A Decade of FDA-Approved Pharmacophore-Based Small Molecules: Advances in Medicinal Chemistry from 2014 to 2024

Randhe Siddhant Sanjaykumar; Chavan Sagar Basavaraj; Anam Sania Md. Arshad; Rohit Singh; Neeraj Mahindroo

doi:10.1055/s-0043-1775470

Synlett, Table of Contents

Synlett 2025; 36(16): 2499-2526
DOI: 10.1055/s-0043-1775470

perspectives

Small Molecules in Medicinal Chemistry

A Decade of FDA-Approved Pharmacophore-Based Small Molecules: Advances in Medicinal Chemistry from 2014 to 2024

Authors

Randhe Siddhant Sanjaykumar‡
Chavan Sagar Basavaraj‡
Anam Sania Md. Arshad
Rohit Singh ∗
Neeraj Mahindroo ∗

Abstract

All articles of this category

Abstract

Over the past decade, the pharmaceutical field has seen significant advancements with the approval of innovative small-molecule drugs by the FDA. These low molecular weight compounds have set new benchmarks in therapy. This review examines their design, medical applications, mechanisms of action, and impact across various areas of medicine. It also emphasizes the key structural features critical to their success, highlighting progress in medicinal chemistry.

1 Introduction

2 Overview of Small Molecule Therapeutics (2014–2024)

3 Pharmacophore Classification and Key Approvals

3.1 2014: Foundational Advancements

3.2 2015–2016: Addressing Rare and Chronic Diseases

3.3 2017–2019: Oncology and Neurological Milestones

3.4 2020–2021: Responses to Global Health Needs

3.5 2022–2024: Cutting-Edge Innovations

3.6 Remdesivir; A Perfect Example of Pharmacophore-Driven Drug Discovery

4 Structural and Mechanistic Insights

4.1 Structural Determinants

4.2 Mechanistic Versatility

5 Therapeutic Breakthroughs

5.1 Oncological Innovations

5.2 Infectious Disease Management

5.3 Neurological and Psychiatric Advances

5.4 Cardiovascular and Related Advances

5.5 Miscellaneous Diseases

5.6 Summary

6 Challenges and Future Perspectives

6.1 Addressing Drug Resistance

6.2 Integrating Artificial Intelligence (AI) in Drug Discovery

6.3 Precision Medicine

6.4 Sustainability in Drug Development

7 Conclusion

Key words

small molecules - FDA - pharmacophore - pharmaceutical chemistry

Full Text

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