Recent advances in DNA gyrase-targeted antimicrobial agents.

Abstract:

:Antimicrobial resistance is one of the greatest challenges facing the world today. In the United States alone, it is responsible for the death of more than 20,000 people each year. DNA gyrase, a well-validated drug target, is involved in bacterial DNA replication, repair and decatenation. Currently, the fluoroquinolone class of antibacterials act via inhibition of the DNA gyrase enzyme. However, their efficacy is hindered by the increasing incidence of antimicrobial resistance. Therefore, in this review, we provide an account regarding the structure of DNA gyrase and quinoline and non-quinolone inhibitors published within the last five years (2015-2019). Further, we also discuss molecular interactions and structure-activity relationship studies of the published inhibitors.

journal_name

Eur J Med Chem

authors

Dighe SN,Collet TA

doi

10.1016/j.ejmech.2020.112326

subject

Has Abstract

pub_date

2020-08-01 00:00:00

pages

112326

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(20)30295-6

journal_volume

199

pub_type

杂志文章,评审
  • Selenium as an interesting option for the treatment of Chagas disease: A review.

    abstract::Chagas disease is one of the most prevalent tropical neglected diseases and causes high mortality and morbidity in endemic countries. Current treatments for this disease, nifurtimox and benznidazole, are ineffective in the chronic phase of the disease and produce severe adverse effects. Therefore, novel therapies are ...

    journal_title:European journal of medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.1016/j.ejmech.2020.112673

    authors: Alcolea V,Pérez-Silanes S

    更新日期:2020-11-15 00:00:00

  • Design and characterization of α-lipoic acyl shikonin ester twin drugs as tubulin and PDK1 dual inhibitors.

    abstract::Shikonin exhibits powerful anticancer activities for various cancer cells, but its poor solubility and strong toxicity hinder its development as clinical anticancer agent. We previously confirmed that shikonin and its derivatives can disturb mitosis through targeting tubulin. In this study, α-lipoic acid, the naturall...

    journal_title:European journal of medicinal chemistry

    pub_type: 杂志文章

    doi:10.1016/j.ejmech.2017.12.019

    authors: Lin HY,Han HW,Sun WX,Yang YS,Tang CY,Lu GH,Qi JL,Wang XM,Yang YH

    更新日期:2018-01-20 00:00:00

  • 1,3-Dihydro-2H-indol-2-ones derivatives: design, synthesis, in vitro antibacterial, antifungal and antitubercular study.

    abstract::1,3-dihydro-2H-indol-2-ones derivatives are reported to exhibit a wide variety of biodynamic activities such as antituberculer, anti HIV, fungicidal, antibacterial, anticonvulsant. These valid observations led us to synthesize some new indole-2-one derivative. Thus, herein we report synthesis of various 5-substituted-...

    journal_title:European journal of medicinal chemistry

    pub_type: 杂志文章

    doi:10.1016/j.ejmech.2011.09.023

    authors: Akhaja TN,Raval JP

    更新日期:2011-11-01 00:00:00

  • Dihydropyrimidinone/1,2,3-triazole hybrid molecules: Synthesis and anti-varicella-zoster virus (VZV) evaluation.

    abstract::By combining the structural features of dihydropyrimidinone and 1,2,3-triazole heterocycles, novel hybrid compounds were synthesized using a simple and convenient method. A series of novel mono and bis 1,2,3-triazole was synthesized via copper-catalyzed Huisgen azide-alkyne cycloadditions (CuAAC) under microwave irrad...

    journal_title:European journal of medicinal chemistry

    pub_type: 杂志文章

    doi:10.1016/j.ejmech.2018.06.028

    authors: Kaoukabi H,Kabri Y,Curti C,Taourirte M,Rodriguez-Ubis JC,Snoeck R,Andrei G,Vanelle P,Lazrek HB

    更新日期:2018-07-15 00:00:00

  • Glycosylation enhances the anti-migratory activities of isomalyngamide A analogs.

