Literature DB >> 30243589

Methyl-containing pharmaceuticals: Methylation in drug design.

Shaoyi Sun1, Jianmin Fu2.   

Abstract

The importance of methyl groups in modulating biological activity, selectivity, solubility, metabolism and pharmacokinetic/pharmacodynamic properties of biologically active molecules is highlighted. The information compiled from selected beneficial cases, focuses mostly on marketed drugs and clinical candidates, and indicates that the methylation strategy has been successful in drug design.
Copyright © 2018 Elsevier Ltd. All rights reserved.

Keywords:  Drug design; Lead optimization; Methyl group; Methylation

Mesh：

Substances：

Year:  2018        PMID： 30243589     DOI： 10.1016/j.bmcl.2018.09.016

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  12 in total

1.  Nickel/Photoredox-Catalyzed Methylation of (Hetero)aryl Chlorides Using Trimethyl Orthoformate as a Methyl Radical Source.

Authors:  Stavros K Kariofillis; Benjamin J Shields; Makeda A Tekle-Smith; Michael J Zacuto; Abigail G Doyle
Journal:  J Am Chem Soc       Date:  2020-04-10       Impact factor: 15.419

2.  Discovery of Stereospecific PARP-1 Inhibitor Isoindolinone NMS-P515.

Authors:  Gianluca Papeo; Paolo Orsini; Nilla R Avanzi; Daniela Borghi; Elena Casale; Marina Ciomei; Alessandra Cirla; Viviana Desperati; Daniele Donati; Eduard R Felder; Arturo Galvani; Marco Guanci; Antonella Isacchi; Helena Posteri; Sonia Rainoldi; Federico Riccardi-Sirtori; Alessandra Scolaro; Alessia Montagnoli
Journal:  ACS Med Chem Lett       Date:  2019-03-13       Impact factor: 4.345

3.  Deaminative Reductive Methylation of Alkylpyridinium Salts.

Authors:  Olivia P Bercher; Shane Plunkett; Thomas E Mortimer; Mary P Watson
Journal:  Org Lett       Date:  2021-08-31       Impact factor: 6.072

4.  Discovery and Preclinical Profiling of GSK3839919, a Potent HIV-1 Allosteric Integrase Inhibitor.

Authors:  Kyle Parcella; Tao Wang; Kyle Eastman; Zhongxing Zhang; Zhiwei Yin; Manoj Patel; Yong Tu; Barbara Zhizhen Zheng; Michael A Walker; Mark G Saulnier; David Frennesson; Michael Bowsher; Eric Gillis; Kevin Peese; Makonen Belema; Christopher Cianci; Ira B Dicker; Brian McAuliffe; Bo Ding; Paul Falk; Jean Simmermacher; Dawn D Parker; Prasanna Sivaprakasam; Kevin Kish; Hal Lewis; Umesh Hanumegowda; Susan Jenkins; John F Kadow; Mark Krystal; Nicholas A Meanwell; B Narasimhulu Naidu
Journal:  ACS Med Chem Lett       Date:  2022-05-09       Impact factor: 4.632

5.  Using Data Science To Guide Aryl Bromide Substrate Scope Analysis in a Ni/Photoredox-Catalyzed Cross-Coupling with Acetals as Alcohol-Derived Radical Sources.

Authors:  Stavros K Kariofillis; Shutian Jiang; Andrzej M Żurański; Shivaani S Gandhi; Jesus I Martinez Alvarado; Abigail G Doyle
Journal:  J Am Chem Soc       Date:  2022-01-05       Impact factor: 16.383

6.  C(sp3)-H methylation enabled by peroxide photosensitization and Ni-mediated radical coupling.

Authors:  Aristidis Vasilopoulos; Shane W Krska; Shannon S Stahl
Journal:  Science       Date:  2021-04-23       Impact factor: 47.728

7.  Selective α-Methylation of Aryl Ketones Using Quaternary Ammonium Salts as Solid Methylating Agents.

Authors:  Johanna Templ; Michael Schnürch
Journal:  J Org Chem       Date:  2022-03-07       Impact factor: 4.354

8.  Scalable (Enantioselective) Syntheses of Novel 3-Methylated Analogs of Pazinaclone, (S)-PD172938 and Related Biologically Relevant Isoindolinones.

Authors:  Antonia Di Mola; Giorgia Nicastro; Lorenzo Serusi; Rosanna Filosa; Mario Waser; Antonio Massa
Journal:  Molecules       Date:  2022-09-01       Impact factor: 4.927

9.  A methylation platform of unconventional inert aryl electrophiles: trimethylboroxine as a universal methylating reagent.

Authors:  Boya Feng; Yudong Yang; Jingsong You
Journal:  Chem Sci       Date:  2020-05-25       Impact factor: 9.825

10.  2-Oxoester Phospholipase A2 Inhibitors with Enhanced Metabolic Stability.

Authors:  Giorgos S Koutoulogenis; Maroula G Kokotou; Daiki Hayashi; Varnavas D Mouchlis; Edward A Dennis; George Kokotos
Journal:  Biomolecules       Date:  2020-03-24
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