A practical drug discovery project at the undergraduate level

Design and Elaboration of a Tractable Tricyclic Scaffold To Synthesize Druglike Inhibitors of Dipeptidyl Peptidase-4 (DPP-4), Antagonists of the C–C Chemokine Receptor Type 5 (CCR5), and Highly Potent and Selective Phosphoinositol-3 Kinase δ (PI3Kδ) Inhibitors

“…In this approach, we wanted to use the molecular scaffold to function as a key molecular recognition group to increase kinase activity and also fine-tune kinase isoform selectivity. In this respect, we were drawn to the exciting possibility of designing a set of potent and selective phosphoinositol-3 kinase δ isoform inhibitors, an area of interest from our University of Nottingham and GlaxoSmithKline research teaching collaboration …”

Modular and divergent synthesis of 2,N3-disubstituted 4-quinazolinones facilitated by regioselective N-alkylation

“…The vast molecular space available for targets in these endeavors provides researchers with varying amounts of laboratory experience an opportunity to contribute to an overarching synthetic goal while maximizing individual impact by focusing on a specific subarea. 5 As a research group at a primarily undergraduate institution, we sought to design a project that would generate meaningful data while offering rich training opportunities for undergraduate students. 6 Several factors influenced our selection of a suitable target for compound library development: (1) biological activity and availability of collaborators for biological assessment and analysis, (2) accessibility to undergraduate researchers in terms of structural complexity and anticipated length of synthetic route, and (3) potential for facile structural modification.…”

Synthesis of Quinolone Antibiotic Analogues: A Multistep Synthetic Chemistry Experiment for Undergraduates

“…This multistep experiment allows for a more challenging synthetic organic chemistry experience for undergraduate students and allows them to carry out organic transformations typically used in the pharmaceutical industry and that are taught in the organic chemistry curriculum, which includes the preparation of acyl chlorides, 1,4-conjugate addition–elimination, heterocycle synthesis, nucleophilic aromatic substitution, and ester hydrolysis. This experiment provides a guided-inquiry based project that is closely aligned with industrial pharmaceutical chemistry and research and contributes to our ongoing work in training “industry-ready” graduates in medicinal chemistry. − …”