Sussex Drug Discovery Centre

One of the problems faced by drug discovery scientists running a screening programme is the correlation of hits (or the lack of correlation) from one assay technique compared to another, run against the same drug target. Most often this occurs as part of screening cascade, when you move from one primary screening method to a secondary confirmation method and a vast majority of hits don’t repeat or have different ranked orders of potency. This can be for good reasons, and why the secondary technique is being used as a counter screen to remove false positives.

This process can also be used to validate a new screening methodology by comparing the correlation of actives from screening file when it is run with two differing techniques against the same target. This latter example was described in a recent publication

This paper has also been described on the Practical Fragments blog. Please…

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New Drug Approvals

Avarofloxacin .HCl/Acorafloxacin. HCl
cas no  1001162-01-1 
3-Quinolinecarboxylic acid, 7-[(3E)-3-(2-amino-1-fluoroethylidene)-1-piperidinyl]-1-cyclopropyl-6-fluoro-1,4-dihydro-8-methoxy-4-oxo-, hydrochloride (1:1)
2. 7-[(3E)-3-(2-amino-1-fluoroethylidene)piperidin-1-yl]-1-cyclopropyl-6-fluoro-8-methoxy-4-oxo-1,4-dihydroquinoline-3-carboxylic acid monohydrochloride
PHASE 2 FURIEX,FOR  acute bacterial skin and skin structure (ABSSSI)Infection, 
February 25, 2013
Avarofloxacin Granted QIDP and Fast Track Designation
JNJ-Q2, JNJ-32729463-AAA

CAS NO   878592-87-1 of base

7-[3-[2-Amino-1(E)-fluoroethylidene]piperidin-1-yl]-1-cyclopropyl-6-fluoro-8-methoxy-4-oxo-1,4-dihydroquinoline-3-carboxylic acid

 

Figure imgf000063_0002

Furiex Pharmaceuticals Inc. announced that the FDA has granted Qualified Infectious Disease Product (QIDP) and Fast Track designation for avarofloxacin (JNJ-Q2). Avarofloxacin is a Phase 3-ready broad-spectrum fluoroquinolone antibiotic for the treatment of acute bacterial skin and skin-structure (ABSSSI) infections, community-acquired pneumonia and has proven to be effective in treating methicillin-resistant Staphylococcus aureus (MRSA) infections.

Avarofloxacin is an investigational novel fluoroquinolone antibiotic that has been shown to be effective in a Phase 2 study of ABSSSI infections. In this study, avarofloxacin demonstrated favorable efficacy for both early clinical response endpoints as well as all clinical cure endpoints for the intent to treat…

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Green Chemistry International

http://pubs.acs.org/doi/abs/10.1021/ed086p488

Greener Solutions for the Organic Chemistry Teaching Lab: Exploring the Advantages of Alternative Reaction Media

Department of Chemistry, University of Oregon, Eugene, OR 97403
Department of Chemistry, Hendrix College, Conway, AR 72032
Department of Chemistry, St. Olaf College, Northfield, MN 55057
J. Chem. Educ., 2009, 86 (4), p 488
DOI: 10.1021/ed086p488
Publication Date (Web): April 1, 2009

Green, Diels-Alder Reaction Procedure.pdf

A major approach for implementing green chemistry is the discovery and development of synthetic strategies that reduce the quantity of solvent needed, eliminate it altogether, or rely on new reaction media. An increasing number of examples have demonstrated that greener reaction solvents or media can enhance performance as well as reduce hazard. Here we describe four experiments designed for the undergraduate organic chemistry laboratory that illustrate both…

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