Literature DB >> 22041057

Pyrrolamide DNA gyrase inhibitors: optimization of antibacterial activity and efficacy.

Brian A Sherer1, Kenneth Hull, Oluyinka Green, Gregory Basarab, Sheila Hauck, Pamela Hill, James T Loch, George Mullen, Shanta Bist, Joanna Bryant, Ann Boriack-Sjodin, Jon Read, Nancy DeGrace, Maria Uria-Nickelsen, Ruth N Illingworth, Ann E Eakin.   

Abstract

The pyrrolamides are a new class of antibacterial agents targeting DNA gyrase, an essential enzyme across bacterial species and inhibition results in the disruption of DNA synthesis and subsequently, cell death. The optimization of biochemical activity and other drug-like properties through substitutions to the pyrrole, piperidine, and heterocycle portions of the molecule resulted in pyrrolamides with improved cellular activity and in vivo efficacy.
Copyright © 2011 Elsevier Ltd. All rights reserved.

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Year:  2011        PMID: 22041057     DOI: 10.1016/j.bmcl.2011.10.010

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


  12 in total

1.  Discovery of inhibitors of 4'-phosphopantetheine adenylyltransferase (PPAT) to validate PPAT as a target for antibacterial therapy.

Authors:  Boudewijn L M de Jonge; Grant K Walkup; Sushmita D Lahiri; Hoan Huynh; Georg Neckermann; Luke Utley; Tory J Nash; Jesse Brock; Maryann San Martin; Amy Kutschke; Michele Johnstone; Valerie Laganas; Laurel Hajec; Rong-Fang Gu; Haihong Ni; Brendan Chen; Kim Hutchings; Elise Holt; David McKinney; Ning Gao; Stephania Livchak; Jason Thresher
Journal:  Antimicrob Agents Chemother       Date:  2013-09-16       Impact factor: 5.191

2.  Optimization of pyrrolamides as mycobacterial GyrB ATPase inhibitors: structure-activity relationship and in vivo efficacy in a mouse model of tuberculosis.

Authors:  Shahul Hameed P; Suresh Solapure; Kakoli Mukherjee; Vrinda Nandi; David Waterson; Radha Shandil; Meenakshi Balganesh; Vasan K Sambandamurthy; Anand Kumar Raichurkar; Abhijeet Deshpande; Anirban Ghosh; Disha Awasthy; Gajanan Shanbhag; Gulebahar Sheikh; Helen McMiken; Jayashree Puttur; Jitendar Reddy; Jim Werngren; Jon Read; Mahesh Kumar; Manjunatha R; Murugan Chinnapattu; Prashanti Madhavapeddi; Praveena Manjrekar; Reetobrata Basu; Sheshagiri Gaonkar; Sreevalli Sharma; Sven Hoffner; Vaishali Humnabadkar; Venkita Subbulakshmi; Vijender Panduga
Journal:  Antimicrob Agents Chemother       Date:  2013-10-14       Impact factor: 5.191

3.  Thermodynamic computational approach to capture molecular recognition in the binding of different inhibitors to the DNA gyrase B subunit from Escherichia coli.

Authors:  Liane Saíz-Urra; Miguel Ángel Cabrera Pérez; Matheus Froeyen
Journal:  J Mol Model       Date:  2013-04-30       Impact factor: 1.810

4.  A novel high-throughput cell-based assay aimed at identifying inhibitors of DNA metabolism in bacteria.

Authors:  Jun Fan; Boudewijn L M de Jonge; Kathy MacCormack; Shubha Sriram; Robert E McLaughlin; Helen Plant; Marian Preston; Paul R Fleming; Robert Albert; Melinda Foulk; Scott D Mills
Journal:  Antimicrob Agents Chemother       Date:  2014-09-22       Impact factor: 5.191

5.  The Rational Design, Synthesis, and Antimicrobial Properties of Thiophene Derivatives That Inhibit Bacterial Histidine Kinases.

