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  3. Strategies for Structural Modification of Small Molecules to Improve Blood-Brain Barrier Penetration: A Recent Perspective

Strategies for Structural Modification of Small Molecules to Improve Blood-Brain Barrier Penetration: A Recent Perspective

  • J Med Chem. 2021 Sep 23;64(18):13152-13173. doi: 10.1021/acs.jmedchem.1c00910.
Baichen Xiong 1,  Yuanyuan Wang 1,  Ying Chen 2,  Shuaishuai Xing 1,  Qinghong Liao 2,  Yao Chen 3,  Qi Li 1 4,  Wei Li 1,  Haopeng Sun 1
Affiliations

Affiliations

  • 1 School of Pharmacy, China Pharmaceutical University, Nanjing 211198, People's Republic of China.
  • 2 Department of Natural Medicinal Chemistry, China Pharmaceutical University, Nanjing 211198, People's Republic of China.
  • 3 School of Pharmacy, Nanjing University of Chinese Medicine, Nanjing 210023, People's Republic of China.
  • 4 School of Basic Medicine, Qingdao University, Qingdao 266071, People's Republic of China.
PMID: 34505508 DOI: 10.1021/acs.jmedchem.1c00910
Abstract

In the development of central nervous system (CNS) drugs, the blood-brain barrier (BBB) restricts many drugs from entering the brain to exert therapeutic effects. Although many novel delivery methods of large molecule drugs have been designed to assist transport, small molecule drugs account for the vast majority of the CNS drugs used clinically. From this perspective, we review studies from the past five years that have sought to modify small molecules to increase brain exposure. Medicinal chemists make it easier for small molecules to cross the BBB by improving diffusion, reducing efflux, and activating carrier transporters. On the basis of their excellent work, we summarize strategies for structural modification of small molecules to improve BBB penetration. These strategies are expected to provide a reference for the future development of small molecule CNS drugs.

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