Structure-Activity Relationships of Pyrimidine Derivatives and their Biological Activity - A Review

Abstract

Background: Heterocycles play a major role in many fields of biochemical and physiological such as amino acids, DNA bases, vitamins, endogenous neurotransmitters, etc. Nitrogencontaining heterocyclic compounds play a vital role in medicinal chemistry and exhibit notable biological and pharmacological activities. In the past two decades, scientists focused more on the diverse biological activities of pyrimidine derivatives. Pyrimidine is a six-membered heterocyclic compound, and it is present naturally in nucleic acid components (uracil, thymine, and cytosine) and vitamin B1; it is a promising lead molecule for synthesising compounds with various substitutions to treat various diseases.

Objective: We focused on the structure-activity relationship of pyrimidine derivatives and its various biological activities reported from 2010 to date.

Results: From this review, we concluded that the position of substituents in the pyrimidine nucleus greatly influences biological activities. Thus, the pyrimidine nucleus showed anti-microbial, anticancer, anti-inflammatory, anti-tubercular, anti-convulsant, antihypertensive, anthelmintic, antidepressant, analgesic, anti-hyperglycemic activities, etc. Conclusion: This study provides an overview of the pyrimidine nucleus and its derivatives from 2010 to date. There is a future scope for identifying a lead molecule for the target biological activity.

Keywords: Heterocycles; biological activities; drug discovery; lead molecule.; pyrimidine; substituents.