Thaddeus A. Tomaszek

South College — United States

Medicine · Health Sciences

28h-index3.4kcitations62works0.02yr avg
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Research Topics

HIV/AIDS drug development and treatment(21), Bone Metabolism and Diseases(16), HIV Research and Treatment(15), Protease and Inhibitor Mechanisms(12), Natural product bioactivities and synthesis(9)

Publications62 total

Discovery of renin inhibitors containing a simple aspartate binding moiety that imparts reduced P450 inhibition
Bioorganic & Medicinal Chemistry Letters·2017Open Access
Azepanone-based inhibitors of human cathepsin S: Optimization of selectivity via the P2 substituent
Bioorganic & Medicinal Chemistry Letters·2011· 13 citedOpen Access
CCDC 637480: Experimental Crystal Structure Determination
The Cambridge Structural Database·2007Open Access
CCDC 637479: Experimental Crystal Structure Determination
The Cambridge Structural Database·2007Open Access
CCDC 637475: Experimental Crystal Structure Determination
The Cambridge Structural Database·2007Open Access
CCDC 637476: Experimental Crystal Structure Determination
The Cambridge Structural Database·2007Open Access
CCDC 637478: Experimental Crystal Structure Determination
The Cambridge Structural Database·2007Open Access
CCDC 637477: Experimental Crystal Structure Determination
The Cambridge Structural Database·2007Open Access
A highly potent inhibitor of cathepsin K (relacatib) reduces biomarkers of bone resorption both in vitro and in an acute model of elevated bone turnover in vivo in monkeys
Bone·2006· 136 cited
Structure Activity Relationships of 5-, 6-, and 7-Methyl-Substituted Azepan-3-one Cathepsin K Inhibitors
Journal of Medicinal Chemistry·2006· 70 citedOpen Access
Azepanone-Based Inhibitors of Human Cathepsin L
Journal of Medicinal Chemistry·2005· 25 citedOpen Access
2-Cyano-4-fluoro-1-thiovalylpyrrolidine analogues as potent inhibitors of DPP-IV
Bioorganic & Medicinal Chemistry Letters·2005· 26 citedOpen Access
4-Aryl-1,2,3-triazole:  A Novel Template for a Reversible Methionine Aminopeptidase 2 Inhibitor, Optimized To Inhibit Angiogenesis in Vivo
Journal of Medicinal Chemistry·2005· 188 citedOpen Access
Human Methionine Aminopeptidase Complex with 4-Aryl-1,2,3-triazole Inhibitor
2005
Benzodioxocin‐3‐ones and N‐acyl‐3‐amino‐3‐buten‐2‐ones: novel classes of cathepsin K cysteine protease inhibitors<sup>*</sup>
Journal of Peptide Research·2004· 4 cited
An Azepanone-Based Inhibitor of Human Cathepsin K with Improved Oral Bioavailability in the Rat and the Monkey
Molecular Pharmaceutics·2003· 9 cited
Potent and selective cathepsin L inhibitors do not inhibit human osteoclast resorption in vitro.
Journal of Biological Chemistry·2003Open Access
Potent and Selective Cathepsin L Inhibitors Do Not Inhibit Human Osteoclast Resorption in Vitro
Journal of Biological Chemistry·2001· 32 citedOpen Access
Azepanone-Based Inhibitors of Human and Rat Cathepsin K
Journal of Medicinal Chemistry·2001· 102 citedOpen Access
Cyclic Ketone Inhibitors of the Cysteine Protease Cathepsin K
Journal of Medicinal Chemistry·2001· 52 citedOpen Access
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Frequent Co-authors

Daniel F. Veber(22), Dennis S. Yamashita(15), Cheryl A. Janson(14), Scott K. Thompson(13), Thomas D. Meek(13), Ward W. Smith(11), Ian E. James(11), Hye-Ja Oh(11), Baoguang Zhao(11), Mark A. Levy(10), Michael W. Lark(10), Robert W. Marquis(10), Michael S. McQueney(10), Maxine Gowen(9), Renée L. DesJarlais(9), Mary J. Bossard(8), Sherin S. Abdel‐Meguid(7), Geoffrey B. Dreyer(7), David G. Tew(7), Martha S. Head(6)