Literature DB >> 15357962

Synthesis and structural-activity relationships of 3-hydroxyquinazoline-2,4-dione antibacterial agents.

Tuan P Tran1, Edmund L Ellsworth, Michael A Stier, John M Domagala, H D Showalter, Stephen J Gracheck, Martin A Shapiro, Themis E Joannides, Rajeshwar Singh.   

Abstract

A series of 3-hydroxyquinazoline-2,4-diones was synthesized and evaluated for antibacterial activity. This series represents a novel addition to the DNA gyrase inhibitor class of antibacterials. Appropriate substitutions onto the core template yielded compounds with excellent potency against E. coli gyrase and significant in vitro Gram-negative and Gram-positive antibacterial activity.

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Year:  2004        PMID: 15357962     DOI: 10.1016/j.bmcl.2004.06.063

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  7 in total

1.  High-throughput screening for inhibitors of Mycobacterium tuberculosis H37Rv.

Authors:  Subramaniam Ananthan; Ellen R Faaleolea; Robert C Goldman; Judith V Hobrath; Cecil D Kwong; Barbara E Laughon; Joseph A Maddry; Alka Mehta; Lynn Rasmussen; Robert C Reynolds; John A Secrist; Nice Shindo; Dustin N Showe; Melinda I Sosa; William J Suling; E Lucile White
Journal:  Tuberculosis (Edinb)       Date:  2009-09-15       Impact factor: 3.131

2.  Probing the differential interactions of quinazolinedione PD 0305970 and quinolones with gyrase and topoisomerase IV.

Authors:  Xiao-Su Pan; Katherine A Gould; L Mark Fisher
Journal:  Antimicrob Agents Chemother       Date:  2009-06-29       Impact factor: 5.191

3.  Synthesis of new quinazolin-2,4-diones as anti-Leishmania mexicana agents.

Authors:  Eduardo Enciso; Juan I Sarmiento-Sánchez; Héctor S López-Moreno; Adrián Ochoa-Terán; Ulises Osuna-Martínez; Evangelina Beltrán-López
Journal:  Mol Divers       Date:  2016-08-16       Impact factor: 2.943

4.  Efficient Synthesis of the 2-amino-6-chloro-4-cyclopropyl-7-fluoro-5-methoxy-pyrido[1,2-c]pyrimidine-1,3-dione core ring system.

Authors:  Jonathan D Rosen; Nadezhda German; Robert J Kerns
Journal:  Tetrahedron Lett       Date:  2009-02-18       Impact factor: 2.415

5.  I2/TBHP mediated domino synthesis of 2-(2,4-dioxo-1,4-dihydroquinazolin-3(2H)-yl)-N-aryl/alkyl benzamides and evaluation of their anticancer and docking studies.

Authors:  Anil Kumar Soda; Phani Krishna C S; Sai Krishna Chilaka; Vamshi Krishna E; Sunil Misra; Sridhar Madabhushi
Journal:  RSC Adv       Date:  2022-06-06       Impact factor: 4.036

6.  Novel and Structurally Diversified Bacterial DNA Gyrase Inhibitors Discovered through a Fluorescence-Based High-Throughput Screening Assay.

Authors:  Eddy E Alfonso; Zifang Deng; Daniel Boaretto; Becky L Hood; Stefan Vasile; Layton H Smith; Jeremy W Chambers; Prem Chapagain; Fenfei Leng
Journal:  ACS Pharmacol Transl Sci       Date:  2022-09-02

7.  1-{[(2,3-Dihydro-1H-inden-2-yl)-oxy]meth-yl}quinazoline-2,4(1H,3H)-dione.

Authors:  Nasser R El-Brollosy; Necmi Dege; Güneş Demirtaş; Mohamed I Attia; Ali A El-Emam; Orhan Büyükgüngör
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2012-05-23
  7 in total

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