Publications

(70) Xu, F., Sherry, B.D., Blizzard, T.A. “Discovery and Chemical Development of Relebactam: A Potent β-Lactamase Inhibitor in Combination with Primaxin® for the Treatment of Serious and Antibiotic-Resistant Bacterial Infections” in “Complete Accounts of Integrated Drug Discovery and Development: Recent Examples from the Pharmaceutical Industry Volume 3. ACS Symposium Series #1369” Pesti, J.A., Abdel-Magid, A.F., Vaidyanathan R. eds. American Chemical Society, Washington, DC, 2020, Chapter 8, 253-284.

(69) Young, K., Painter, R.E., Raghoobar, S.L., Hairston, N.N., Racine, F., Wisniewski, D., Balibar, C.J., Villafania, A., Zhang, R., Sahm, D. F., Blizzard, T., Murgolo, N., Hammond, M.L., Motyl, M.R. “In vitro studies evaluating the activity of imipenem in combination with relebactam against Pseudomonas aeruginosa BMC Microbiology, 2019, 19, 150

(68) Powles, M.A., Galgoci, A., Misura, A., Colwell, L., Dingley, K., Tang, W., Wu, J., Blizzard, T., Motyl, M., Young, K. “In vivo Efficacy of Relebactam (MK-7655) in Combination with Imipenem/Cilastatin in Murine Infection Models”  Antimicrobial Agents & Chemotherapy 2018, 62:eo2577-17

(67) Blizzard, T.A., Singh, S., Patil, B., Chidurala, N., Komanduri, V., Debnath, S., Belyakov, S., Crespo, A., Struck, A., Kurtz, M., Wiltsis, J., Shen, X., Sonatore, L., Arocho, M., Lewis, D., Ogletree, M., Biftu, T.  “Heterocyclic Core Analogs Of A Direct Thrombin Inhibitor.” Bioorg. Med. Chem. Lett. 2014, 24, 1111.

(66) Blizzard, T.A., Chen, H., Kim, S., Wu, J., Bodner, R., Gude, C., Imbriglio, J., Young, K., Park, Y., Ogawa, A., Raghoobar, S., Hairston, N., Painter, R.E., Wisniewski, D., Scapin, G., Fitzgerald, P., Sharma, N., Lu, J., Hermes, J., Hammond, M.  “Discovery of MK-7655, a Beta-Lactamase Inhibitor For Combination With Primaxin.” Bioorg. Med. Chem. Lett. 2014 24, 780.

(65) Chen, H., Blizzard, T.A., Kim, S., Wu, J., Young, K., Park, Y., Ogawa, A., Raghoobar, S., Painter, R.E., Wisniewski, D., Hairston, N., Fitzgerald, P., Sharma, N., Scapin, G., Lu, J., Hermes, J., Hammond, M.  “Side Chain SAR of Bicyclic beta-Lactamase Inhibitors (BLIs). 2.  N-Alkylated and Open Chain Analogs of MK-8712. “ Bioorg. Med. Chem. Lett. 2011, 21, 4267.

(64) Blizzard, T.A., Chen, H., Kim, S., Wu, J., Young, K., Park, Y., Ogawa, A., Raghoobar, S., Painter, R.E., Hairston, N., Lee, S.H., Misura, A., Felcetto, T., J., Ha, S., Hickey, E., Hermes, J., Hammond, M.  “Side Chain SAR Of Bicyclic Beta-Lactamase Inhibitors (BLIs). 1. Discovery Of A Class C BLI For Combination With Imipenem.”  Bioorg. Med. Chem. Lett. 2010, 20, 918.

(63) Blizzard, T.A.  “Selective Estrogen Receptor Modulator Medicinal Chemistry At Merck. A Review.”  Curr. Top. Med. Chem. 2008, 8, 792.

(62) Aloysius, H.A., Silva-Elipe, M.V., Arison, B.H., Faidley,  T.D.,  Michael,  B.F., Blizzard,  T.A., Thompson, D.R., Shoop, W.L., and Tschirret-Guth, R.A.  “Comparative Disposition And Metabolism Of Paraherquamide In Gerbils, Dogs And Sheep.”  Drug Metab. & Disp. 2008, 36, 1659.

