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Boosting Anti-Inflammatory Potency of Zafirlukast by Designed Polypharmacology.
Schierle, Simone; Flauaus, Cathrin; Heitel, Pascal; Willems, Sabine; Schmidt, Jurema; Kaiser, Astrid; Weizel, Lilia; Goebel, Tamara; Kahnt, Astrid S; Geisslinger, Gerd; Steinhilber, Dieter; Wurglics, Mario; Rovati, G Enrico; Schmidtko, Achim; Proschak, Ewgenij; Merk, Daniel.
Affiliation
  • Schierle S; Institute of Pharmaceutical Chemistry , Goethe University Frankfurt , Max-von-Laue-Straße 9 , D-60438 Frankfurt , Germany.
  • Flauaus C; Institute of Pharmacology, College of Pharmacy , Goethe University Frankfurt , Max-von-Laue-Straße 9 , D-60438 Frankfurt , Germany.
  • Heitel P; Institute of Pharmaceutical Chemistry , Goethe University Frankfurt , Max-von-Laue-Straße 9 , D-60438 Frankfurt , Germany.
  • Willems S; Institute of Pharmaceutical Chemistry , Goethe University Frankfurt , Max-von-Laue-Straße 9 , D-60438 Frankfurt , Germany.
  • Schmidt J; Institute of Pharmaceutical Chemistry , Goethe University Frankfurt , Max-von-Laue-Straße 9 , D-60438 Frankfurt , Germany.
  • Kaiser A; Institute of Pharmaceutical Chemistry , Goethe University Frankfurt , Max-von-Laue-Straße 9 , D-60438 Frankfurt , Germany.
  • Weizel L; Institute of Pharmaceutical Chemistry , Goethe University Frankfurt , Max-von-Laue-Straße 9 , D-60438 Frankfurt , Germany.
  • Goebel T; Institute of Pharmaceutical Chemistry , Goethe University Frankfurt , Max-von-Laue-Straße 9 , D-60438 Frankfurt , Germany.
  • Kahnt AS; Institute of Pharmaceutical Chemistry , Goethe University Frankfurt , Max-von-Laue-Straße 9 , D-60438 Frankfurt , Germany.
  • Geisslinger G; Institute of Clinical Pharmacology , Goethe University Frankfurt , Theodor-Stern-Kai 7 , D-60590 Frankfurt , Germany.
  • Steinhilber D; Institute of Pharmaceutical Chemistry , Goethe University Frankfurt , Max-von-Laue-Straße 9 , D-60438 Frankfurt , Germany.
  • Wurglics M; Institute of Pharmaceutical Chemistry , Goethe University Frankfurt , Max-von-Laue-Straße 9 , D-60438 Frankfurt , Germany.
  • Rovati GE; Institute of Pharmacological Sciences , University of Milan , Via Balzaretti 9 , I-20133 Milan , Italy.
  • Schmidtko A; Institute of Pharmacology, College of Pharmacy , Goethe University Frankfurt , Max-von-Laue-Straße 9 , D-60438 Frankfurt , Germany.
  • Proschak E; Institute of Pharmaceutical Chemistry , Goethe University Frankfurt , Max-von-Laue-Straße 9 , D-60438 Frankfurt , Germany.
  • Merk D; Institute of Pharmaceutical Chemistry , Goethe University Frankfurt , Max-von-Laue-Straße 9 , D-60438 Frankfurt , Germany.
J Med Chem ; 61(13): 5758-5764, 2018 07 12.
Article in En | MEDLINE | ID: mdl-29878767
ABSTRACT
Multitarget design offers access to bioactive small molecules with potentially superior efficacy and safety. Particularly multifactorial chronic inflammatory diseases demand multiple pharmacological interventions for stable treatment. By minor structural changes, we have developed a close analogue of the cysteinyl-leukotriene receptor antagonist zafirlukast that simultaneously inhibits soluble epoxide hydrolase and activates peroxisome proliferator-activated receptor γ. The triple modulator exhibits robust anti-inflammatory activity in vivo and highlights the therapeutic potential of designed multitarget agents.
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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Tosyl Compounds / Drug Design / Anti-Inflammatory Agents, Non-Steroidal / Polypharmacology Limits: Animals / Humans Language: En Journal: J Med Chem Journal subject: QUIMICA Year: 2018 Document type: Article Affiliation country: Germany
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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Tosyl Compounds / Drug Design / Anti-Inflammatory Agents, Non-Steroidal / Polypharmacology Limits: Animals / Humans Language: En Journal: J Med Chem Journal subject: QUIMICA Year: 2018 Document type: Article Affiliation country: Germany