Chapter 2 · Book Chapter
Paid Access Peer Reviewed

AI-Assisted Design of Heterocyclic Scaffolds

Prof. Nagargoje Sangram Gangadhar1, Prof. Kashmira Kailas Malusare2,*

Corresponding author: [email protected]

Abstract

Artificial intelligence (AI) is transforming modern drug discovery by enabling the rapid design and optimization of biologically active molecules. Among these, heterocyclic scaffolds occupy a central position because they are present in the majority of approved pharmaceuticals and exhibit diverse biological activities. Conventional approaches to heterocyclic scaffold design are often time-consuming, expensive and dependent on extensive experimental screening, leading to high failure rates during drug development. The integration of AI techniques, including machine learning, deep learning, generative models and predictive analytics, has significantly accelerated the identification of novel heterocyclic compounds with improved pharmacological properties. AI-driven platforms can analyse large chemical and biological datasets, predict molecular properties, estimate toxicity, optimize synthesis pathways and identify promising lead molecules with greater accuracy than traditional methods. Furthermore, the combination of chemistry, biology and computer science has enabled the development of intelligent computational tools that support rational drug design and personalized medicine. This review discusses the evolution of drug discovery, the limitations of conventional heterocyclic scaffold design, the emergence of AI in medicinal chemistry and the growing role of computational intelligence in pharmaceutical research.

Artificial IntelligenceHeterocyclic ScaffoldsMedicinal ChemistryDrug DiscoveryMachine LearningDeep LearningComputational IntelligenceMolecular DesignLead OptimizationPharmaceutical Research

Author Affiliations

  • 1 Associate Professor, Department of Pharmaceutical Chemistry, Rashtriya College of Pharmacy, Hatnoor, Maharashtra, India.
  • 2 Assistant Professor, Department of Pharmacology, Dr. Kolpe Institute of Pharmacy, Kolpewadi, Maharashtra, India.

How to Cite this Chapter

Gangadhar, N. S., & Malusare, K. K. (2026). AI-Assisted Design of Heterocyclic Scaffolds. In V. Khairnar, U. R. Mandage, & S. D. Pawar (Eds.), Next-Generation Heterocyclic Scaffolds for Precision Therapeutics (pp. 49–93). WiseLeaf Scientific Ventures. https://doi.org/10.66079/wiseleaf.next-generation-heterocyclic-scaffolds.2026
Back to the full volume

Related WiseLeaf titles