Authors:  Thibaut Boibessot; Christopher P Zschiedrich; Alexandre Lebeau; David Bénimèlis; Catherine Dunyach-Rémy; Jean-Philippe Lavigne; Hendrik Szurmant; Zohra Benfodda; Patrick Meffre
Journal:  J Med Chem       Date:  2016-09-26       Impact factor: 7.446

6.  Discovery of Pyrazolopyridones as a Novel Class of Gyrase B Inhibitors Using Structure Guided Design.

Authors:  Jason B Cross; Jing Zhang; Qingyi Yang; Michael F Mesleh; Jan Antoinette C Romero; Bin Wang; Doug Bevan; Katherine M Poutsiaka; Felix Epie; Terence Moy; Anu Daniel; Joseph Shotwell; Brian Chamberlain; Nicole Carter; Ole Andersen; John Barker; M Dominic Ryan; Chester A Metcalf; Jared Silverman; Kien Nguyen; Blaise Lippa; Roland E Dolle
Journal:  ACS Med Chem Lett       Date:  2016-02-16       Impact factor: 4.345

7.  Tricyclic GyrB/ParE (TriBE) inhibitors: a new class of broad-spectrum dual-targeting antibacterial agents.

Authors:  Leslie W Tari; Xiaoming Li; Michael Trzoss; Daniel C Bensen; Zhiyong Chen; Thanh Lam; Junhu Zhang; Suk Joong Lee; Grayson Hough; Doug Phillipson; Suzanne Akers-Rodriguez; Mark L Cunningham; Bryan P Kwan; Kirk J Nelson; Amanda Castellano; Jeff B Locke; Vickie Brown-Driver; Timothy M Murphy; Voon S Ong; Chris M Pillar; Dean L Shinabarger; Jay Nix; Felice C Lightstone; Sergio E Wong; Toan B Nguyen; Karen J Shaw; John Finn
Journal:  PLoS One       Date:  2013-12-26       Impact factor: 3.240

8.  Exploring the Chemical Space of Benzothiazole-Based DNA Gyrase B Inhibitors.

Authors:  Žiga Skok; Michaela Barančoková; Ondřej Benek; Cristina Durante Cruz; Päivi Tammela; Tihomir Tomašič; Nace Zidar; Lucija Peterlin Mašič; Anamarija Zega; Clare E M Stevenson; Julia E A Mundy; David M Lawson; Anthony Maxwell; Danijel Kikelj; Janez Ilaš
Journal:  ACS Med Chem Lett       Date:  2020-10-15       Impact factor: 4.345

9.  Practical Synthesis and Application of Halogen-Doped Pyrrole Building Blocks.

Authors:  Andrej Emanuel Cotman; Thomas Guérin; Ivana Kovačević; Davide Benedetto Tiz; Martina Durcik; Federica Fulgheri; Štefan Možina; Daniela Secci; Maša Sterle; Janez Ilaš; Anamarija Zega; Nace Zidar; Lucija Peterlin Mašič; Tihomir Tomašič; Frédéric R Leroux; Gilles Hanquet; Danijel Kikelj
Journal:  ACS Omega       Date:  2021-03-30

10.  Isolation, characterization, anti-MRSA evaluation, and in-silico multi-target anti-microbial validations of actinomycin X2 and actinomycin D produced by novel Streptomyces smyrnaeus UKAQ_23.

Authors:  Kamal A Qureshi; Avinash D Bholay; Pankaj K Rai; Hamdoon A Mohammed; Riaz A Khan; Faizul Azam; Mariusz Jaremko; Abdul-Hamid Emwas; Piotr Stefanowicz; Mateusz Waliczek; Monika Kijewska; Ehab A Ragab; Medhat Rehan; Gamal O Elhassan; Md Jamir Anwar; Dinesh K Prajapati
Journal:  Sci Rep       Date:  2021-07-15       Impact factor: 4.379

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