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Review
. 2018;57(1):113-233.
doi: 10.1016/bs.pmch.2018.01.002. Epub 2018 Mar 22.

Current Trends in Macrocyclic Drug Discovery and beyond-Ro5

Sulejman Alihodžić  1 , Mirjana Bukvić  1 , Ivaylo J Elenkov  1 , Antun Hutinec  1 , Sanja Koštrun  1 , Dijana Pešić  1 , Gordon Saxty  1 , Linda Tomašković  1 , Dinko Žiher  1
Affiliations
Review

Current Trends in Macrocyclic Drug Discovery and beyond-Ro5

Sulejman Alihodžić et al. Prog Med Chem. 2018.

Abstract

This chapter will discuss the recent literature of macrocycles and drug-like property space moving beyond the rule of five (bRo5). Trends in chemical classes that fall within this definition are discussed and the impact of the latest technologies in the field assessed. The physicochemical properties, which have provided both successes and challenges, especially in scale-up, are discussed. A recent patent literature is reviewed and the chapter concludes with a perspective on the future of macrocyclic drug discovery.

Keywords: 3D properties; Drug discovery; Hard target; Increased complexity; Macrocycles; Oral bioavailability; PPI; beyond-Ro5.

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