Recent employee publications

Discovery of N-Substituted 3-Amino-4-(3-boronopropyl)pyrrolidine-3-carboxylic Acids as Highly Potent Third-Generation Inhibitors of Human Arginase I and II

Michael C. Van Zandt, G. Erik Jagdmann, Darren L. Whitehouse, Minkoo Ji, Jennifer Savoy, Olga Potapova, Alexandra Cousido-Siah, Andre Mitschler, Eduardo I. Howard, Anna Marie Pyle, and Alberto D. Podjarny
Journal of Medicinal Chemistry 2019 62 (17), 8164-8177
DOI: 10.1021/acs.jmedchem.9b00931

Small molecules that target group II introns are potent antifungal agents

Fedorova, Olga; Jagdmann, G. Erik; Adams, Rebecca L.; Yuan, Lin; Van Zandt, Michael; Pyle, Anna Marie
Nature Chemical Biology (2018), 14 (12), 1073-1078
PMID: 30323219. PMCID: PMC6239893. DOI: 10.1038/s41589-018-0142-0

Method of preparing (3r,4s)-3-acetamido-4-allyl-n-(tert-butyl) pyrrolidine-3-carboxamide

Van Zandt, Michael C.; Savoy, Jennifer L.
WO 2018209290 A1, 60 pp (2018)
https://patents.google.com/patent/WO2018209290A1/en

Total synthesis of protectin DX, a potent proresolving lipid mediator

Dworak, Jessica; Jagdmann, G. Erik; Van Zandt, Michael
Abstracts of Papers, 256th ACS National Meeting & Exposition, Boston, MA, United States, August 19-23, 2018 (2018), ORGN-648

Editing N-Glycan Site Occupancy with Small-Molecule Oligosaccharyltransferase Inhibitors

Rinis, Natalia; Golden, Jennifer E.; Marceau, Caleb D.; Carette, Jan E.; Van Zandt, Michael C.; Gilmore, Reid; Contessa, Joseph N.
Cell Chemical Biology (2018), 25(10), 1231-1241.e4
PMID: 30078634. PMCID: PMC6337728. DOI: 10.1016/j.chembiol.2018.07.005

Preparation of boron compounds and using compositions and methods for inhibiting arginase activity

Sjogren, Eric B.; Li, Jim; Chen, Lijing; Billedeau, Roland J.; Stanton, Timothy F.; Van Zandt, Michael; Whitehouse, Darren; Jagdmann, Gunnar E., Jr.; Petersen, Lene Raunkjaer; Parlati, Francesco; et al.
WO 2018119440 A1, 220 pp (2018)
https://patents.google.com/patent/WO2017075363A1/en

Compositions and methods relating to salts of specialized pro-resolving mediators of inflammation

Sciavolino, Frank C.; Mathias, Gary; Van Zandt, Michael; Jagdmann, G. Erik; Dworak, Jessica
WO 2017210604 A1, 109 pp (2018)
https://patents.google.com/patent/US20180116990A1/

Topical application of aminoglycoside antibiotics enhances host resistance to viral infections in a microbiota-independent manner

Gopinath, Smita; Kim, Myoungjoo V.; Rakib, Tasfia; Wong, Patrick W.; van Zandt, Michael; Barry, Natasha A.; Kaisho, Tsuneyasu; Goodman, Andrew L.; Iwasaki, Akiko
Nature Microbiology (2018), 3(5), 611-621
PMID: 29632368. PMCID: PMC5918160. DOI: 10.1038/s41564-018-0138-2

Compositions and methods for inhibiting arginase activity

Sjogren, Eric B.; Li, Jim; Van Zandt, Michael; Whitehouse, Darren.
WO 2017075363 A1, 54 pp (2017)
https://patents.google.com/patent/US20160375044A1/en

Ring constrained analogs as arginase inhibitors

Van Zandt, Michael; Jagdmann, Jr., Gunnar Erik
WO 2013158262, 52 pp (2013)
https://patents.google.com/patent/WO2017191130A3/en

Crystal structure of Schistosoma mansoni arginase, a potential drug target for the treatment of schistosomiasis

Hai, Yang; Edwards, Jennifer E.; Van Zandt, Michael C.; Hoffmann, Karl F.; Christianson, David W.
Biochemistry (2014), 53(28), 4671-4684
PMCID: PMC4138072. DOI: 10.1021/bi5004519

Synthesis of quaternary α-amino acid-based arginase inhibitors via the Ugi reaction

