 50 values ranging from 16.6 to 26.9 and 17.2 to 36.9 lmol L À1 , respectively (for 5-fluorouracil IC 50 : 17.7 to 38.8 lmol L À1 ). Phosphorylmethyl methylcarbamothioate, in particular was more potent than 5-fluorouracil against all tested human carcinoma cell lines. ª 2015 The Authors. Production and hosting by Elsevier B.V. on behalf of King Saud University. This is an open access article under the CC BY-NC-ND license (http://creativecommons.org/licenses/by-nc-nd/4.0/).

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“…There are two main strategies for the discovery of new drugs; either to search for a novel lead compound or to modify the structure of a known drug 8 . In the second strategy, two or more pharmacophores are often combined in one molecule to obtain the synergistic effect 9 . Sulfonamide derivatives have numerous biological activities including antibacterial 10 , carbonic anhydrase inhibitor 11 , insulin release inducer 12 , antiviral 13 , antifungal 14 , anticancer 15 and anti-inflammatory activities 16 .…”

Section: Introductionmentioning

confidence: 99%

Design, synthesis, antimicrobial evaluation and molecular docking studies of some new 2,3-dihydrothiazoles and 4-thiazolidinones containing sulfisoxazole

Nasr

Bondock

Eid

2015

Journal of Enzyme Inhibition and Medicinal Chemistry

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Microbial resistance to the available drugs poses a serious threat in modern medicine. We report the design, synthesis and in vitro antimicrobial evaluation of new functionalized 2,3-dihydrothiazoles and 4-thiazolidinones tagged with sulfisoxazole moiety. Compound 8d was most active against Bacillis subtilis (MIC, 0.007 mg/mL). Moreover, compounds 7c-d and 8c displayed significant activities against B. subtilis and Streptococcus pneumoniae (MIC, 0.03-0.06 mg/mL and 0.06-0.12 mg/mL versus ampicillin 0.24 mg/mL and 0.12 mg/mL; respectively). Compounds 7a and 7c-d were highly potent against Escherichia coli (MIC, 0.49-0.98 mg/mL versus gentamycin 1.95 mg/mL). On the other hand, compounds 7e and 9c were fourfolds more active than amphotericin B against Syncephalastrum racemosum. Molecular docking studies showed that the synthesized compounds could act as inhibitors for the dihydropteroate synthase enzyme (DHPS). This study is a platform for the future design of more potent antimicrobial agents.

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Dual Action-Based Approaches to Antibacterial Agents

Cited by 80 publications

References 40 publications

Mycoses and Antifungals: reviewing the basis of a current problem that still is a biotechnological target for marine products

Mycoses and Antifungals: reviewing the basis of a current problem that still is a biotechnological target for marine products

One-pot three-component synthesis of peptidomimics for investigation of antibacterial and antineoplastic properties

Design, synthesis, antimicrobial evaluation and molecular docking studies of some new 2,3-dihydrothiazoles and 4-thiazolidinones containing sulfisoxazole

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