    abstract::Three, new, fully synthetic glycosylated isomalyngamide A analogs 4-6 were prepared and evaluated for their anti-migratory activities in human breast cancer cells. The results of the study show that two glycosylated derivatives 4 and 5, containing mannose and galactose appendages, suppress metastatic events (e.g., mig...

    journal_title:European journal of medicinal chemistry

    pub_type: 杂志文章

    doi:10.1016/j.ejmech.2013.03.044

    authors: More SV,Chang TT,Chiao YP,Jao SC,Lu CK,Li WS

    更新日期:2013-06-01 00:00:00

  • Antagonizing STAT3 activation with benzo[b]thiophene 1, 1-dioxide based small molecules.

    abstract::STAT3 is an attractive therapeutic target for cancer therapy. However, due to low potency or poor druggability, none of its inhibitors are clinically available. Herein, a series of aminobenzo[b]thiophene 1, 1-dioxides with good drug-likeness properties were designed, synthesized and evaluated as STAT3 inhibitors. Most...

    journal_title:European journal of medicinal chemistry

    pub_type: 杂志文章

    doi:10.1016/j.ejmech.2016.09.068

    authors: Zhang W,Ma T,Li S,Yang Y,Guo J,Yu W,Kong L

    更新日期:2017-01-05 00:00:00

  • Identification of novel benzothiopyranone compounds against Mycobacterium tuberculosis through scaffold morphing from benzothiazinones.

    abstract::In this study, three novel series of benzoxazinone, benzothiopyranone and benzopyranone derivatives were designed through scaffold morphing from benzothiazinones to target DprE1. All compounds were evaluated for their in vitro activities against Mycobacterium tuberculosis and cytotoxicity against Vero cell line. Among...

    journal_title:European journal of medicinal chemistry

    pub_type: 杂志文章

    doi:10.1016/j.ejmech.2018.09.042

    authors: Li P,Wang B,Zhang X,Batt SM,Besra GS,Zhang T,Ma C,Zhang D,Lin Z,Li G,Huang H,Lu Y

    更新日期:2018-12-05 00:00:00

  • Design, synthesis and screening of 1, 2, 4-triazinone derivatives as potential antitumor agents with apoptosis inducing activity on MCF-7 breast cancer cell line.

    abstract::Some triazinone derivatives are designed and synthesized as potential antitumor agents. Triazinone derivatives 4c, 5e and 7c show potent anticancer activity over MCF-7 breast cancer cells higher than podophyllotoxin (podo) by approximate 6-fold. DNA flow cytometry analysis for the compounds 3c, 4c, 5e, 6c and 7c show ...

    journal_title:European journal of medicinal chemistry

    pub_type: 杂志文章

    doi:10.1016/j.ejmech.2018.07.003

    authors: Zaki I,Abdelhameid MK,El-Deen IM,Abdel Wahab AHA,Ashmawy AM,Mohamed KO

    更新日期:2018-08-05 00:00:00

  • Design, synthesis, pharmacological evaluation and molecular dynamics of β-amino acids morphan-derivatives as novel ligands for opioid receptors.

    abstract::Structure-Activity Relationship (SAR) is a current approach in the design of new pharmacological agents. We previously reported the synthesis of a novel analogue of morphine, a 2-azabicyclo[3.3.1]nonane, which contains a β-amino acid. This bicyclic core exhibits two distinctive chemical handles for further elaboration...

    journal_title:European journal of medicinal chemistry

    pub_type: 杂志文章

    doi:10.1016/j.ejmech.2015.06.025

    authors: Nieto CT,Gonzalez-Nunez V,Rodríguez RE,Diez D,Garrido NM

    更新日期:2015-08-28 00:00:00

  • Synthesis of new N3-substituted dihydropyrimidine derivatives as L-/T- type calcium channel blockers.

