Literature DB >> 15330746

Exploitation of silicon medicinal chemistry in drug discovery.

John S Mills1, Graham A Showell.   

Abstract

There remains considerable pressure on the pharmaceutical industry to increase productivity and reduce the attrition of drug candidates. Genomics, parallel chemistry and high-throughput biology have not yielded the anticipated benefits, resulting in a renewed focus on validated targets and an aim to generate drugs directed towards such targets, which have a clear advantage. One strategy to identify and develop best-in-class drugs is to apply a high degree of innovation in chemistry and apply this to targets from gene families that have been clinically validated as tractable and drugable. The application of organosilicon medicinal chemistry in the context of privileged structures to aid drug design and development is one such innovative approach that is reviewed in this paper.

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Year:  2004        PMID: 15330746     DOI: 10.1517/13543784.13.9.1149

Source DB:  PubMed          Journal:  Expert Opin Investig Drugs        ISSN: 1354-3784            Impact factor:   6.206


  10 in total

1.  Exploring organosilane amines as potent inhibitors and structural probes of influenza a virus M2 proton channel.

Authors:  Jun Wang; Chunlong Ma; Yibing Wu; Robert A Lamb; Lawrence H Pinto; William F DeGrado
Journal:  J Am Chem Soc       Date:  2011-08-12       Impact factor: 15.419

2.  Regio- and Stereoselective Rhodium(II)-Catalyzed C-H Functionalization of Organosilanes by Donor/Acceptor Carbenes Derived from Aryldiazoacetates.

Authors:  Zachary J Garlets; Elliot F Hicks; Jiantao Fu; Eric A Voight; Huw M L Davies
Journal:  Org Lett       Date:  2019-06-11       Impact factor: 6.005

3.  Efficient, enantioselective assembly of silanediol protease inhibitors.

Authors:  Yingjian Bo; Swapnil Singh; Hoan Quoc Duong; Cui Cao; Scott McN Sieburth
Journal:  Org Lett       Date:  2011-03-07       Impact factor: 6.005

4.  Silicon Incorporated Morpholine Antifungals: Design, Synthesis, and Biological Evaluation.

Authors:  Gorakhnath R Jachak; Remya Ramesh; Duhita G Sant; Shweta U Jorwekar; Manjusha R Jadhav; Santosh G Tupe; Mukund V Deshpande; D Srinivasa Reddy
Journal:  ACS Med Chem Lett       Date:  2015-09-22       Impact factor: 4.345

5.  Design, Synthesis, and Identification of Silicon Incorporated Oxazolidinone Antibiotics with Improved Brain Exposure.

Authors:  B Seetharamsingh; Remya Ramesh; Santoshkumar S Dange; Pankaj V Khairnar; Smita Singhal; Dilip Upadhyay; Sridhar Veeraraghavan; Srikant Viswanadha; Swaroop Vakkalanka; D Srinivasa Reddy
Journal:  ACS Med Chem Lett       Date:  2015-10-26       Impact factor: 4.345

6.  Synthesis, Reactivity, Functionalization, and ADMET Properties of Silicon-Containing Nitrogen Heterocycles.

Authors:  Scott J Barraza; Scott E Denmark
Journal:  J Am Chem Soc       Date:  2018-05-15       Impact factor: 15.419

7.  Harnessing the β-Silicon Effect for Regioselective and Stereoselective Rhodium(II)-Catalyzed C-H Functionalization by Donor/Acceptor Carbenes Derived from 1-Sulfonyl-1,2,3-triazoles.

Authors:  Zachary J Garlets; Huw M L Davies
Journal:  Org Lett       Date:  2018-04-11       Impact factor: 6.005

8.  High-speed vibration-milling-promoted synthesis of symmetrical frameworks containing two or three pyrrole units.

Authors:  Marco Leonardi; Mercedes Villacampa; J Carlos Menéndez
Journal:  Beilstein J Org Chem       Date:  2017-09-15       Impact factor: 2.883

9.  Silicon-containing GABA derivatives, silagaba compounds, as orally effective agents for treating neuropathic pain without central-nervous-system-related side effects.

Authors:  Hiroshi Fukasawa; Hideaki Muratake; Ai Ito; Hideyuki Suzuki; Yohei Amano; Marina Nagae; Kiyoshi Sugiyama; Koichi Shudo
Journal:  ACS Chem Neurosci       Date:  2014-04-30       Impact factor: 4.418

Review 10.  Recent Advances in the Biological Investigation of Organometallic Platinum-Group Metal (Ir, Ru, Rh, Os, Pd, Pt) Complexes as Antimalarial Agents.

Authors:  Mziyanda Mbaba; Taryn M Golding; Gregory S Smith
Journal:  Molecules       Date:  2020-11-12       Impact factor: 4.411

  10 in total

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