Nefzi’s Medicinal Chemistry lab is part of the Drug Discovery and Drug Delivery Nucleus, collaborative labs that provide access to a combination of enabling technologies, services and equipment, expertise, and hands-on training by key senior researcher staff to help scientists engage in research at the interface of chemistry and human biology. Our small molecule, peptide, and peptidomimetic libraries are ready-to-use chemical libraries used for drug discovery, lab drug screening, drug target identification, and other pharmaceutical-related applications. They are available for high-throughput screening (HTS) and high-content screening (HCS).
Compounds identified from the screening of the CTS-FIU collection have several key advantages when considering optimization. First, the data generated upon the identification of hits inherently contains a significant amount of SAR around a core scaffold. This can be utilized to identify critical features for the activity and/or selectivity of ligands. Secondly, all the compounds in the CTS-FIU collection contain multiple sites for functionality modification. Early work from our laboratory has shown the utility of mixture-based chemical libraries for the de novo identification of highly active antimicrobial compounds, antimalarial, potent analgesic, antifibrotic compounds, and novel antitumor agents.

• Active research areas in Nefzi’s group include:
• Discovery of novel small molecule inhibitors of type I collagen as potential therapeutics for fibrosis
• Discovery and Development of Novel Antimalarial Drugs
• Developing peripherally restricted small molecule heterocyclic peptidomimetics as safer analgesics
• Identification of small molecule compounds as novel Alzheimer’s therapeutics
•  Hit to lead optimization for the discovery of new chemical probes LMTK3 inhibitors for the treatment of breast cancer
• Discovery of small molecules to treat lung injury.

The MedChem Lab has the following aims:

• Synthetic chemistry & Medicinal chemistry
• Small molecule drug-like libraries
•  Peptide, cyclic peptide, and peptidomimetic libraries
•  Structure-activity relationship (SAR) studies
• Hit to lead optimization
•  Target-based drug design
•  Computational chemistry
•  Invitro PK studies

Nefzi’s research has been supported by the National Institute of Health (NIH), the National Institute of Allergy and Infectious Diseases (NIAID), the National Institute on Drug Abuse (NIDA), the National Cancer Institute (NCI), the National Institute of Aging (NIA), the National Science Foundation (NSF), Dr. Ralph and Marian Falk Medical Research Trust, and HWCOM Pilot grant.