The emergence of the C–H functionalization strategy in medicinal chemistry and drug discovery

R Jana, HM Begam, E Dinda - Chemical Communications, 2021 - pubs.rsc.org
Owing to the market competitiveness and urgent societal need, an optimum speed of drug
discovery is an important criterion for successful implementation. Despite the rapid ascent of …

Structural alert/reactive metabolite concept as applied in medicinal chemistry to mitigate the risk of idiosyncratic drug toxicity: a perspective based on the critical …

AF Stepan, DP Walker, J Bauman… - Chemical research in …, 2011 - ACS Publications
Because of a preconceived notion that eliminating reactive metabolite (RM) formation with
new drug candidates could mitigate the risk of idiosyncratic drug toxicity, the potential for RM …

Magnetic chitosan-copper nanocomposite: A plant assembled catalyst for the synthesis of amino-and N-sulfonyl tetrazoles in eco-friendly media

N Motahharifar, M Nasrollahzadeh… - Carbohydrate …, 2020 - Elsevier
A greener, cost efficient and simple method is described to prepare copper nanoparticles
(NPs) immobilized on the magnetic chitosan (one of the more versatile polysaccharides) …

A systematic comparison of the properties of clinically used angiotensin II type 1 receptor antagonists

MC Michel, C Foster, HR Brunner, L Liu… - Pharmacological …, 2013 - Elsevier
Angiotensin II type 1 receptor antagonists (ARBs) have become an important drug class in
the treatment of hypertension and heart failure and the protection from diabetic nephropathy …

Bioactivation potential of thiophene-containing drugs

D Gramec, L Peterlin Mašič… - Chemical research in …, 2014 - ACS Publications
Thiophene is a five-membered, sulfur-containing heteroaromatic ring commonly used as a
building block in drugs. It is considered to be a structural alert, as its metabolism can lead to …

International Union of Basic and Clinical Pharmacology. XCIX. Angiotensin receptors: interpreters of pathophysiological angiotensinergic stimuli

SS Karnik, H Unal, JR Kemp, KC Tirupula… - Pharmacological …, 2015 - Elsevier
The renin angiotensin system (RAS) produced hormone peptides regulate many vital body
functions. Dysfunctional signaling by receptors for RAS peptides leads to pathologic states …

Repurposing old drugs to fight multidrug resistant cancers

J Dinić, T Efferth, AT García-Sosa, J Grahovac… - Drug Resistance …, 2020 - Elsevier
Overcoming multidrug resistance represents a major challenge for cancer treatment. In the
search for new chemotherapeutics to treat malignant diseases, drug repurposing gained a …

Late-stage azolation of benzylic C‒H bonds enabled by electrooxidation

Z Ruan, Z Huang, Z Xu, S Zeng, P Feng… - Science China Chemistry, 2021 - Springer
The installation of azoles via C–H/N–H cross-coupling is significantly underdeveloped,
particularly in benzylic C–H azolation due to the requirement for external chemical oxidants …

Genetic polymorphism of the human cytochrome P450 2C9 gene and its clinical significance

B Wang, J Wang, SQ Huang, HH Su… - Current drug …, 2009 - ingentaconnect.com
Human cytochrome P450 2C9 (CYP2C9) accounts for∼ 20% of total hepatic CYP content
and metabolizes∼ 15% clinically used drugs including S-warfarin, tolbutamide, phenytoin …

Role of pharmacologically active metabolites in drug discovery and development

A Fura - Drug discovery today, 2006 - Elsevier
Pharmacologically active metabolites can contribute significantly to the overall therapeutic
and adverse effects of drugs. Therefore, to fully understand the mechanism of action of …