Peer-Reviewed Publications

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2021

Pyrazole‐Thiazole core‐containing analogs exhibit adjunctive activity with meropenem against carbapenem‐resistant enterobacteriaceae (CRE).

Kim, C.; Kassu, M.; Smith, K. P.; Kirby, J. E.; Manetsch, R. ChemMedChem 2021.

Aminoalkoxycarbonyloxymethyl ether prodrugs with a ph-triggered release mechanism: a case study improving the solubility, bioavailability, and efficacy of antimalarial 4(1H)-quinolones with single dose cures.

Monastyrskyi, A.; Brockmeyer, F.; LaCrue, A. N.; Zhao, Y.; Maher, S. P.; Maignan, J. R.; Padin-Irizarry, V.; Sakhno, Y. I.; Parvatkar, P. T.; Asakawa, A. H.; Huang, L.; Casandra, D.; Mashkouri, S.; Kyle, D. E.; Manetsch, R. J. Med. Chem. 2021.

A comprehensive review of 4(1H)-quinolones and 4(1H)-pyridones for the development of an effective antimalarial.

Asakawa, A. H.; Manetsch, R. In Plasmodium Species and Drug Resistance [Working Title]; IntechOpen, 2021; Vol. 4, pp 1–30.

Synthesis of mono- and bisperoxide-bridged artemisinin dimers to elucidate the contribution of dimerization to antimalarial activity.

Lichorowic, C. L.; Zhao, Y.; Maher, S. P.; Padín-Irizarry, V.; Mendiola, V. C.; de Castro, S. T.; Worden, J. A.; Casandra, D.; Kyle, D. E.; Manetsch, R. ACS Infect. Dis. 2021.

Naegleria fowleri: protein structures to facilitate drug discovery for the deadly, pathogenic free-living amoeba. 

Tillery, L.; Barrett, K.; Goldstein, J.; Lassner, J. W.; Osterhout, B.; Tran, N. L.; Xu, L.; Young, R. M.; Craig, J.; Chun, I.; Dranow, D. M.; Abendroth, J.; Delker, S. L.; Davies, D. R.; Mayclin, S. J.; Calhoun, B.; Bolejack, M. J.; Staker, B.; Subramanian, S.; Phan, I.; Lorimer, D, D.; Peter, J. M.; Edwards, T. E.; Kyle, D. E.; Rice, C. A.; Morris, J. C.; Leahy, J. W.; Manetsch, R.; Barrett, L. K.; Smith, C. L.; Van Voorhis, W. C. PLoS One 2021, 16 (3 March), 1–19.

Cyclic thiosulfinates as a novel class of disulfide cleavable cross-linkers for rapid hydrogel synthesis.

Aluri, K. C.; Hossain, M. A.; Kanetkar, N.; Miller, B. C.; Dowgiallo, M. G.; Sivasankar, D.; Sullivan, M. R.; Manetsch, R.; Konry, T.; Ekenseair, A.; Agar, J. N. Bioconjug. Chem. 2021, 32 (3), 584–594.

Photoaffinity labeled unnatural amino acid crosslinking stabilizes a trans-signaling conformation between the d2-5ht2a receptor heteromer. 

Winn, B. T.; Kim, C.; Cui, M.; Manetsch, R.; Logothetis, D. E. Biophys. J. 2021, 120 (3), 327a.

2020

Unnatural amino acid receptor incorporation as a novel photoaffinity tool for gpcr heteromer signaling studies.

Winn, B. T.; Kim, C.; Cui, M.; Manetsch, R.; Logothetis, D. E. Biophys. J. 2020, 118 (3), 95a-96a.

New strategies and structural considerations in development of therapeutics for carbapenem-resistant enterobacteriaceae.

Brennan-Krohn, T.; Manetsch, R.; O’Doherty, G. A.; Kirby, J. E. Transl. Res. 2020, 220, 14–32.

2019

A Whole-Cell Screen for Adjunctive and Direct Antimicrobials Active Against Carbapenem-Resistant Enterobacteriaceae. 

Smith; K P; Dowgiallo, M D; Chiaraviglio, L; Parvatkar, P; Kim, C; Manetsch, R; Kirby, J E. SLAS Discov. 2019, 24 (8), 842-853.

2018

Metal-Free Cross-Dehydrogenative Coupling (CDC): Molecular Iodine as a Versatile Catalyst/Reagent for CDC Reactions.

Parvatkar, P. T.; Manetsch, R.; Banik, B. K. Chem. - An Asian J. 2018, No. Cdc, 1–26.

Cyclic Thiosulfinates and Cyclic Disulfides Selectively Cross-Link Thiols While Avoiding Modification of Lone Thiols.

