Literature DB >> 16054358

Synthesis and SAR of novel oxazolidinones: discovery of ranbezolid.

Biswajit Das1, Sonali Rudra, Ajay Yadav, Abhijit Ray, A V S Raja Rao, A S S V Srinivas, Ajay Soni, Suman Saini, Shalini Shukla, Manisha Pandya, Pragya Bhateja, Sunita Malhotra, Tarun Mathur, S K Arora, Ashok Rattan, Anita Mehta.   

Abstract

Novel oxazolidinones were synthesized containing a number of substituted five-membered heterocycles attached to the 'piperazinyl-phenyl-oxazolidinone' core of eperezolid. Further, the piperazine ring of the core was replaced by other diamino-heterocycles. These modifications led to several compounds with potent activity against a spectrum of resistant and susceptible gram-positive organisms, along with the identification of ranbezolid (RBx 7644) as a clinical candidate.

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Year:  2005        PMID: 16054358     DOI: 10.1016/j.bmcl.2005.06.063

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


  8 in total

1.  Potent oxazolidinone antibacterials with heteroaromatic C-ring substructure.

Authors:  Hideyuki Suzuki; Iwao Utsunomiya; Koichi Shudo; Takaji Fujimura; Masakatsu Tsuji; Issei Kato; Toshiaki Aoki; Akira Ino; Tsutomu Iwaki
Journal:  ACS Med Chem Lett       Date:  2013-09-22       Impact factor: 4.345

2.  Characterization of the Core Ribosomal Binding Region for the Oxazolidone Family of Antibiotics Using Cryo-EM.

Authors:  Alexander Wright; Kieran Deane-Alder; Edward Marschall; Rebecca Bamert; Hari Venugopal; Trevor Lithgow; David W Lupton; Matthew J Belousoff
Journal:  ACS Pharmacol Transl Sci       Date:  2020-05-13

3.  Mode of action of Ranbezolid against staphylococci and structural modeling studies of its interaction with ribosomes.

Authors:  Vandana Kalia; Rajni Miglani; Kedar P Purnapatre; Tarun Mathur; Smita Singhal; Seema Khan; Sreedhara R Voleti; Dilip J Upadhyay; Kulvinder Singh Saini; Ashok Rattan; V Samuel Raj
Journal:  Antimicrob Agents Chemother       Date:  2008-12-15       Impact factor: 5.191

4.  4,5-Disubstituted oxazolidinones: High affinity molecular effectors of RNA function.

Authors:  Rajaneesh Anupam; Abhijit Nayek; Nicholas J Green; Frank J Grundy; Tina M Henkin; John A Means; Stephen C Bergmeier; Jennifer V Hines
Journal:  Bioorg Med Chem Lett       Date:  2008-05-06       Impact factor: 2.823

5.  Syntheses and biological studies of novel spiropiperazinyl oxazolidinone antibacterial agents using a spirocyclic diene derived acylnitroso Diels-Alder reaction.

Authors:  Cheng Ji; Weimin Lin; Garrett C Moraski; Jane A Thanassi; Michael J Pucci; Scott G Franzblau; Ute Möllmann; Marvin J Miller
Journal:  Bioorg Med Chem       Date:  2012-04-18       Impact factor: 3.641

6.  Antimicrobial and antiurease activities of newly synthesized morpholine derivatives containing an azole nucleus.

Authors:  Hakan Bektaş; Sule Ceylan; Neslihan Demirbaş; Sengül Alpay-Karaoğlu; Bahar Bilgin Sökmen
Journal:  Med Chem Res       Date:  2012-11-29       Impact factor: 1.965

Review 7.  The Drug Discovery and Development Industry in India-Two Decades of Proprietary Small-Molecule R&D.

Authors:  Edmond Differding
Journal:  ChemMedChem       Date:  2017-06-01       Impact factor: 3.466

8.  In Vitro Activities of LCB 01-0648, a Novel Oxazolidinone, against Gram-Positive Bacteria.

Authors:  Sang-Hun Oh; Josep Kim; Sung-Yoon Baek; Sang-Eun Chae; Hee-Soo Park; Young-Lag Cho; Jin-Hwan Kwak
Journal:  Molecules       Date:  2017-03-03       Impact factor: 4.411

  8 in total

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