Discovery of C-shaped aurone human neutrophil elastase inhibitors

Author:

Lucas S. D.12345,Carrasco M. P.12345,Gonçalves L. M.12345,Moreira R.12345,Guedes R. C.12345

Affiliation:

1. Research Institute for Medicines (iMed.ULisboa)

2. Faculty of Pharmacy

3. Universidade de Lisboa

4. 1649-003 Lisboa

5. Portugal

Abstract

Aurones were discovered as sub-micromolar HNE inhibitors. The activity is rationalized by a C-shape conformation that allows tight binding to HNE S1 and S2 pockets.

Funder

Fundação para a Ciência e a Tecnologia

Publisher

Royal Society of Chemistry (RSC)

Subject

Pharmaceutical Science,Biochemistry,Drug Discovery,Molecular Medicine,Pharmacology,Organic Chemistry

Reference22 articles.

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4. Unexpected Active-Site Flexibility in the Structure of Human Neutrophil Elastase in Complex with a New Dihydropyrimidone Inhibitor

5. F. von Nussbaum , V.Li , S.Anlauf , M.Bechem , M.Delbeck , H.Gielen-Haertwig , A.Harrenga , H.Haning , D.Karthaus , D.Lang , K.Lustig , D.Meibom , J.Mittendorf , M.Schäfer , S.Schäfer and J.Schamberger , presented in part at the XXIII International Symposium on Medicinal Chemistry, Lisbon, Portugal , 2014

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