This book is very useful for students of the Faculty of Pharmacy, Faculty of Medicine (include nursing), Faculty of Animals Medical, Faculty of Dentistry, researchers, lecturer, chemist and other professions who are interested in the field of medicine. This book is an application Medicinal Chemistry, particular Drug Design and Development. Medicinal Chemistry is a compulsory subject in the Faculty of Pharmacy in Indonesia. This book as a response and responsibility of the author to share the experience. Drug discovery is one of the tasks pharmacy profession. The author is deeply concerned with pharmaceutical condition in developing countries specially Indonesia. For example, there are more than 80 Faculty of Pharmacy in Indonesia, to date there is no pharmacist who invented the synthetic drugs that popular in the world. If Prof. B.J. Habibie from Indonesia can create CN235 and R80 aircraft, pharmacist in developing countries specially Indonesia must be as inventor of a new drug. From the past until now, drug discovery is only carried out by pharmacist from modern country.