(61) Blizzard, T.A., Gude, C., Morgan, J.D., Chan, W., Birzin, E.T., Mojena, M., Tudela, C., Chen, F., Knecht, K., Su, Q., Kraker, B., Mosley, R.T., Holmes, M.A., Rohrer, S.P., and Hammond, M.L.  “Androstene-3,5-diene Analogs As ER-beta Selective SERMs.”  Bioorg. Med. Chem. Lett. 2007, 17, 6295.

(60) Blizzard, T.A., Gude, C., Chan, W., Birzin, E.T., Mojena, M., Tudela, C., Chen, F., Knecht, K., Su, Q., Kraker, B., Holmes, M.A., Rohrer, S.P., and Hammond, M.L.  “Bridged Androstenediol Analogs As ER-beta Selective SERMs.”  Bioorg. Med. Chem. Lett. 2007, 17, 2944.

(59) Blizzard, T.A., Gude, C., Morgan, J.D., Chan, W., Birzin, E.T., Mojena, M., Tudela, C., Chen, F., Knecht, K., Su, Q., Kraker, B., Mosley, R.T., Holmes, M.A., Sharma, N., Fitzgerald, P.M.D., Rohrer, S.P., and Hammond, M.L.  “Androstenediol Analogs As Estrogen Receptor Beta Selective SERMs.” Bioorg. Med. Chem. Lett. 2006, 16, 834.

(58) Blizzard, T.A., Morgan, J.D., Chan, W., Birzin, E.T., Pai, L., Hayes, E.C., DaSilva, C.A., Mosley, R.T., Yang, Y.T., Rohrer, S.P., DiNinno, F., and Hammond, M.L.  “Estrogen Receptor Ligands: Part 14. Application Of Novel  Antagonist Side Chains To Existing Platforms.” Bioorg. Med. Chem. Lett. 2005, 15, 5124.

(57) Blizzard, T.A.  “Book Review:  Natural Products Synthesis II: Targets, Methods, Concepts. Topics In Current Chemistry, 244.”  J. Am. Chem. Soc. 2005, 127, 13080.

(56) Blizzard, T.A., DiNinno, F., Chen, H.Y., Kim, S., Wu, J.Y., Chan, W., Birzin, E.T., Yang, Y.T., Pai, L., Hayes, E.C., DaSilva, C.A., Rohrer, S.P., Schaeffer, J.M., and Hammond, M.L.  “Estrogen Receptor Ligands: Part 13. Dihydrobenzoxathiin SERAMs With An Optimized Antagonist Side Chain.”  Bioorg. Med. Chem. Lett. 2005, 15, 3912.

(55) Tan, Q., Blizzard, T.A., Morgan, J.D., Birzin, E.T., Chan, W., Yang, Y.T., Pai, L., Hayes, E.C., DaSilva, C.A., Mitra, S.W., Yudkovitz, J., Wilkinson, H.A., Sharma, N., Fitzgerald, P.M.D., Li, S., Colwell, L., Fisher, J.E., Adamski, S., Reszka, A.A., Kimmel, D., DiNinno, F.D., Rohrer, S.P., Freedman, L.P., Schaeffer, J.M., Hammond M.L. “Estrogen receptor ligands. Part 10: Chromanes: Old Scaffolds for New SERAMs.” Bioorg. Med. Chem. Lett. 2005, 15, 1675.

(54) Blizzard, T.A., DiNinno, F., Morgan, J.D., Chen, H.Y., Wu, J.Y., Kim, S., Chan, W., Birzin, E.T., Yang, Y.T., Pai, L., Fitzgerald, P.M.D., Sharma, N., Li, Y., Zhang, Z., Hayes, E.C., DaSilva, C.A., Tang, W., Rohrer, S.P., Schaeffer, J.M., and Hammond, M.L.  “Estrogen Receptor Ligands: Part 9. Dihydrobenzoxathiin SERAMs With Alkyl Substituted Pyrrolidine Side Chains And Linkers.”  Bioorg. Med. Chem. Lett. 2005, 15, 101.