    abstract::Cardiovascular diseases (CVDs) are the main cause of deaths worldwide. Up-to-date, hypertension is the most significant contributing factor to CVDs. Recent clinical studies recommend calcium channel blockers (CCBs) as effective treatment alone or in combination with other medications. Being the most clinically useful ...

    journal_title:European journal of medicinal chemistry

    pub_type: 杂志文章

    doi:10.1016/j.ejmech.2017.03.080

    authors: Teleb M,Zhang FX,Farghaly AM,Aboul Wafa OM,Fronczek FR,Zamponi GW,Fahmy H

    更新日期:2017-07-07 00:00:00

  • Heterocyclic pharmacochemistry of new rhinovirus antiviral agents: A combined computational and experimental study.

    abstract::Rhinovirus (RV), member of the Enterovirus genus, is known to be involved in more than half of the common colds. Through advances in molecular biology, rhinoviruses have also been associated with exacerbations of chronic pulmonary diseases (e.g. asthma, chronic obstructive pulmonary disease (COPD) and cystic fibrosis)...

    journal_title:European journal of medicinal chemistry

    pub_type: 杂志文章

    doi:10.1016/j.ejmech.2017.09.036

    authors: Da Costa L,Scheers E,Coluccia A,Rosetti A,Roche M,Neyts J,Terme T,Cirilli R,Mirabelli C,Silvestri R,Vanelle P

    更新日期:2017-11-10 00:00:00

  • Synthesis and antiproliferative activity of a series of novel 6-substituted pyrido[3,2-d]pyrimidines as potential nonclassical lipophilic antifolates targeting dihydrofolate reductase.

    abstract::Dihydrofolate reductase (DHFR) has been a well-recognized target for the treatment of many diseases. Based on 8,10-dideazaminopterins, which are classical antifolates that potently inhibit DHFR, we have designed a series of novel 2,4-diamino-6-substituted pyrido[3,2-d]pyrimidines. By removing the glutamate moiety and ...

    journal_title:European journal of medicinal chemistry

    pub_type: 杂志文章

    doi:10.1016/j.ejmech.2017.01.033

    authors: Wang M,Yang J,Yuan M,Xue L,Li H,Tian C,Wang X,Liu J,Zhang Z

    更新日期:2017-03-10 00:00:00

  • Synthesis, characterization and antiamoebic activity of new indole-3-carboxaldehyde thiosemicarbazones and their Pd(II) complexes.

    abstract::In continuation of our research on thiosemicarbazones and their metal complexes as antiamoebic agents, a new series of indole-3-carboxaldehyde thiosemicarbazones (TSC) 1-7 were prepared by condensing indole-3-carboxaldehyde with cycloalkylaminothiocarbonyl hydrazines. Their palladium(II) complexes of the [Pd(TSC)Cl2] ...

    journal_title:European journal of medicinal chemistry

    pub_type: 杂志文章

    doi:10.1016/j.ejmech.2007.02.012

    authors: Husain K,Abid M,Azam A

    更新日期:2007-10-01 00:00:00

  • Structure-based discovery of selective BRPF1 bromodomain inhibitors.

    abstract::Bromodomain and plant homeodomain (PHD) finger containing protein 1 (BRPF1) is a member of subfamily IV of the human bromodomains. Experimental evidence suggests that BRPF1 is involved in leukemia. In a previous high-throughput docking campaign we identified several chemotypes targeting the BRPF1 bromodomain. Here, ph...

    journal_title:European journal of medicinal chemistry

    pub_type: 杂志文章

    doi:10.1016/j.ejmech.2018.05.037

    authors: Zhu J,Zhou C,Caflisch A

    更新日期:2018-07-15 00:00:00

  • Novel tacrine-1,2,3-triazole hybrids: In vitro, in vivo biological evaluation and docking study of cholinesterase inhibitors.

    abstract::A new series of tacrine-1,2,3-triazole hybrids were designed, synthesized, and evaluated as potent dual cholinesterase inhibitors. Most of synthesized compounds showed good in vitro inhibitory activities toward both acetylcholinesterase (AChE) and butyrylcholinesterase (BChE). Among them, 7-chloro-N-((1-(4-methoxybenz...

