Fluorine and fluorinated motifs in the design and application of bioisosteres for drug design

NA Meanwell - Journal of medicinal chemistry, 2018 - ACS Publications
The electronic properties and relatively small size of fluorine endow it with considerable
versatility as a bioisostere and it has found application as a substitute for lone pairs of …

Applications of fluorine in medicinal chemistry

EP Gillis, KJ Eastman, MD Hill… - Journal of medicinal …, 2015 - ACS Publications
The role of fluorine in drug design and development is expanding rapidly as we learn more
about the unique properties associated with this unusual element and how to deploy it with …

Highlights on US FDA-approved fluorinated drugs over the past five years (2018–2022)

S Ali, J Zhou - European journal of medicinal chemistry, 2023 - Elsevier
The objective of this review is to provide an update on the fluorine-containing drugs
approved by US Food and Drug Administration in the span of past five years (2018–2022) …

Synopsis of some recent tactical application of bioisosteres in drug design

NA Meanwell - Journal of medicinal chemistry, 2011 - ACS Publications
The concept of isosterism between relatively simple chemical entities was originally
contemplated by James Moir in 1909, a notion further refined by HG Grimm's hydride …

From 2000 to mid-2010: A fruitful decade for the synthesis of pyrazoles

S Fustero, M Sánchez-Roselló, P Barrio… - Chemical …, 2011 - ACS Publications
In the past decade, interest in pyrazole chemistry has significatively increased mainly due to
the discovery of the interesting properties exhibited by a great number of pyrazole …

Plasma protein binding: from discovery to development

T Bohnert, LS Gan - Journal of pharmaceutical sciences, 2013 - Elsevier
The importance of plasma protein binding (PPB) in modulating the effective drug
concentration at pharmacological target sites has been the topic of significant discussion …

Insecticidal anthranilic diamides: a new class of potent ryanodine receptor activators

GP Lahm, TP Selby, JH Freudenberger… - Bioorganic & Medicinal …, 2005 - Elsevier
A novel class of anthranilic diamides has been discovered with exceptional insecticidal
activity on a range of Lepidoptera. These compounds have been found to exhibit their action …

A comprehensive listing of bioactivation pathways of organic functional groups

AS Kalgutkar, I Gardner, RS Obach… - Current drug …, 2005 - ingentaconnect.com
The occurrence of idiosyncratic adverse drug reactions during late clinical trials or after a
drug has been released can lead to a severe restriction in its use and even in its withdrawal …

Discovery of the Novel Antithrombotic Agent 5-Chloro-N-({(5S)-2-oxo-3- [4-(3-oxomorpholin-4-yl)phenyl]-1,3-oxazolidin-5-yl}methyl)thiophene- 2-carboxamide (BAY …

S Roehrig, A Straub, J Pohlmann… - Journal of medicinal …, 2005 - ACS Publications
Despite recent progress in antithrombotic therapy, there is still an unmet medical need for
safe and orally available anticoagulants. The coagulation enzyme Factor Xa (FXa) is a …

The pharmacological landscape and therapeutic potential of serine hydrolases

DA Bachovchin, BF Cravatt - Nature reviews Drug discovery, 2012 - nature.com
Serine hydrolases perform crucial roles in many biological processes, and several of these
enzymes are targets of approved drugs for indications such as type 2 diabetes, Alzheimer's …