(53) Blizzard, T.A., DiNinno, F., Morgan, J.D., Wu, J.Y., Chen, H.Y., Kim, S., Chan, W., Birzin, E.T., Yang, Y.T., Pai, L., Zhang, Z., Hayes, E.C., DaSilva, C.A., Tang, W., Rohrer, S.P., Schaeffer, J.M., and Hammond, M.L.  “Estrogen Receptor Ligands: Part 8. Dihydrobenzoxathiin SERAMs With Heteroatom Substituted Side Chains.”  Bioorg. Med. Chem. Lett. 2004, 14, 3865.

(52) Blizzard, T.A., DiNinno, F., Morgan, J.D., Chen, H.Y., Wu, J.Y., Gude, C., Kim, S., Chan, W., Birzin, E.T., Yang, Y.T., Pai, L., Zhang, Z., Hayes, E.C., DaSilva, C.A., Tang, W., Rohrer, S.P., Schaeffer, J.M., and Hammond, M.L.  “Estrogen Receptor Ligands. Part 7: Dihydrobenzoxathiin SERAMs With Bicyclic Amine Side Chains.”  Bioorg. Med. Chem. Lett. 2004, 14, 3861.

(51) Blizzard, T.A., Mosley, R.T., Birzin, E.T., Chan, W., and Hammond, M.L.  “Comparison Of 2-Phenylspiroindenes And 2-Phenylspiroindenediones As Estrogen Receptor Ligands – Modelling and Binding Data Don’t Agree!”  Bioorg. Med. Chem. Lett. 2004, 14, 1317.

(50) Peekhaus, N.T., Ferrer, M., Chang, T.,  Kornienko, O., Schneeweis, J.E., Smith, T.S., Hoffman, I., Mitnaul, L.J., Chin, J., Fischer, P.A., Blizzard, T.A., Birzin, E.T., Chan, W., Inglese, J., Strulovici, B., Rohrer, S.P., and Schaeffer, J.M.  “A beta-Lactamase Dependent Ga14-Estrogen Receptor betaTransactivation Assay for the Ultra High Throughput Screening of Estrogen Receptor beta Agonists in a 3,456-Well Format.” Assay & Drug Devel. Technol.  2003, 1, 789.

(49) Blizzard, T.A.  “Book Review:  Progress in the Chemistry of Organic Natural Products, 85.” J. Am. Chem. Soc. 2003, 125, 10145.

(48) Blizzard, T.A., Morgan, J.D., Mosley, R.T., Frisch, K., Birzin, E.T., Rohrer, S.P., and Hammond, M.L.  “2-Phenylspiroindenes: A Novel Class of Selective Estrogen Receptor Modulators (SERMs).”  Bioorg. Med. Chem. Lett. 2003, 13, 479.

(47) Chen, C., Ngui, J.S., Doss, G.A., Wang, R.W., Cai, X., DiNinno, F.P., Blizzard, T.A., Hammond, M.L., Stearns, R.A., Evans, D.C., Baillie, T.A., Tang, W.  “Cytochrome P450 3A4-Mediated Bioactivation of Raloxifene:  Irreversible Enzyme Inhibition and Thiol Adduct Formation.”  Chem. Res. Toxicol.  2002, 15, 907.

(46) Blizzard, T.A., Kim, R.M., Morgan, J.D., Chang, J., Kohler, J., Kilburn, R., Chapman, K., Hammond, M.L. “Antibacterial Activity Of G6-Quaternary Ammonium Derivatives Of A Lipophilic Vancomycin Analog.” Bioorg. Med. Chem. Lett. 2002, 12, 849.

(45) Blizzard, T.A. “2-Hydroxyethyl Phenyl Sulfone” in Encyclopedia of Reagents for Organic Synthesis On-line Edition, Wiley, Chichester, England  2001.

(44) Blizzard, T.A. “Titanium(IV) Fluoride” in Encyclopedia of Reagents for Organic Synthesis On-line Edition, Wiley, Chichester, England 2001.