Golebiowski, Adam; Whitehouse, Darren; Beckett, R. Paul; Van Zandt, Michael; Ji, Min Koo; Ryder, Todd R.; Jagdmann, Erik; Andreoli, Monica; Lee, Yung; Sheeler, Ryan; et al.
Bioorganic & Medicinal Chemistry Letters (2013), 23(17), 4837-4841
PMID: 23886684. DOI: 10.1016/j.bmcl.2013.06.092

Enantioselective synthesis of orthogonally protected (2R,3R)-(-)-epicatechin derivatives, key intermediates in the de novo chemical synthesis of (-)-epicatechin glucuronides and sulfates

Zhang, Mingbao; Jagdmann, G. Erik, Jr.; Van Zandt, Michael; Beckett, Paul; Schroeter, Hagen
Tetrahedron Asymmetry (2013), 24(7), 362-373
https://doi.org/10.1016/j.tetasy.2013.02.012

Discovery of (R)-2-Amino-6-borono-2-(2-(piperidin-1-yl)ethyl) hexanoic Acid and Congeners As Highly Potent Inhibitors of Human Arginases I and II for Treatment of Myocardial Reperfusion Injury

Van Zandt, Michael C.; Whitehouse, Darren L.; Golebiowski, Adam; Ji, Min Koo; Zhang, Mingbao; Beckett, R. Paul; Jagdmann, G. Erik; Ryder, Todd R.; Sheeler, Ryan; Andreoli, Monica; et al.
Journal of Medicinal Chemistry (2013), 56(6), 2568-2580
PMID: 23472952. DOI: 10.1021/jm400014c

2-Substituted-2-amino-6-boronohexanoic acids as arginase inhibitors

Golebiowski, Adam; Paul Beckett, R.; Van Zandt, Michael; Ji, Min Koo; Whitehouse, Darren; Ryder, Todd R.; Jagdmann, Erik; Andreoli, Monica; Mazur, Adam; Padmanilayam, Manyian; et al.
Bioorganic & Medicinal Chemistry Letters (2013), 23(7), 2027-2030
PMID: 23453840. DOI: 10.1016/j.bmcl.2013.02.024

Chemical Synthesis and Characterization of Epicatechin Glucuronides and Sulfates: Bioanalytical Standards for Epicatechin Metabolite Identification

Zhang, Mingbao; Jagdmann, G. Erik; Van Zandt, Michael; Sheeler, Ryan; Beckett, Paul; Schroeter, Hagen
Journal of Natural Products (2013), 762), 157-169
PMID: 23356946. DOI: 10.1021/np300568m

Discovery of [3-(4,5,7-trifluoro-benzothiazol-2-ylmethyl)-pyrrolo [2,3-b]pyridin-1-yl]acetic acids as highly potent and selective inhibitors of aldose reductase for treatment of chronic diabetic complications

Van Zandt, Michael C.; Doan, Brian; Sawicki, Diane R.; Sredy, Janet; Podjarny, Alberto D.
Bioorganic & Medicinal Chemistry Letters (2009), 19(7), 2006-2008
https://doi.org/10.1016/j.bmcl.2009.02.037

Discovery of 3-[(4,5,7-Trifluorobenzothiazol-2-yl)methyl]indole- N-acetic Acid (Lidorestat) and Congeners as Highly Potent and Selective Inhibitors of Aldose Reductase for Treatment of Chronic Diabetic Complications

Van Zandt, Michael C.; Jones, Michael L.; Gunn, David E.; Geraci, Leo S.; Jones, J. Howard; Sawicki, Diane R.; Sredy, Janet; Jacot, Jorge L.; DiCioccio, A. Thomas; Petrova, Tatiana; et al.
Journal of Medicinal Chemistry (2005), 48(9), 3141-3152
PMID: 15857120. DOI: 10.1021/jm0492094

Design and synthesis of highly potent and selective (2-arylcarbamoyl-phenoxy)-acetic acid inhibitors of aldose reductase for treatment of chronic diabetic complications

Van Zandt, Michael C.; Sibley, Evelyn O.; McCann, Erin E.; Combs, Kerry J.; Flam, Brenda; Sawicki, Diane R.; Sabetta, Al; Carrington, Anne; Sredy, Janet; Howard, Eduardo; et al.
Bioorganic & Medicinal Chemistry Letters (2004), 12(21), 5661-5675
PMID: 15465344. DOI: 10.1016/j.bmc.2004.07.062

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