Donnelly, D. P.; Dowgiallo, M. G.; Salisbury, J. P.; Aluri, K. C.; Iyengar, S.; Chaudhari, M.; Mathew, M.; Miele, I.; Auclair, J. R.; Lopez, S. A.; Manetsch, R.; Agar, J. N. J. Am. Chem. Soc. 2018, 140 (24), 7377–7380.

Design and Synthesis of Orally Bioavailable Piperazine Substituted 4(1H)-Quinolones with Potent Antimalarial Activity: Structure-Activity and Structure-Property Relationship Studies.

Neelarapu, R.; Maignan, J. R.; Lichorowic, C. L.; Monastyrskyi, A.; Mutka, T. S.; LaCrue, A. N.; Blake, L. D.; Casandra, D.; Mashkouri, S.; Burrows, J. N.; Willis, P. A.; Kyle, D. E.; Manetsch, R. J. Med. Chem. 2018, 61 (4), 1450–1473.

2017

Synthesis, characterization, and cellular localization of a fluorescent probe of the antimalarial 8-aminoquinoline primaquine.

McQueen, A.; Blake, L. D.; Azhari, A.; Kemp, M. T.; McGaha, T. W.; Namelikonda, N.; Larsen, R. W.; Manetsch, R.; Kyle, D. E. Bioorg. Med. Chem. Lett. 2017, 27 (20), 4597–4600.

Menoctone Resistance in Malaria Parasites Is Conferred by M133I Mutations in Cytochrome b That Are Transmissible through Mosquitoes.

Blake, L. D.; Johnson, M. E.; Siegel, S. V.; McQueen, A.; Iyamu, I. D.; Shaikh, A. K.; Shultis, M. W.; Manetsch, R.; Kyle, D. E. Antimicrob. Agents Chemother. 2017, 61 (8), 1–13.

Progress in the Optimization of 4(1H)-Quinolone Derivatives as Antimalarials Targeting the Erythrocytic, the Exoerythrocytic and the Transmitting Stages of the Malaria Parasite.

Brockmeyer, F.; Manetsch, R. Chim. Int. J. Chem. 2017, 71 (4), 213–219.

Characterizing the Antimicrobial Activity of N2,N4-Disubstituted Quinazoline-2,4-Diamines toward Multidrug-Resistant Acinetobacter baumannii.

Fleeman, R.; Van Horn, K. S.; Barber, M. M.; Burda, W. N.; Flanigan, D. L.; Manetsch, R.; Shaw, L. N. Antimicrob. Agents Chemother. 2017, 61 (6), 1–11.

2016

ICI 56,780 Optimization: Structure-Activity Relationship Studies of 7-(2-Phenoxyethoxy)-4(1H)-quinolones with Antimalarial Activity.

Maignan, J. R.; Lichorowic, C. L.; Giarrusso, J.; Blake, L. D.; Casandra, D.; Mutka, T. S.; LaCrue, A. N.; Burrows, J. N.; Willis, P. A.; Kyle, D. E.; Manetsch, R. J. Med. Chem. 2016, 59 (14), 6943–6960.

Spirocyclic chromanes exhibit antiplasmodial activities and inhibit all intraerythrocytic life cycle stages

Roberts, B. F.; Iyamu, I. D.; Lee, S.; Lee, E.; Ayong, L.; Kyle, D. E.; Yuan, Y.; Manetsch, R.; Chakrabarti, D. Int. J. Parasitol. Drugs Drug Resist. 2016, 6, 85–92.

3-Trifluoromethyl-3-aryldiazirine photolabels with enhanced ambient light stability 

Kumar, A. B.; Tipton, J. D.; Manetsch, R.  Chem. Commun. 2016, 52, 2729-2732.

2015

SAR refinement of antileishmanial N2,N4-disubstituted quinazoline-2,4-diamines

Zhu, X.; Van Horn, K. S.; Barber, M. M.; Yang, S.; Wang, M. Z.; Manetsch, R.; Werbovetz, K. A. Bioorg. Med. Chem. 2015, 23, 5182–5189.

Metal-Free Arylation of Ethyl Acetoacetate with Hypervalent Diaryliodonium Salts: An Immediate Access to Diverse 3-Aryl-4(1   H )-Quinolones

Monastyrskyi, A.; Namelikonda, N. K.; Manetsch, R.  J. Org. Chem. 2015, 4, 2513–2520.

Synthesis and Evaluation of a Novel Adenosine-Ribose Probe for Global-Scale Profiling of Nucleoside and Nucleotide-Binding Proteins

Mahajan, S.; Manetsch, R.; Merkler, D. J.; Stevens Jr., S. M.  PLoS One 2015, 10, 1–17.

