Course Catalog

Designing around Toxicophores in Drug Discovery

This course will focus understanding the role of metabolic activation in the manifestation of drug toxicity. Background information on the role of reactive metabolites in drug-induced liver injury and other forms of drug-induced toxicity will be followed by a comprehensive survey of toxicophores. Each vignette provides the mechanistic organic chemistry underlying the activation of a particular toxicophore, illustrated by examples from the literature that capture problematic drugs and drug design strategies that have been employed to circumvent the processes.

This course is based on short course presentations made at consecutive ACS ProSpectives conferences in 2008 and 2009. It has also been presented internally at Bristol-Myers Squibb as part of internal medicinal chemistry courses. This course can be taken in conjunction with Applications of Bioisosteres in Drug Design.

Course Details

Key Topics

  • Tactical application of isosteres in drug design
  • Designing around toxicophores
  • Drug activation by endogenous enzymes

Information

This course will focus understanding the role of metabolic activation in the manifestation of drug toxicity. Background information on the role of reactive metabolites in drug-induced liver injury and other forms of drug-induced toxicity will be followed by a comprehensive survey of toxicophores. Each vignette provides the mechanistic organic chemistry underlying the activation of a particular toxicophore, illustrated by examples from the literature that capture problematic drugs and drug design strategies that have been employed to circumvent the processes.

This course is based on short course presentations made at consecutive ACS ProSpectives conferences in 2008 and 2009. It has also been presented internally at Bristol-Myers Squibb as part of internal medicinal chemistry courses. This course can be taken in conjunction with Applications of Bioisosteres in Drug Design.

Who Should Attend

These courses will appeal to practicing medicinal chemists at all stages of their careers, at both the PhD and BS/MS levels.

Benefits

The course attendees will learn how to apply isosteres to the drug design process and how to avoid introducing structural elements with incipient metabolic activation issues. The courses will be of value to medicinal chemists in any area of drug discovery.

Course Locations

Date

TBA

Check-in opens at 7:30 a.m. on the day of the course.

Course runs from 1:00 p.m. to 5:00 p.m.

Register Via Mail

Venue

The course fee includes a course binder.

Five for Four! Register five people for one course, one person for five courses, or any combination in between and your fifth registration is free. Note: This discount is only available if you register by fax or mail and mention this discount. May not be combined with any other offer.


Pricing

About the Instructor

  • Nicholas A. Meanwell

    is Executive Director of Discovery Chemistry at Bristol-Myers Squibb Research and Development and a co-chair of the Tactical Approaches to the Challenge of Drug Failure ACS ProSpectives Conference.