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  • MAY 2020 Issue has been successfully launched on 1 May 2020.



Nidhi Kala* and Sokindra Kumar


Bioisosterism is a unique strategy of molecular modification of lead compound to improve its pharmacodynamic & pharmacokinetic properties. The aim of bioisosterism is to boost the physical, biological & pharmacological properties as well as rectify the toxicity of lead molecule. The present review highlight the vital role of in Structural activity relationship of lead molecule. Bioisosterism has played a central role in the development of drug molecules almost from the outset of the pharmaceutical industry. The promise of bioisosterism is that the properties of a compound can be fine-tuned without affecting its underlying biological activity. This promise is not however without its challenges. Successfully applying bioisosterism to achieve the desired molecular outcome is difficult because of the fundamental problem that chemical structure is an unreliable indicator of biological activity. Small changes in a molecule can have a profound impact on a compound’s activity, specificity and toxicity, whilst completely different chemotypes may have near identical biological activity profiles. More rigorous and reproducible methods for suggesting relevant, non-obvious and yet synthetically intuitive bioisosteres would have wide applicability.

Keywords: Isosterism, Bioisosterism, SAR, Retroisosterism.

[Full Text Article]

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