Isosterism or bioisosterism is one of the approaches most frequently used in the design of new molecules 1. Bhalerao department of pharmachemistry mgvs pharmacy. In this context, a critical appraisal of the concepts of isosterism and bioisosterism is put forward, isosterism is redefined, and bioisosterism is discarded in favor of the new concept of bioanalogy. The extensive application of isosterism to modify a part of a. The use of bioisosterism in drug design and molecular. Bioisosterism is a strategy of medicinal chemistry for the rational design of new drugs, applied with a lead compound lc as a special process of molecular modification 1. In a broad sense, bioisosteres may be identified as. The broadest definition of bioisosteres is, groups or molecules those have. In medicinal chemistry, bioisosteres are chemical substituents or groups with similar physical or.
Bioisosterism is used to reduce toxicity, change bioavailabilty, or modify the activity of the lead compound, and may alter the metabolism of the lead. This article belongs to the special issue recent effective application of bioisosterism. Bioisosterism and isosterism by swapnil ratnakar bhalerao free download as powerpoint presentation. The extensive application of isosterism to modify a part of a biologically active molecule to get. A useful strategy for molecular modification and drug. The use of bioisosterism in drug design and molecular modification priyanka l. Isosterism definition, the quality or state of being isosteric.
Beyond markush protecting activity not chemical structure pdf. In this case, the replacement of the phenol by heterocyclic nhcontaining rings was performed in order to slow metabolism and hence to. Pdf input of isosteric and bioisosteric approach in drug design. The notion of isosterism was introduced in 1919 by langmuir. Pharmaceuticals free fulltext bioisosteric replacement as a.
Download fulltext pdf input of isosteric and bioisosteric approach in drug design article pdf available in journal chemical society of pakistan volume 36no. In nature, we have identified many examples of isosterism as a. Isosterism and bioisosterism in drug design pdf may 7, application of isosteres in drug design oxetanes in drug discovery 2 exchangeable group isosterism in which the properties of discrete. The most popular surrogates for phenolic functions are nh groups rendered acidic through the presence of an electronattracting group. Pdf the use of bioisosterism in drug design and molecular. Subset of bioisosterism identification of the core functional or structural element. Aug 1, isosterism and bioisosterism in drug design. Pdf input of isosteric and bioisosteric approach in drug. Introduction isoelectronic, created the concept of isosterism to define atoms or organic or inorganic molecules which possess the bioisosterism is a strategy.
Pdf bioisosterism has unique relevance in the field of. Isosterism can also contribute to the productive application in the design and optimization of catalysts on organic chemistry. The second part inves tigates methods that apply knowledge bases of experimental data from a. Isosterism and bioisosterism case studies with muscarinic.
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