2014

Orally bioavailable 6-chloro-7-methoxy-4(1H)-quinolones efficacious against multiple stages of Plasmodium

Cross, R. M.; Flanigan, D. L.; Monastyrskyi, A.; LaCrue, A. N.; Sáenz, F. E.; Maignan, J. R.; Mutka, T. S.; White, K. L.; Shackleford, D. M.; Bathurst, I.; et al.  J. Med. Chem. 2014, 57, 8860–8879.

4(1H)-Pyridone and 4(1H)-Quinolone Derivatives as Antimalarials with Erythrocytic, Exoerythrocytic, and Transmission Blocking Activities (Review)

Monastyrskyi, A.; Kyle, D. E.; Manetsch, R. Curr Top Med Chem, 2014; 1693-1705.

In silico characterization of an atypical MAPK phosphatase of Plasmodium falciparum as a suitable target for drug discovery

Campbell, C. O.; Santiago, D. N.; Guida, W. C.; Manetsch, R.; Adams, J. H.  Chem. Biol. Drug Des. 2014, 84, 158–168.

Regioselective O 2′, O 3′-Deacetylations of Peracetylated Ribonucleosides by Using Tetra- n -butylammonium Fluoride

Kumar, A. B.; Manetsch, R.  European J. Org. Chem. 2014, 3551–3555.

Antibacterial activity of a series of N2,N4-disubstituted quinazoline-2,4-diamines

Van Horn, K. S.; Burda, W. N.; Fleeman, R.; Shaw, L. N.; Manetsch, R.  J. Med. Chem. 2014, 57, 3075–3093.

Antileishmanial activity of a series of N2,N4-disubstituted quinazoline-2,4-diamines

Van Horn, K. S.; Zhu, X.; Pandharkar, T.; Yang, S.; Vesely, B.; Vanaerschot, M.; Dujardin, J.-C.; Rijal, S.; Kyle, D. E.; Wang, M. Z.; et al.  J. Med. Chem. 2014, 57, 5141–5156.

2013

4-(1H)-Quinolones and 1,2,3,4-Tetrahydroacridin-9(10H)-ones prevent the transmission of Plasmodium falciparum to Anopheles freeborni

Sáenz, F. E.; Lacrue, A. N.; Cross, R. M.; Maignan, J. R.; Udenze, K. O.; Manetsch, R.; Kyle, D. E.  Antimicrob. Agents Chemother. 2013, 57, 6187–6195.

Quinolone-3-diarylethers: A new class of drugs for a new era of malaria eradication

Nilsen, A.; LaCrue, A.; White, K. L.; Forquer, I. P.; Cross, R. M.; Marfurt, J.; Mather, M. W.; Delves, M. J.; Shackleford, D. M.; Saenz, F. E.; Morrisey, J. M.; Steuten, J.; Mutka, T.; Li, Y.; Wirjanata, G.; Ryan, E.; Duffy, S.; Kelly, J. X.; Sebayang, B. F.; Zeeman, A-M.; Noviyanti, R.; Sinden, R. E.; Kocken, C. H. M.; Price, R. N.; Avery, V. M.; Angulo-Barturen, I.; Jiménez-Díaz, M. B.; Ferrer, S.; Herreros, E.; Sanz, L. M.; Benito, F. J. G.; Bathurst, I.; Burrows, J.; Siegl, P.; Guy, R. K.; Winter, R. W.; Vaidya, A. B.; Charman, S. A.; Kyle, D. E.; Manetsch, R.; Riscoe, M. K.  Sci Transl Med, 2013, 5, 177.

A simple base-mediated amidation of aldehydes with azides

Kulkarni, S. S.; Hu, X.; Manetsch, R.  Chem. Commun. (Camb). 2013, 49, 1193–1195.

4(1H)-Quinolones with liver stage activity against Plasmodium berghei

Lacrue, A. N.; Sáenz, F. E.; Cross, R. M.; Udenze, K. O.; Monastyrskyi, A.; Stein, S.; Mutka, T. S.; Manetsch, R.; Kyle, D. E.  Antimicrob. Agents Chemother. 2013, 57, 417–424.

2012

Fluorescent properties and resonance energy transfer of 3,4-bis(2,4-difluorophenyl)-maleimide

Nacheva, K. P.; Maza, W. a; Myers, D. Z.; Fronczek, F. R.; Larsen, R. W.; Manetsch, R.  Org. Biomol. Chem. 2012, 10, 7840–7846.