(43) Blizzard, T.A. “Chemistry and Biology of Semi-synthetic Avermectins in The Biology-Chemistry Interface: A Tribute To Koji Nakanishi.” Marcel Dekker, New York, 1999, Chapter 9, 257.

(42) Ratcliffe, R.W., Wilkening, R.R., Wildonger, K.J., Waddell, S.T., Santorelli, G.M., Morgan, J.D., Blizzard, T.A., Hammond, M.L., Heck, J.V., Huber, J., Kohler, J., Dorso, K.L., St. Rose, E., Sundelof, J.G., May, W.J., and Hammond, G.G. “Synthesis and Properties of 2-(Naphthosultamyl)methyl-Carbapenems With Potent Anti-MRSA Activity:  Discovery of L-786,392.”  Bioorg. Med. Chem. Lett. 1999, 9, 679.

(41) Wilkening, R.R., Ratcliffe, R.W., Wildonger, K.J., Cama, L.D., Dykstra, K.D., DiNinno, F,P., Blizzard, T.A., Hammond, M.L., Heck, J.V., Dorso, K.L., St. Rose, E., Kohler, J., and Hammond, G.G.  “Synthesis and Activity of 2-(Sulfonamido)methyl-Carbapenems:  Discovery of a Novel, Anti-MRSA 1,8-Napthosultam Pharmacophore.”  Bioorg. Med. Chem. Lett. 1999, 9, 673.

(40) Rosen, H., Hajdu, R., Silver, L., Kropp, H., Dorso, K., Kohler, J., Sundelof, J.G., Huber, J., Hammond, G.G., Jackson, J.J., Gill, C., Thompson, R., Pelak, B.A., Epstein-Toney, J.H., Lankas, G., Wilkening, R.R., Wildonger, K.J., Blizzard, T.A., DiNinno, F.P., Ratcliffe, R.W., Heck, J.V., Kozarich, J.W., and Hammond, M.L. “Reduced Immunotoxicity And Preservation Of Antibacterial Activity In A Releasable Side Chain Carbapenem Antibiotic”  Science  1999, 283, 703.

(39) Meinke, P.T., Shoop, W.L., Michael, B.F., Blizzard, T.A., Dawson, G.R., Fisher, M.H., and Mrozik, H.  “Synthesis of gem-Difluoro-Avermectin Derivatives: Potent Anthelmintic and Anticonvulsant Agents.”  Bioorg. Med. Chem. Lett1998, 8, 3643.

(38) Waddell, S.T., Santorelli, G.M., Blizzard, T.A., Graham, A., and Occi, J.  “Synthesis and Antibacterial Activity of O-Methyl Derivatives of Azalide Antibiotics:  II.  6-OMe Derivatives Via Clarithromycin.” Bioorg. Med. Chem. Lett. 1998, 8, 1321.

(37) Waddell, S.T., Santorelli, G.M., Blizzard, T.A., Graham, A., and Occi, J.  “Synthesis and Antibacterial Activity of O-Methyl Derivatives of Azalide Antibiotics:  I.  4″, 11, and 12-OMe Derivatives Via Direct Methylation.”  Bioorg. Med. Chem. Lett.  1998, 8, 549.

(36) Waddell, S. T., Eckert, J.M., and Blizzard, T. A.  “Chimeric Azalides with Functionalized Western Portions.”  Heterocycles  1996, 43, 2325.

(35) Blizzard, T.A. “2-(Trimethylsilyl)ethyl Chloroformate” in Encyclopedia of Reagents for Organic Synthesis,  Wiley, Chichester, England 1995, Vol. 7, 5262.

(34) Blizzard, T.A. “2-(Trimethylsilyl)ethoxy Carbonyl Imidazole” in Encyclopedia of Reagents for Organic Synthesis,  Wiley, Chichester, England 1995, Vol. 7, 5259.

(33) Blizzard, T.A.  “Dichloroalane” in Encyclopedia of Reagents for Organic Synthesis.  Wiley, Chichester, England 1995, Vol. 3, 1655.

(32) Blizzard, T.A.  “Dibromoalane” in Encyclopedia of Reagents for Organic Synthesis.  Wiley, Chichester, England 1995, Vol. 3, 1545.

