Fluorine in Medicinal Chemistry Export

@article{citeulike:4170964, abstract = {Fluorinated compounds are synthesized in pharmaceutical research on a routine basis and many marketed compounds contain fluorine. The present review summarizes some of the most frequently employed strategies for using fluorine substituents in medicinal chemistry. Quite often, fluorine is introduced to improve the metabolic stability by blocking metabolically labile sites. However, fluorine can also be used to modulate the physicochemical properties, such as lipophilicity or basicity. It may exert a substantial effect on the conformation of a molecule. Increasingly, fluorine is used to enhance the binding affinity to the target protein. Recent 3D-structure determinations of protein complexes with bound fluorinated ligands have led to an improved understanding of the nonbonding protein-ligand interactions that involve fluorine.}, address = {Discovery Research, Pharmaceuticals Division, Roche, CH 4070 Basel, Switzerland, Fax: (+41) 61-6881745}, author = {B\"{o}hm, Hans-Joachim and Banner, David and Bendels, Stefanie and Kansy, Manfred and Kuhn, Bernd and M\"{u}ller, Klaus and Obst-Sander, Ulrike and Stahl, Martin}, citeulike-article-id = {4170964}, citeulike-linkout-0 = {http://dx.doi.org/10.1002/cbic.200301023}, citeulike-linkout-1 = {http://view.ncbi.nlm.nih.gov/pubmed/15122635}, citeulike-linkout-2 = {http://www.hubmed.org/display.cgi?uids=15122635}, citeulike-linkout-3 = {http://www3.interscience.wiley.com/cgi-bin/abstract/108561883/ABSTRACT}, doi = {10.1002/cbic.200301023}, journal = {ChemBioChem}, keywords = {flurorine, modeling, protein\_ligand\_interaction, roche}, number = {5}, pages = {637--643}, posted-at = {2009-03-13 12:49:37}, priority = {2}, title = {Fluorine in Medicinal Chemistry}, url = {http://dx.doi.org/10.1002/cbic.200301023}, volume = {5}, year = {2004} }

TY - JOUR ID - citeulike:4170964 L3 - citeulike-article-id:4170964 N2 - Fluorinated compounds are synthesized in pharmaceutical research on a routine basis and many marketed compounds contain fluorine. The present review summarizes some of the most frequently employed strategies for using fluorine substituents in medicinal chemistry. Quite often, fluorine is introduced to improve the metabolic stability by blocking metabolically labile sites. However, fluorine can also be used to modulate the physicochemical properties, such as lipophilicity or basicity. It may exert a substantial effect on the conformation of a molecule. Increasingly, fluorine is used to enhance the binding affinity to the target protein. Recent 3D-structure determinations of protein complexes with bound fluorinated ligands have led to an improved understanding of the nonbonding protein-ligand interactions that involve fluorine. IS - 5 JF - ChemBioChem AD - Discovery Research, Pharmaceuticals Division, Roche, CH 4070 Basel, Switzerland, Fax: (+41) 61-6881745 EP - 643 TI - Fluorine in Medicinal Chemistry VL - 5 SP - 637 KW - flurorine KW - modeling KW - protein_ligand_interaction KW - roche AU - Böhm, Hans-Joachim AU - Banner, David AU - Bendels, Stefanie AU - Kansy, Manfred AU - Kuhn, Bernd AU - Müller, Klaus AU - Obst-Sander, Ulrike AU - Stahl, Martin PY - 2004/// UR - http://dx.doi.org/10.1002/cbic.200301023 ER -