Spirocyclic scaffolds in medicinal chemistry

K Hiesinger, D Dar'in, E Proschak… - Journal of Medicinal …, 2020 - ACS Publications
Spirocyclic scaffolds are incorporated in various approved drugs and drug candidates. The
increasing interest in less planar bioactive compounds has given rise to the development of …

Quest for novel chemical entities through incorporation of silicon in drug scaffolds

R Ramesh, DS Reddy - Journal of Medicinal Chemistry, 2017 - ACS Publications
In order to optimize a lead molecule for further development, bioisosteric replacements are
generally adopted as one of the strategies. Silicon appears to be the right choice as a …

The role of silicon in drug discovery: a review

JL Panayides, DL Riley, F Hasenmaile… - RSC Medicinal …, 2024 - pubs.rsc.org
This review aims to highlight the role of silicon in drug discovery. Silicon and carbon are
often regarded as being similar with silicon located directly beneath carbon in the same …

Progress in the medicinal chemistry of silicon: C/Si exchange and beyond

S Fujii, Y Hashimoto - Future Medicinal Chemistry, 2017 - Taylor & Francis
Application of silyl functionalities is one of the most promising strategies among various
'elements chemistry'approaches for the development of novel and distinctive drug …

Construction of benzosiloles, six-and eight-membered silacyclic skeletons, via a Pd-catalyzed intramolecular Mizoroki–Heck Reaction of vinylsilanes

K Ouyang, Y Liang, Z ** - Organic letters, 2012 - ACS Publications
Construction of Benzosiloles, Six- and Eight-Membered Silacyclic Skeletons, via a Pd-Catalyzed
Intramolecular Mizoroki–Heck Reaction of Vinylsilanes | Organic Letters ACS ACS Publications …

Synthetic approaches for the construction of five-and six-membered silaazacycles

W Wang, L Gao, Z Song - Synthesis, 2022 - thieme-connect.com
Silaazacycles (or azasilacycles), containing both nitrogen and silicon atoms, are appealing
ring structures in the development of silicon-containing functional molecules. The …

Direct Syn Addition of Two Silicon Atoms to a C≡C Triple Bond by Si−Si Bond Activation: Access to Reactive Disilylated Olefins

M Ahmad, AC Gaumont, M Durandetti… - Angewandte Chemie …, 2017 - Wiley Online Library
A catalytic intramolecular silapalladation of alkynes affords, in good yields and
stereoselectively, syn‐disilylated heterocycles of different chemical structure and size. When …

Can Silicon Make an Excellent Drug Even Better? An in vitro and in vivo Head‐to‐Head Comparison between Loperamide and Its Silicon Analogue Sila‐Loperamide

M Geyer, E Wellner, U Jurva, S Saloman… - …, 2015 - Wiley Online Library
Abstract Loperamide (1a), an opioid receptor agonist, is in clinical use as an antidiarrheal
agent. Carbon/silicon exchange (sila‐substitution) at the 4‐position of the piperidine ring of …

Disila-analogues of the synthetic retinoids EC23 and TTNN: synthesis, structure and biological evaluation

JBG Gluyas, C Burschka, S Dörrich, J Vallet… - Organic & …, 2012 - pubs.rsc.org
Silicon chemistry offers the potential to tune the effects of biologically active organic
molecules. Subtle changes in the molecular backbone caused by the exchange of a carbon …

Drug design based on the carbon/silicon switch strategy

R Tacke, S Dörrich - Atypical Elements in Drug Design, 2016 - Springer
Silicon chemistry has been demonstrated to be a novel source of chemical diversity in drug
design. The carbon/silicon switch strategy, ie, the strategic replacement of a carbon atom …