Synthesis and structure-activity relationship studies of 1,3-disubstituted 2-propanols as BACE-1 inhibitors

Kumar, A. B.; Anderson, J. M.; Melendez, A. L.; Manetsch, R.  Bioorg. Med. Chem. Lett. 2012, 22, 4740–4744.

Sulfo-click reaction via in situ generated thioacids and its application in kinetic target-guided synthesis

Namelikonda, N. K.; Manetsch, R.  Chem. Commun. (Camb). 2012, 48, 1526–1528.

2011

Synthesis, antimalarial activity, and structure-activity relationship of 7-(2-phenoxyethoxy)-4(1H)-quinolones

Cross, R. M.; Namelikonda, N. K.; Mutka, T. S.; Luong, L.; Kyle, D. E.; Manetsch, R.; Monastyrskyi, A.; Burrows, J. N.  J. Med. Chem. 2011, 54, 8321–8327.

Design, synthesis and photoactivation studies of fluorous photolabels

Kumar, A. B.; Anderson, J. M.; Manetsch, R.  Org. Biomol. Chem. 2011, 9, 6284–6292.

Screening of protein-protein interaction modulators via sulfo-click kinetic target-guided synthesis

Kulkarni, S. S.; Hu, X.; Doi, K.; Wang, H.-G.; Manetsch, R.  ACS Chem. Biol. 2011, 6, 724–732.

Optimization of 1,2,3,4-tetrahydroacridin-9(10H)-ones as antimalarials utilizing structure-activity and structure-property relationships

Cross, R. M.; Maignan, J. R.; Mutka, T. S.; Luong, L.; Sargent, J.; Kyle, D. E.; Manetsch, R.  J. Med. Chem. 2011, 54, 4399–4426 

2010

Divergent route to access structurally diverse 4-quinolones via mono or sequential cross-couplings

Cross, R. M.; Manetsch, R.  J. Org. Chem. 2010, 75, 8654–8657.

Endochin optimization: structure-activity and structure-property relationship studies of 3-substituted 2-methyl-4(1H)-quinolones with antimalarial activity

Cross, R. M.; Monastyrskyi, A.; Mutka, T. S.; Burrows, J. N.; Kyle, D. E.; Manetsch, R.  J. Med. Chem. 2010, 53, 7076–7094.

Kinetic target-guided synthesis

Hu, X.; Manetsch, R.  Chem. Soc. Rev. 2010, 39, 1316–1324.

2008

Probing gorge dimensions of cholinesterases by freeze-frame click chemistry

Radić, Z.; Manetsch, R.; Fournier, D.; Sharpless, K. B.; Taylor, P. Chem. Biol. Interact. 2008, 175, 161–165.

Bcl-XL-templated assembly of its own protein-protein interaction modulator from fragments decorated with thio acids and sulfonyl azides

Hu, X.; Sun, J.; Wang, H.; Manetsch, R.  J. Am. Chem. Soc. 2008, 130, 13820–13821.

2006

In situ click chemistry: A powerful means for lead discovery (Review)

Sharpless, B.; Manetsch, R.  Expert Opinion on Drug Discovery 2006; 1: 525-538.

2005

Molecular basis of interactions of cholinesterases with tight binding inhibitors

Radić, Z.; Manetsch, R.; Krasiński, A.; Raushel, J.; Yamauchi, J.; Garcia, C.; Kolb, H.; Sharpless, K. B.; Taylor, P.  Chem. Biol. Interact. 2005, 157-158, 133–141.

Mechanistic study of proton transfer and hysteresis in catalytic antibody 16E7 by site-directed mutagenesis and homology modeling

Zheng, L.; Manetsch, R.; Woggon, W.-D.; Baumann, U.; Reymond, J.-L.  Bioorg. Med. Chem. 2005, 13, 1021–1029.

In situ selection of lead compounds by click chemistry: target-guided optimization of acetylcholinesterase inhibitors

Krasiński, A.; Radić, Z.; Manetsch, R.; Raushel, J.; Taylor, P.; Sharpless, K. B.; Kolb, H. C.  J. Am. Chem. Soc. 2005, 127, 6686–6692.

2004

A catalytic antibody against a tocopherol cyclase inhibitor

Manetsch, R.; Zheng, L.; Reymond, M. T.; Woggon, W.-D.; Reymond, J.-L. Chemistry 2004, 10, 2487–2506.

In situ click chemistry: enzyme inhibitors made to their own  specifications

Manetsch, R.; Krasiński, A.; Radić, Z.; Raushel, J.; Taylor, P.; Sharpless, K. B.; Kolb, H. C. J. Am. Chem. Soc. 2004, 126, 12809–12818 .