    journal_title:European journal of medicinal chemistry

    pub_type: 杂志文章

    doi:10.1016/j.ejmech.2016.11.008

    authors: Najafi Z,Mahdavi M,Saeedi M,Karimpour-Razkenari E,Asatouri R,Vafadarnejad F,Moghadam FH,Khanavi M,Sharifzadeh M,Akbarzadeh T

    更新日期:2017-01-05 00:00:00

  • Novel 1,3-thiazolidin-4-one derivatives as promising anti-Candida agents endowed with anti-oxidant and chelating properties.

    abstract::Pursuing our recent outcomes regarding the antifungal activity of N-substituted 1,3-thiazolidin-4-ones, we synthesized thirty-six new derivatives introducing aliphatic, cycloaliphatic and heteroaromatic moieties at N1-hydrazine connected with C2 position of the thiazolidinone nucleus and functionalizing the lactam nit...

    journal_title:European journal of medicinal chemistry

    pub_type: 杂志文章

    doi:10.1016/j.ejmech.2016.04.012

    authors: Secci D,Carradori S,Bizzarri B,Chimenti P,De Monte C,Mollica A,Rivanera D,Zicari A,Mari E,Zengin G,Aktumsek A

    更新日期:2016-07-19 00:00:00

  • Synthesis, structure and structure-activity relationship analysis of 3-tert-butoxycarbonyl-2-arylthiazolidine-4-carboxylic acid derivatives as potential antibacterial agents.

    abstract::Nine 2-arylthiazolidine-4-carboxylic acid derivatives and nine 3-tert-butoxycarbonyl-2-arylthiazolidine-4-carboxylic acid derivatives were synthesized to screen for their antibacterial activities. Compounds 5, 14-18 were first reported. Their chemical structures were clearly determined by (1)H NMR, (13)C NMR, ESI mass...

    journal_title:European journal of medicinal chemistry

    pub_type: 杂志文章

    doi:10.1016/j.ejmech.2009.04.014

    authors: Song ZC,Ma GY,Lv PC,Li HQ,Xiao ZP,Zhu HL

    更新日期:2009-10-01 00:00:00

  • 4(1H)-quinolone derivatives overcome acquired resistance to anti-microtubule agents by targeting the colchicine site of β-tubulin.

    abstract::Developing new therapeutic strategies to overcome drug resistance of cancer cells is an ongoing endeavor. From among 2 million chemicals, we identified ethyl 4-oxo-2-phenyl-1,4-dihydroquinoline-6-carboxylate (AS1712) as a low-toxicity inhibitor of lung cancer cell proliferation and xenograft tumor growth. We show that ...

    journal_title:European journal of medicinal chemistry

    pub_type: 杂志文章

    doi:10.1016/j.ejmech.2019.111584

    authors: Lin MS,Hong TM,Chou TH,Yang SC,Chung WC,Weng CW,Tsai ML,Cheng TR,Chen JJW,Lee TC,Wong CH,Chein RJ,Yang PC

    更新日期:2019-11-01 00:00:00

  • Platinated benzonaphthyridone is a stronger inhibitor of poly(ADP-ribose) polymerase-1 and a more potent anticancer agent than is the parent inhibitor.

    abstract::Inhibitors of poly(ADP-ribose) polymerase-1 (PARP-1) have shown to be promising in clinical trials against cancer and other diseases, and lots of efforts have been put into the development of organic compounds as more potent PARP-1 inhibitors. Here we describe a strategy to conveniently obtain metal-based PARP-1 inhib...

    journal_title:European journal of medicinal chemistry

    pub_type: 杂志文章

    doi:10.1016/j.ejmech.2013.10.062

    authors: Wang B,Qian H,Yiu SM,Sun J,Zhu G

    更新日期:2014-01-01 00:00:00

  • Synthesis and characterization of novel phosphonocarboxylate inhibitors of RGGT.