(31) Mrozik, H., Eskola, P., Arison, B., Linn, B., Lusi, A., Matzuk, A., Shih, T., Tischler, M., Waksmunski, F., Wyvratt, M., Blizzard, T., Margiatto, G., Fisher, M., Shoop, W., and Egerton, J.  “4”-Deoxy-4”-Aminoavermectins With Potent Broad Spectrum Antiparasitic Activities.”  Bioorg. Med. Chem. Lett. 1995, 5, 2435.

(30) Waddell, S., Ratcliffe, R., Szumiloski, S., Wildonger, K., Wilkening, R., Blizzard, T., Huber, J., Kohler, J., Dorso, K., St. Rose, E., Sundelof, J., and  Hammond. G. “Benzothiazolylthio Carbapenems:  Potent Anti-MRSA Agents.” Bioorg. Med. Chem. Lett1995, 5, 1427.

(29) Blizzard, T.A.  “Recent Progress in the Synthesis of Avermectins and Milbemycins.  A Review.” Org. Prep. & Proc. Int. 1994, 26, 617.

(28) Shankaran, K., Wilkening, R.R., Blizzard, T.A., Ratcliffe, R.W., Heck, J.V., Graham, A.C., and Herbert, C.M.  “Preparation and Activities of 4″-epi and 4″-Amino Analogs Derived from 9-deoxo-8a-aza-8a-homoerythromycin A.”  Bioorg. Med. Chem. Lett., 1994, 4, 1111.

(27) Blizzard, T.A., Mrozik, H., and Fisher, M.H.  “Avermectin B1-8,9-oxide:  Stereochemistry, Reactivity, and Bioactivity.”  Bioorg. Med. Chem. Lett., 1993, 3, 2093.

(26) Waddell, S.T. and Blizzard, T.A.  “Semisynthesis of Linear Fragments Corresponding to the Eastern Portion of Azalide Antibiotics.”  Bioorg. Med. Chem. Lett.,  1993, 3, 1757.

(25)  Waddell, S.T. and Blizzard, T.A.  “Chimeric Azalides with Simplified Western Portions.”  Tet. Lett.,  1993, 34, 5385.

(24) Blizzard, T.A., Margiatto, G.M., Mrozik, H., and Fisher, M.H.  “A Novel Fragmentation Reaction of Avermectin Aglycones.”  J. Org. Chem. 1993, 58, 3201.

(23) Waddell, S.T. and Blizzard, T.A.  “Novel Reactions of Carbohydrate Dithianes:  1,4-dithiepins via an Intramolecular 1,4-alkoxy Relay.”   Heterocycles 1993, 36, 1213.

(22) Waddell, S.T. and Blizzard, T.A. “Base Catalyzed Ring Opening Reactions of Erythromycin A.”  Tet. Lett., 1992, 33, 7827.

(21) Shankaran, K., and Blizzard, T.A. “Synthesis and Activities of 9-Pyrrolo-9-Deoxo-Erythromycin Analogs.”  Bioorg. Med. Chem. Lett., 1992, 2, 1555.

(20) Blizzard, T.A., Margiatto, G.M., Mrozik, H., Shoop, W.L., Frankshun, R.A., and Fisher, M.H.  “Synthesis and Biological Activity of 13-epi-Avermectins:  Potent Anthelmintic Agents With An Increased Margin of Safety.”  J. Med. Chem., 1992, 35, 3873.

(19) Schaeffer, J.M., Blizzard, T.A., Ondeyka, J., Goegelman, R., Sinclair, P.J., and Mrozik, H.  “[3H] Paraherquamide Binding to Caenorhabditis Elegans:  Studies on a Potent New Anthelmintic Agent.”  Biochem. Pharmacol., 1992, 43, 679.

(18) Blizzard, T., Margiatto, G., Linn, B., Mrozik, H., and Fisher, M. “Avermectin Analogs With a Spacer Between the Aglycone and the Disaccharide.”  Bioorg. Med. Chem. Lett., 1991, 1, 369.

