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Marcelo Nieto, Ph.D.
Associate Professor of Pharmaceutical Sciences
(618) 650‑5130
Fax: (618) 650‑5145

Medicinal Chemistry
B.S., Chemistry (Organic Chemistry), 1992, National University of Córdoba, Córdoba, Argentina, 1992.
Ph.D., Chemistry, 1999, National University of Córdoba, Córdoba, Argentina
Postdoctoral, 2000-2002, The University of Mississippi

Research: Medicinal Chemistry & Natural Products

My research interests are focused in two main areas:

  1. Rational combinatorial libraries design
  2. Natural products-based drug discovery

Both of these are geared toward the discovery of novel anti-infective agents with unique mechanism of action.

My lab has successfully worked on the development of a focused library of N-benzenesulfonyl-heterocycles that include more than 200 members. From this library, we have found one lead compound as antibacterial, more specifically a compound with a moderate activity against E. coli. In addition, we have identified four compounds with antiparasitic activity. The results were useful in the study of structure activity relationships and refining of the lead compounds.

In the natural product area, we have successfully completed the bioassay-guided isolation and characterization of one anti-Staphylococcus aureus compound from the plant Verbesina negrensis. Our plans include the study of plants from the Venezuelan Andean region that have been traditionally used as gastroprotective. The goal of this research is to identify and isolate natural products that are active against Helicobacter pylori, a Gram-negative bacterium that causes gastritis that leads to gastric ulcer and stomach cancer.

Selected Publications

F. Mora, L. Alpan, N. de Tommasi, V. McCracken, M. Nieto. “Bioactivity-guided isolation of a new antibacterial germacrene from Verbesina negrensis”. Submitted to J. Ethnopharmacol. (July 2012)

F. Mora, L. Alpan, V. McCracken, M. Nieto. “Chemical and Biological Aspects of the genus Verbesina”. Submitted to Nat. Prod. J. (April 2012).

M. Nieto, A. Pierini, N. Singh, C. McCurdy, R. Manzo, M. R. Mazzieri. "A Theoretical Study of Antibacterial Benzenesulfonamides Fluoroquinolones (BSFQ)" Med. Chem. (2012) 8 (3), 349-360.

R. Pagliero, R. Mercado, V. McCracken, M. Mazzieri, M. Nieto. Rapid and Simple Synthesis of N-Benzenesulfonyl derivatives of heterocycles and their Antimicrobial Properties. Lett. Drug Des. Discov.. (2011) 8(9), 778-791. Selected as “Editors choice” for this issue.

L. Hergert, M. Nieto, M. Becerra, I. Albesa, M. Mazzieri. “Synthesis of N-Benzenesulfonylbenzotriazole Derivatives and Evaluation of their Antimicrobial Activity”. Lett. Drug Des. Discov.. (2008) 5(5), 313-318.

B. Kane, M. Nieto, C. McCurdy, D. Ferguson. “A unique binding epitope for salvinorin A, a non-nitrogenous kappa-opioid receptor agonist”. FEBS J. (2006) 273, 1966-74.

M. Nieto, F. Alovero, R. Manzo, M. Mazzieri. Benzenecarboxamide Analogues of Fluoroquinolones (BCFQs). Antibacterial Activity and SAR Studies. Lett. Drug Design and Discovery (2006) 3(2), 108-111.

C. McCurdy, K. Sufka, J. Warnick, M. Nieto. Analgesic Profile of Salvinorin A, a Structurally Unique Kappa Opioid Agonist. Pharmacol, Biochem and Behavior, (2006) 83, 109-113.

M. Nieto, F. Alovero, R. Manzo, M. Mazzieri. "A New Class Of Fluoroquinolone: Benzenesulfonamideflu-oroquinolones (BSFQs). Antibacterial Activity And SAR Studies. II" EurJMedChem (2005) 40(4), 361-369.

M. Nieto, A. Phillip, J. Poupaert, C. McCurdy. “Solution-Phase Parallel Synthesis of Spirohydantoins Derivatives” J. Comb. Chem. (2005) 7(2), 258-263.

C. McCurdy, M. Nieto, B. Kane, D. Ferguson. Non-nitrogenous kappa opioid receptor ligands based on salvinorin A, a unique and naturally occurring opiate lead. Fundamental and Clinical Pharmacology, 2004, 18, 597. DOI: 10.1111/j.1472-8206.2004.00288.xC.

C. McCurdy, K. Sufka, J. Warnick, M. Nieto. “Salvinorin A, a kappa opioid receptor agonist, is a fast acting, potent analgesic”. The AAPS Journal-Drug Addiction-From Basic Research to Therapies Volume 6 (AAPS-NIDA Symposium Frontiers in Science, September 2004)

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