    abstract::Phosphonocarboxylate (PC) analogs of the anti-osteoporotic drugs, bisphosphonates, represent the first class of selective inhibitors of Rab geranylgeranyl transferase (RabGGTase, RGGT), an enzyme implicated in several diseases including ovarian, breast and skin cancer. Here we present the synthesis and biological char...

    journal_title:European journal of medicinal chemistry

    pub_type: 杂志文章

    doi:10.1016/j.ejmech.2014.06.062

    authors: Coxon FP,Joachimiak L,Najumudeen AK,Breen G,Gmach J,Oetken-Lindholm C,Way R,Dunford JE,Abankwa D,Błażewska KM

    更新日期:2014-09-12 00:00:00

  • Discovery of novel triazolo[4,3-b]pyridazin-3-yl-quinoline derivatives as PIM inhibitors.

    abstract::PIM kinase family (PIM-1, PIM-2 and PIM-3) is an appealing target for the discovery and development of selective inhibitors, useful in various disease conditions in which these proteins are highly expressed, such as cancer. The significant effort put, in the recent years, towards the development of small molecules exh...

    journal_title:European journal of medicinal chemistry

    pub_type: 杂志文章

    doi:10.1016/j.ejmech.2019.02.022

    authors: Martínez-González S,Rodríguez-Arístegui S,Gómez de la Oliva CA,Hernández AI,González Cantalapiedra E,Varela C,García AB,Rabal O,Oyarzabal J,Bischoff JR,Klett J,Albarrán MI,Cebriá A,Ajenjo N,García-Serelde B,Gómez-Casero E,

    更新日期:2019-04-15 00:00:00

  • Fructose-1,6-bisphosphatase inhibitors: A new valid approach for management of type 2 diabetes mellitus.

    abstract::The rising incidence of diabetes and confines allied with clinical therapies emphasized the need to explore new molecular targets to develop novel, effective and safer antihyperglycemic agents. Excessive endogenous glucose production by gluconeogenesis is a primary determinant of hyperglycemia in patients with type 2 ...

    journal_title:European journal of medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.1016/j.ejmech.2017.09.029

    authors: Kaur R,Dahiya L,Kumar M

    更新日期:2017-12-01 00:00:00

  • Synthesis, antibacterial evaluation and QSAR studies of 7-[4-(5-aryl-1,3,4-oxadiazole-2-yl)piperazinyl] quinolone derivatives.

    abstract::A series of 7-[4-(5-aryl-1,3,4-oxadiazole-2-yl)piperazinyl] quinolones (I-XXI) were synthesized using an appropriate synthetic route and characterized by elemental and spectral analysis. The antibacterial activities of all the synthesized compounds were evaluated against identifiable bacterial strains. Compounds III, ...

    journal_title:European journal of medicinal chemistry

    pub_type: 杂志文章

    doi:10.1016/j.ejmech.2011.04.035

    authors: Kumar R,Kumar A,Jain S,Kaushik D

    更新日期:2011-09-01 00:00:00

  • Optimization of novel oxidative DIMs as Nur77 modulators of the Nur77-Bcl-2 apoptotic pathway.

    abstract::Nur77, an orphan nuclear receptor, is a member of the nuclear receptor superfamily. Nur77 plays important roles in various biological processes. Previously we reported that BI1071(DIM-C-pPhCF3+MeSO3-), an oxidized form and methanesulfonate salt of (4-CF3-Ph-C-DIM), can modulate Nur77's non-genomic apoptotic pathway th...

    journal_title:European journal of medicinal chemistry

    pub_type: 杂志文章

    doi:10.1016/j.ejmech.2020.113020

    authors: Tu X,Chen X,Zhang D,Gao M,Liang J,Bao G,Zhang J,Peng S,Zhang X,Zeng Z,Su Y

    更新日期:2021-02-05 00:00:00

  • β-Ionone and its analogs as promising anticancer agents.

