Lead Discovery and Lead Optimization: A Useful Strategy in Molecular  Modification of Lead Compound in Analog Design

Ashutosh Kumar Patidar; Selvam G; Jeyakandan M; Ashok Kumar Mobiya; Ajay Bagherwal; Gaurav Sanadya; Ramraj Mehta

doi:10.37285/ijddd.2.2.4

Articles

Vol. 2 No. 2 (2011): April – June 2011

Lead Discovery and Lead Optimization: A Useful Strategy in Molecular Modification of Lead Compound in Analog Design

Ashutosh Kumar Patidar^▸^▾
Selvam G^▸^▾
Jeyakandan M^▸^▾
Ashok Kumar Mobiya^▸^▾
Ajay Bagherwal^▸^▾
Gaurav Sanadya^▸^▾
Ramraj Mehta^▸^▾

Requires Subscription or Fee pdf (INR 2000)

DOI: https://doi.org/10.37285/ijddd.2.2.4
Submitted: November 28, 2024
Published: 2024-12-08

Abstract

The current trend in the drug design is to develop new clinically effective agents through the molecular modification of a lead nucleus. A lead compound in drug discovery is a chemical compound that has pharmacological or biological activity. Lead optimization is the synthetic modification of a biologically active compound, to fulfill all stereoelectronic, physicochemical, pharmacokinetic and toxicologic required for clinical usefulness. The main objective of this review is to discuss the methods of lead discovery, lead optimization and its role in molecular modification of lead compound in analog design.

References

[1] Kulkarni, V.M.; Bothara, K.G. Drug Design; 4 Ed.; Nirali Prakashan, 2006; pp 1-13.
[2] Huber, W. J. Mol. Recognit. 2005, 18, 273-281.
[3] Abraham, D.J. Burgers Medicinal Chemistry and Drug Design (Drug Discovery); Cannon J.G., 6 Ed.; John Wiley & Sons, 1998; Vol. 1, pp 689-694.
[4] Patrick G.L. An Introduction to Medicinal Chemistry; 3 Ed.; University Press: Oxford, 2005, pp 200-217.
[5] Hong, H.; Tong, W.; Xie, Q.; Fang, H.; Perkins, R. SAR QSAR Environ. Res. 2005, 16(4), 339-347.
[6] Erlanson, D.A.; Dowell, R.S.; Brien, T. J. Med. Chem. 2004, 47(14), 3463-3482.
[7] Fejzo, J.; Lepre, C.A.; Peng, J.W.; Moore, J. M. Chem. Biol. 1999, 6, 755-769.
[8] Gill, A. Mini. Rev. Med. Chem. 2004, 4, 301-311.
[9] Fattori, D. Drug Discovery Today 2004, 9, 229-238.
[10] Landon, C.; Legrain, M.; Menin, L.; Schott, V. Protein Sci. 2004, 13, 703-713.
[11] Huth, J.R.; Sun, C. Comb. Chem. High Throughput Screening 2002, 5, 631-643.

Keywords

Lead discovery
Lead optimization
Molecular modification
Analog design

How to Cite

Patidar, A. K., G, S., M, J., Mobiya, A. K., Bagherwal, A., Sanadya, G., & Mehta, R. (2024). Lead Discovery and Lead Optimization: A Useful Strategy in Molecular Modification of Lead Compound in Analog Design . International Journal of Drug Design and Discovery, 2(2), 458–463. https://doi.org/10.37285/ijddd.2.2.4

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[1] [1] Kulkarni, V.M.; Bothara, K.G. Drug Design; 4 Ed.; Nirali Prakashan, 2006; pp 1-13.

[2] [2] Huber, W. J. Mol. Recognit. 2005, 18, 273-281.

[3] [3] Abraham, D.J. Burgers Medicinal Chemistry and Drug Design (Drug Discovery); Cannon J.G., 6 Ed.; John Wiley & Sons, 1998; Vol. 1, pp 689-694.

[4] [4] Patrick G.L. An Introduction to Medicinal Chemistry; 3 Ed.; University Press: Oxford, 2005, pp 200-217.

[5] [5] Hong, H.; Tong, W.; Xie, Q.; Fang, H.; Perkins, R. SAR QSAR Environ. Res. 2005, 16(4), 339-347.

[6] [6] Erlanson, D.A.; Dowell, R.S.; Brien, T. J. Med. Chem. 2004, 47(14), 3463-3482.

[7] [7] Fejzo, J.; Lepre, C.A.; Peng, J.W.; Moore, J. M. Chem. Biol. 1999, 6, 755-769.

[8] [8] Gill, A. Mini. Rev. Med. Chem. 2004, 4, 301-311.

[9] [9] Fattori, D. Drug Discovery Today 2004, 9, 229-238.

[10] [10] Landon, C.; Legrain, M.; Menin, L.; Schott, V. Protein Sci. 2004, 13, 703-713.

[11] [11] Huth, J.R.; Sun, C. Comb. Chem. High Throughput Screening 2002, 5, 631-643.