Bioactive Molecules via Morita–Baylis–Hillman Chemistry

Ch. N. S. Sai Pavan Kumar; Vaidya Rao Jayathirtha

doi:10.1055/a-2535-1306

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DOI: 10.1055/a-2535-1306

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Small Molecules in Medicinal Chemistry

Bioactive Molecules via Morita–Baylis–Hillman Chemistry

Ch. N. S. Sai Pavan Kumar

^bDepartment of Chemistry, School of Applied Science and Humanities, Vignan’s Foundation for Science, Technology and Research, Vadlamudi, Guntur 522213, Andhra Pradesh, India

^cDepartment of Chemistry, Vignan Degree & P.G. College, Palakaluru Road, Guntur 520 009, Andhra Pradesh, India

,

Vaidya Rao Jayathirtha∗

^aOrganic Synthesis and Process Chemistry Department, AcSIR-Ghaziabad, CSIR-Indian Institute of Chemical Technology, Uppal Road Tarnaka, Hyderabad – 500007, Telangana, India

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Abstract

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Abstract

Morita–Baylis–Hillman (MBH) chemistry was applied to the synthesis of a variety of new chemical entities and their bioactivity was evaluated. Various substances synthesized via MBH chemistry have: antimalarial, anti-inflammatory, antidiabetic, antimicrobial, antitubercular, and anticancer activity and also act as phosphodiesterase inhibitors. There are a few instances animal model and biology studies explored. Several hits and lead molecules are identified and their IC₅₀ values listed. The simplicity of Morita–Baylis–Hillman chemistry provides a realistic, impactful option for the pharma industry.

1 Introduction

2 Antimalarial Activity

3 Anti-inflammatory Activity of MBH Adducts Coupled to Heterocycles

4 Antidiabetic Activity of Epalrestat Analogues Derived from MBH Adducts

5 Antimicrobial Activity

6 Antitubercular Activity of N-Cinnamyl-isatins

7 Inhibitors of Phosphodiesterase-3 (PDE3); Cardiotonic Agents

8 Anticancer Activity

9 Asymmetric Morita–Baylis–Hillman Reactions

10 Conclusion

Keywords

Morita–Baylis–Hillman - MBH - heterocycles - bioactive molecules - pharmaceuticals

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References

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