Talk:Bioisostere

Sila substitution

Besides the substitutions mentioned in the article, there is the replacment of carbon with silicon. This is called sila substitution. Like the other mentioned substitutions, it has applicability in medicine. In particular, sila modified medicines have greater lipophilicity and less hydrophilicity. Also, depending on factors like silicon's different electronegativity, bonding angles, and bond lengths, these medicines can have different properties than the medcines of which they are modifications. There is research in HIV treatment, immunosuppresion, and reducing inflamation. See: http://www.ingentaconnect.com/content/ben/ddro/2005/00000002/00000006/art00006 GreySun (talk) 21:31, 21 November 2009 (UTC)

No mention of patent breaking as motivation for identifying bioisosteres for key functional groups in existing drugs

Clearly, avoiding patented chemical structures is a highly desirable goal of every pharmaceutical company. This is one of the major applications of the much more complicated, and modern, strategy of computation/automated combinatorial library construction, which (in this particular case) has the goal of finding chemical structures that cannot be predicted easily by an informed chemist/biochemist/pharmacologist/doctor. On the other hand, the much simpler strategy involves identifying key aspects of an existing compound that can be exchanged/modified without changing activity. This might include changing a peripheral part of the molecule that is not directly involved in active-site binding or recognition. If, on the other hand, the change requires that another functional group with the same, or nearly so, chemical behavior replace the original, then the goal becomes finding such a biostere to break a patent.184.189.220.114 (talk) 19:19, 8 March 2013 (UTC)

I agree that one of the main purposes of using a bioisostere is to avoid patents. This is significant enough to be stated in the lead (aka lede). The lead is greatly flawed (as of 6/14/2023). It states you can change bioisosteres in the "same chemical compound" which is by definition false. It states that replacing one bioisostere with another is done "without making significant changes to the chemical structure", again false. Worse, of course, is that changes to bioavailability, toxicity, activity, or metabolic pathway are OBVIOUSLY significant, contradicting the claim otherwise. That is, the lead is self-contradictory. It is also the case that the term "lead compound" would generally be understood to mean a chemical compound containing the element Lead, Pb. Without defining this awkward term and an authoritative reference to justify its use, it should be removed. The worst thing about this article is the fact that it doesn't mention that the term refers to the *shape* of the molecular structure. I am not familiar with the term's etymology, but the three root terms; bio, iso, stere, suggest it is intended to refer to biologically active same-shaped compounds.40.142.183.146 (talk) 00:04, 15 June 2023 (UTC)

Changes?

I'm thinking about some changes to this page.

• Role of bioisosterism in pharmaceutical industry (patent-breaking, drug design)
• A table of common bioisosteres including graphics

Thoughts? — Preceding unsigned comment added by Iandoxsee (talk • contribs) 19:14, 20 March 2015 (UTC)