(17) Blizzard, T., Bostrom, L., Margiatto, G., Mrozik, H., and Fisher, M.  “Conversion of Avermectin B1 to 19-epi-Avermectin B1.” Tet. Lett., 1991, 32, 2723.

(16) Blizzard, T.A., Margiatto, G., Mrozik, H., Schaeffer, J.M., and Fisher, M.H.  “Chemical Modification of Paraherquamide.  4.  1-N-Substituted Analogs.”  Tet. Lett., 1991, 32, 2441.

(15) Blizzard, T.A., Margiatto, G., Mrozik, H., Schaeffer, J.M., and Fisher, M.H.  “Chemical Modification of Paraherquamide.  3.  Vinyl Ether Modified Analogs.”  Tet. Lett., 1991, 32, 2437.

(14) Blizzard, T.A., Mrozik, H., Preiser, F.A., and Fisher, M.H.  “Synthesis, Reactivity, and Bioactivity of Avermectin B1-3,4-oxide.” Tet. Lett., 1990, 31, 4965.

(13) Blizzard, T.A., Fisher, M.H., Mrozik, H., and Shih, T.L. “Avermectins and Milbemycins. Recent Progress in the Chemical Synthesis of Antibiotics.”   Springer Verlag, Berlin, 1990, Ch. 3, 65.

(12) Blizzard, T.A., Mrozik, H., Fisher, M.H., and Schaeffer, J.M.  “Chemical Modification of Paraherquamide.  2.  Replacement of the C-14 Methyl Group.”  J. Org. Chem., 1990, 55, 2256.

(11) Blizzard, T.A., Rosegay, A., Mrozik, H., and Fisher, M.H.  “Preparation of Paraherquamide Labelled With Deuterium or Tritium.”  J. Labelled Compounds and Radiopharm., 1990, 28, 461.

(10) Gargiulo, D., Blizzard, T.A., and Nakanishi , K.  “Synthesis of Mosesin-4, A Naturally Occurring Steroid Saponin With Shark Repellent Activity, and its Analog 7-beta-Galactosyl Ethyl Cholate.”  Tetrahedron, 1989, 45, 5423.

(9) Blizzard, T.A., Ruby, C.L., Mrozik, H., and Fisher, M.H.  “Brine Shrimp (Artemia salina) as a Convenient Bio-assay for Avermectin Analogs.”  J. Antibiot., 1989, 42, 1304.

(8) Blizzard, T.A., Marino, G., Mrozik, H., Fisher, M.H., Hoogsteen, K, and Springer, J.P. “Chemical Modification of Paraherquamide.  1.  Unusual Reactions and Absolute Stereochemistry.”  J. Org. Chem., 1989, 54, 2657.

(7) Blizzard, T.A., Marino, G., Mrozik, H., and Fisher, M.H.  “An Improved Preparation of the Avermectin Disaccharide Unit.”  J. Org. Chem., 1989, 54, 1756.

(6) Blizzard, T.A., Mrozik, H., and Fisher, M.H.  “Chemical Degradation of Avermectin B1.”  Tet. Lett., 1988, 29, 3163.

(5) Javitt, N.B., Kok, E., Carubbi, F., Blizzard, T.A., Gut, M., and Byon, C.Y. “Bile Acid Synthesis:  Metabolism of 3-beta-Hydroxy-5-Cholenoic Acid to Chenodeoxycholic Acid.”  J. Biol. Chem., 1986, 261, 12486.

(4) Roush, W.R., and Blizzard, T.A.  “Synthesis of Verrucarin B.”  J. Org. Chem., 1984, 49, 4332.

(3) Roush, W.R. and Blizzard, T.A.  “Synthesis of Epoxytrichothecenes:  Verrucarin J and Verrucarin J Isomers.”  J. Org. Chem., 1984, 49, 1772.

(2) Roush, W.R. and Blizzard, T.A. “Synthesis of Verrucarin J.”  J. Org. Chem., 1983, 48, 758.

(1) Roush, W.R., Blizzard, T.A., and Basha, F.Z.  “Methodology for the Synthesis of the Acyclic Portions of Verrucarins A and J.”  Tet. Lett., 1982, 23, 2331.