Structure--activity relationships are foundational concepts in biochemistry and drug design. Despite their importance, it can be difficult to create and execute laboratory activities that allow students to directly observe the interactions between small-molecule drugs and their biomolecular targets. Here, we report an activity that investigates…

The concept of co-amorphous systems is introduced in an integrated laboratory experiment, designed for advanced chemistry students, using solvent-free, environmentally friendly mechanochemistry. The dual-drug naproxen-cimetidine co-amorphous system (NPX-CIM) is investigated as an example of the emergent field of medicinal mechanochemistry.…

The spectrophotometric determination of the percent composition of an aspirin tablet is a common first-year, general chemistry undergraduate laboratory procedure. The experiment requires that a known amount of pure acetylsalicylic acid be quantitatively converted into the soluble disodium salicylic acid that is further reacted with excess…

Plant-derived natural products are an important source of potential medicines and continue to have a major impact on the drug discovery process. Natural product discovery assignments provide an opportunity to present various experimental techniques to undergraduate students in introductory medicinal chemistry. This assignment was developed to…

In this laboratory experiment, students explore the aquatic photochemical fate of ranitidine and cimetidine, two common pharmaceutical pollutants found in wastewater. It provides an engaging environmental context for students to develop knowledge of reaction kinetics and photochemistry as well as skill in using analytical instrumentation. This…

We describe a 2 h general-chemistry experiment that introduces college students not only to the concepts, synthesis, and applications of nanomaterials at an early stage but also the use of a spectrophotometer for quantification and unknown determination based on Beer's Law. The procedure involves students (1) preparing a nanocomposite by…

Zinc oxide is a common additive in food, cosmetics, and medicines. Here, we describe the validation of methods to analyze two pharmaceutical samples containing ZnO--talc powder and dermal ointment--by ethylenediaminetetraacetic acid (EDTA) titration. The methods developed were implemented as a practical class to students of a Quantitative Analysis…

An experiment for the synthesis of N-acyl derivatives of natural amino acids has been developed as part of the Distributed Drug Discovery (D3) program. Students use solid-phase synthesis techniques to complete a three-step, combinatorial synthesis of six products, which are analyzed using LC-MS and NMR spectroscopy. This protocol is suitable for…

Here, students determine aspirin (acetylsalicylic acid) mass in pharmaceutical tablets using a colorimetric method. Aspirin, salicylate, and salicylic acid do not absorb visible light. Thus, in alkaline medium, acetylsalicylic acid was hydrolyzed to salicylate; then, it was reacted with an acidic Fe(III) solution, and a violet complex was formed.…

A semester-long research project for second-semester organic chemistry lab sections was developed. Student projects were based on preliminary data from faculty research that suggested the natural product neurolenin B to be a treatment for lymphatic filariasis. Students isolated neurolenins from the Central American plant "Neurolaena…

Laboratory experiments were developed to introduce students to the quantitation of drugs of abuse by high performance liquid chromatography-tandem mass spectrometry (LC-MS/MS). Undergraduate students were introduced to internal standard quantitation and the LC-MS/MS method optimization for cocaine. Cocaine extracted from paper currency was…

Integrative, research-based experiences have shown tremendous potential as effective pedagogical approaches. Pharmaceutical development is an exciting field that draws heavily on organic chemistry and biochemistry techniques. A capstone drug synthesis/analysis laboratory is described where biochemistry students synthesize azo-stilbenoid compounds…

A laboratory sequence is described that is suitable for upper-level biochemistry or molecular biology laboratories that combines project-based and traditional laboratory experiments. In the project-based sequence, the individual laboratory experiments are thematically linked and aim to show how a bacterial antibiotic sensing noncoding RNA (the…

"Drug Discovery" is a 13-week lecture and laboratory-based course that was developed to introduce non-science majors to foundational chemistry and biochemistry concepts as they relate to the unifying theme of drug discovery. The first part of this course strives to build students' understanding of molecules, their properties, the…

Caffeine (1,3,7-trimethylxanthine) is an alkaloid stimulant that is popular in beverages. Fluorescence-coupled methods have been used to measure the caffeine content in coffee, tea, soft drinks, energy drinks, and cosmetics. In this experiment, we have developed a method for detecting caffeine in beverages utilizing the effect of the caffeine…