    abstract::β-Ionone is an end-ring analog of β-carotenoids which widely distributed in fruit and vegetables. Recent studies have demonstrated anti-proliferative, anti-metastatic and apoptosis induction properties of β-ionone in vitro and in vivo. Also, the studies have focused on investigating the β-ionone action on different ty...

    journal_title:European journal of medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.1016/j.ejmech.2016.07.037

    authors: Ansari M,Emami S

    更新日期:2016-11-10 00:00:00

  • Translocator protein ligands based on N-methyl-(quinolin-4-yl)oxypropanamides with properties suitable for PET radioligand development.

    abstract::Modifications to an N-methyl-(quinolin-4-yl)oxypropanamide scaffold were explored to discover leads for developing new radioligands for PET imaging of brain TSPO (translocator protein), a biomarker of neuroinflammation. Whereas contraction of the quinolinyl portion of the scaffold or cyclization of the tertiary amido ...

    journal_title:European journal of medicinal chemistry

    pub_type: 杂志文章

    doi:10.1016/j.ejmech.2016.08.046

    authors: Brouwer C,Jenko KJ,Zoghbi SS,Morse CL,Innis RB,Pike VW

    更新日期:2016-11-29 00:00:00

  • Design, synthesis and antifungal activities of novel pyrrole alkaloid analogs.

    abstract::A series of novel analogs of pyrrole alkaloid were designed and synthesized by a facile method and their structures were characterized by 1H NMR, 13C NMR and high-resolution mass spectrometry (HRMS). The structure of compound 2a was identified by 2D NMR including heteronuclear multiple-quantum coherence (HMQC), hetero...

    journal_title:European journal of medicinal chemistry

    pub_type: 杂志文章

    doi:10.1016/j.ejmech.2011.01.031

    authors: Wang MZ,Xu H,Liu TW,Feng Q,Yu SJ,Wang SH,Li ZM

    更新日期:2011-05-01 00:00:00

  • Known drug space as a metric in exploring the boundaries of drug-like chemical space.

    abstract::In this work, marketed drug compounds (or known drug space) were used as a metric to test the principles of eliminating parent structures of the nitrenium ion (aryl-amine/nitro compounds) as well as sulphur and halogen containing molecules from screening compound collections. Molecules containing such moieties and/or ...

    journal_title:European journal of medicinal chemistry

    pub_type: 杂志文章

    doi:10.1016/j.ejmech.2009.08.014

    authors: Mirza A,Desai R,Reynisson J

    更新日期:2009-12-01 00:00:00

  • Structural analysis of inhibition of Mycobacterium tuberculosis methionine aminopeptidase by bengamide derivatives.

    abstract::Natural product-derived bengamides possess potent antiproliferative activity and target human methionine aminopeptidases for their cellular effects. Using bengamides as a template, several derivatives were designed and synthesized as inhibitors of methionine aminopeptidases of Mycobacterium tuberculosis, and initial a...

    journal_title:European journal of medicinal chemistry

    pub_type: 杂志文章

    doi:10.1016/j.ejmech.2011.11.017

    authors: Lu JP,Yuan XH,Ye QZ

    更新日期:2012-01-01 00:00:00

  • Targeting Aryl hydrocarbon receptor for next-generation immunotherapies: Selective modulators (SAhRMs) versus rapidly metabolized ligands (RMAhRLs).

    abstract::Aryl Hydrocarbon Receptor (AhR) constitutes a major network hub of genomic and non-genomic signaling pathways, connecting host's immune cells to environmental factors. It shapes innate and adaptive immune processes to environmental stimuli with species-, cell- and tissue-type dependent specificity. Although an ever in...

    journal_title:European journal of medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.1016/j.ejmech.2019.111842

    authors: Dolciami D,Ballarotto M,Gargaro M,López-Cara LC,Fallarino F,Macchiarulo A

    更新日期:2020-01-01 00:00:00