2025 (Current Year) Faculty Courses School of Life Science and Technology Undergraduate major in Life Science and Technology

Pharmaceutical Chemistry

Academic unit or major: Undergraduate major in Life Science and Technology
Instructor(s): Mako Kamiya / Toshinori Fujie / Yoshiaki Masaki
Class Format: Lecture (Face-to-face)
Media-enhanced courses: -
Day of week/Period (Classrooms): 1-2 Tue / 1-2 Fri
Class: -
Course Code: LST.A343
Number of credits: 200
Course offered: 2025
Offered quarter: 2Q
Syllabus updated: Mar 19, 2025
Language: Japanese

Syllabus

Course overview and goals

The purpose of this lecture is to understand the development and action of pharmaceuticals. Firstly, practical knowledge of heterocyclic compounds which frequently appear as biologically active compounds and pharmaceuticals will be given, followed by their artificial synthesis and modification based on organic chemistry and derived medicines. Then, the history and flow of drug discovery will be outlined. This course gives lectures on not only practical organic reactions and syntheses but also the industrial production of medicines, obtained via the study of structure-activity relationship and molecular recognition. While this course, if necessary, allows students to review the subjects on nature, reactivity, analysis, and synthesis of organic compounds mastered during Organic Chemistry I (alkanes and haloalkanes)~IV (carbonyl compounds and amines), it provides them with more practical knowledge and theory of a higher level, by discussing concrete examples of the access to biologically active compounds or pharmaceuticals, the structure-activity relationship, and the matching study of drugs to their receptors in the design of artificial pharmaceutical drugs. Thus, this course has students acquire the practical ability to manage organic chemistry in the preparation of bioactive molecules and understand the broad area covered by organic chemistry including the extension to industrial production.

Course description and aims

By the end of this course, students will be able to:
1. Understand and explain that organic chemistry plays a critical role not only in the reaction and synthesis but also in the treatment of lead compounds and the structure-activity relationship in the development of pharmaceutical drugs.
2. Understand and explain the nature, reactions, and synthesis of heterocyclic compounds frequently found in pharmaceutical drugs.
3. Understand and explain the diversity of structures of naturally occurring products or biomolecules and their corresponding synthetic methods.
4. Understand and explain the process of molecular modification from naturally occurring products or biomolecules to pharmaceutical drugs.
5. Understand and explain the way to industrial production of pharmaceutical drugs.

Keywords

naming of medicines, lead compounds, molecular modification, structure-activity relationship, random screening, receptor, drug metabolism, heterocycles, biomolecules, natural organic compounds, pharmacokinetics, optically active compounds, molecular recognition

Competencies

Specialist skills
Intercultural skills
Communication skills
Critical thinking skills
Practical and/or problem-solving skills

Class flow

All classes and the exam are planned to be given face to face. However, the styles can be changed depending on the situation of COVID-19. Handout will be shared for each class, but the textbook shown below will also be used. Students are given concise exercise for the last 10 minutes of each class, and their solutions and remarks will be explained at the beginning of the next class.
Note: The 3rd test for understanding will be held on the 15th class, though it will be during the period of final exam and supplementary class.

Course schedule/Objectives

	Course schedule	Objectives
Class 1	Heterocyclic compounds and pharmaceuticals	Understand and explain the nature of heterocyclic compounds in pharmaceuticals and their synthesis.
Class 2	Aliphatic heterocyclic compounds and pharmaceuticals	Understand and explain the nature of aliphatic heterocyclic compounds in pharmaceuticals andtheir synthesis.
Class 3	Aromatic heterocyclic compound and pharmaceuticals	Understand and explain the nature of aromaticheterocyclic compounds in pharmaceuticals andtheir synthesis.
Class 4	Heterocyclic compounds and biological activity	Understand and explain the biological activities of heterocyclic compounds in nature.
Class 5	The 1st test for understanding
Class 6	History, current status, and flow of drug discovery and development	Understand and explain the history and current status and the flow of drug discovery and development.
Class 7	Recent research for drug discovery	Understand and explain recent trends in drug discovery research, including genomic drug discovery and biopharmaceuticals.
Class 8	Target biomolecules of drugs	Understand and explain the functions of target biomolecules of drugs, their interactions with drugs, and their mode of action.
Class 9	Typical pharmaceuticals I	Understand and explain the mechanism of action of typical drugs.
Class 10	The 2nd test for understanding
Class 11	Basics of drug development	Understand and explain the definition of drug, intellectual property, generics, drug hazards, norms, biostatistics, and R&D process for drug development.
Class 12	Pharmacokinetics and drug delivery systems	Understand and explain the design of drug molecules and drug delivery systems considering pharmacokinetics that is important in drug development.
Class 13	Structure of pharmaceuticals	Understand and explain the structure, bioisosterism, and chemical parameters that allow a drug to exhibit pharmacological action.
Class 14	Typical pharmaceuticals II	Understand and explain the mechanism of action of typical drugs.

Study advice (preparation and review)

To enhance effective learning, students are encouraged to spend approximately 100 minutes preparing for class and another 100 minutes reviewing class content afterwards (including assignments) for each class.
They should do so by referring to textbooks and other course material.

Textbook(s)

The 1~5th classes: The Japanese translation of K. Peter C. Vollhardt, Neil E. Schore, Organic Chemistry, 8th Edition (Last volume), Chapter 25, Kagakudojin (Japanese).
The 6~15th classes:Drug Discovery Science/Medicinal Chemistry, 2nd Edition, Kagakudojin (Japanese).

Reference books, course materials, etc.

If necessary, references are shown in class.

Evaluation methods and criteria

Students will be assessed on the concise exercise problems in each class (30%) and a final exam (70%).

Related courses

LST.A202 ： Organic Chemistry I (alkanes and haloalkanes)
LST.A207 ： Organic Chemistry II (alcohols and alkenes)
LST.A212 ： Organic Chemistry III (benzene and ketones)
LST.A217 ： Organic Chemistry IV (carbonyl compounds and amines)
LST.A333 ： Bioorganic Chemistry

Prerequisites

Not required.

Contact information (e-mail and phone) Notice : Please replace from ”[at]” to ”@”(half-width character).

M. Kamiya: kamiya.m.ad[at]m.titech.ac.jp、045-924-5233; T. Fujie: t_fujie[at]bio.titech.ac.jp, 045-924-5712; Y. Masaki: ymasaki[at]bio.titech.ac.jp, 045-924-5109

Office hours

Appointment by e-mail is recommended. M. Kamiya: R1A Bldg. 3F Room＃ 307; T. Fujie: B2 Bldg. 10F Room＃ 1022; Y. Masaki: B2 Bldg. 12F Room＃1232