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Literature DB >> 16997550

Identification of a novel boron-containing antibacterial agent (AN0128) with anti-inflammatory activity, for the potential treatment of cutaneous diseases.

Stephen J Baker¹, Tsutomu Akama, Yong-Kang Zhang, Vittorio Sauro, Chetan Pandit, Rajeshwar Singh, Maureen Kully, Jehangir Khan, Jacob J Plattner, Stephen J Benkovic, Ving Lee, Kirk R Maples.

Abstract

A series of borinic acid picolinate esters were synthesized and screened for their minimum inhibitory concentration (MIC) against Gram-positive and -negative bacteria. Our lead compounds were then screened for anti-inflammatory activity. From these studies, we identified 3-hydroxypyridine-2-carbonyloxy-bis(3-chloro-4-methylphenyl)borane (2g, AN0128) as having the best combination of anti-bacterial and anti-inflammatory activities. This compound is now in clinical development for dermatological conditions.

Entities: Chemical Disease

Mesh：

Substances：

Year: 2006 PMID： 16997550 DOI： 10.1016/j.bmcl.2006.08.130

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

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Cited

14 in total

1. A Comparison of the Structure and Bonding in the Aliphatic Boronic R-B(OH)₂ and Borinic R-BH(OH) acids (R=H; NH₂, OH, and F): A Computational Investigation.

Authors: Niny Z Rao; Joseph D Larkin; Charles W Bock
Journal: Struct Chem Date: 2015-12-30 Impact factor: 1.887

2. Probing the general time scale question of boronic acid binding with sugars in aqueous solution at physiological pH.

Authors: Nanting Ni; Sarah Laughlin; Yingji Wang; You Feng; Yujun Zheng; Binghe Wang
Journal: Bioorg Med Chem Date: 2012-03-10 Impact factor: 3.641

3. Discovery of novel orally bioavailable oxaborole 6-carboxamides that demonstrate cure in a murine model of late-stage central nervous system african trypanosomiasis.

Authors: Bakela Nare; Stephen Wring; Cyrus Bacchi; Beth Beaudet; Tana Bowling; Reto Brun; Daitao Chen; Charles Ding; Yvonne Freund; Eric Gaukel; Ali Hussain; Kurt Jarnagin; Matthew Jenks; Marcel Kaiser; Luke Mercer; Elena Mejia; Andy Noe; Matt Orr; Robin Parham; Jacob Plattner; Ryan Randolph; Donna Rattendi; Cindy Rewerts; Jessica Sligar; Nigel Yarlett; Robert Don; Robert Jacobs
Journal: Antimicrob Agents Chemother Date: 2010-07-26 Impact factor: 5.191

Identification of a novel boron-containing antibacterial agent (AN0128) with anti-inflammatory activity, for the potential treatment of cutaneous diseases.

1. A Comparison of the Structure and Bonding in the Aliphatic Boronic R-B(OH)₂ and Borinic R-BH(OH) acids (R=H; NH₂, OH, and F): A Computational Investigation.

2. Probing the general time scale question of boronic acid binding with sugars in aqueous solution at physiological pH.

3. Discovery of novel orally bioavailable oxaborole 6-carboxamides that demonstrate cure in a murine model of late-stage central nervous system african trypanosomiasis.

4. Inhibition of the class C beta-lactamase from Acinetobacter spp.: insights into effective inhibitor design.

5. Formation of pinacol boronate esters via pyridine iodoborane hydroboration.

6. [5-Hydroxy-3-phenyl-1-(pyridin-2-yl)pyrazol-5-olato]diphenylboron.

7. Effect of S-PRG Eluate on Biofilm Formation and Enzyme Activity of Oral Bacteria.

8. Click reactions and boronic acids: applications, issues, and potential solutions.

9. Diversity Analysis and Bioresource Characterization of Halophilic Bacteria Isolated from a South African Saltpan.

10. Design, Synthesis and Evaluation of Oxazaborine Inhibitors of the NLRP3 Inflammasome.