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 …

The application of prodrugs as a tool to enhance the properties of nucleoside reverse transcriptase inhibitors

LR Fernandes, JR Lopes, AF Bonjorno, JLB Prates… - Viruses, 2023 - mdpi.com
Antiretroviral Therapy (ART) is an effective treatment for human immunodeficiency virus
(HIV) which has transformed the highly lethal disease, acquired immunodeficiency …

Regioselective Ni-Catalyzed reductive alkylsilylation of acrylonitrile with unactivated alkyl bromides and chlorosilanes

J Sun, Y Zhou, R Gu, X Li, A Liu, X Zhang - Nature Communications, 2022 - nature.com
Transition-metal catalyzed carbosilylation of alkenes using carbon electrophiles and
silylmetal (-B,-Zn) reagents as the nucleophiles offers a powerful strategy for synthesizing …

Development of a Dihydroquinoline–Pyrazoline GluN2C/2D-Selective Negative Allosteric Modulator of the N-Methyl-d-aspartate Receptor

MP D'Erasmo, NS Akins, P Ma, Y Jing… - ACS Chemical …, 2023 - ACS Publications
Subunit-selective inhibition of N-methyl-d-aspartate receptors (NMDARs) is a promising
therapeutic strategy for several neurological disorders, including epilepsy, Alzheimer's and …

An O-Benzyl Phosphonamidate Prodrug of Tenofovir for the Treatment of Hepatitis B Virus Infection

Q Zhang, Y Peng, J Hou, Y Chen, B Liu… - Journal of Medicinal …, 2022 - ACS Publications
A series of new O-(substituted benzyl) phosphoramidate prodrugs of tenofovir for the
treatment of hepatitis B virus (HBV) infections have been designed and synthesized. An …

Prodrugs of a 1-Hydroxy-2-oxopiperidin-3-yl Phosphonate Enolase Inhibitor for the Treatment of ENO1-Deleted Cancers

VC Yan, CD Pham, ES Ballato, KL Yang… - Journal of Medicinal …, 2022 - ACS Publications
Cancers harboring homozygous deletion of the glycolytic enzyme enolase 1 (ENO1) are
selectively vulnerable to inhibition of the paralogous isoform, enolase 2 (ENO2). A previous …

Building Metabolically Stable and Potent Anti-HIV Thioether-Lipid Analogues of Tenofovir Exalidex: A thorough Pharmacological Analysis

MP D'Erasmo, SK Sharma, N Pribut… - Journal of Medicinal …, 2024 - ACS Publications
Inherently limited by poor bioavailability, antiviral agent tenofovir (TFV) is administered to
people living with HIV in prodrug form. However, current prodrugs are prematurely …

Expanding the toolbox of metabolically stable lipid prodrug strategies

KS Toti, N Pribut, M D'Erasmo, M Dasari… - Frontiers in …, 2023 - frontiersin.org
Nucleoside-and nucleotide-based therapeutics are indispensable treatment options for
patients suffering from malignant and viral diseases. These agents are most commonly …

Comparative pharmacology of a bis-pivaloyloxymethyl phosphonate prodrug inhibitor of enolase after oral and parenteral administration

VC Yan, Y Barekatain, YH Lin, N Satani… - ACS Pharmacology & …, 2023 - ACS Publications
Metabolically labile prodrugs can experience stark differences in catabolism incurred by the
chosen route of administration. This is especially true for phosph (on) ate prodrugs, in which …

Lipid-conjugated nucleoside monophosphate and monophosphonate prodrugs: a versatile drug delivery paradigm

Y Zhang, C Fan, J Zhang, X Tian, W Zuo… - European Journal of …, 2024 - Elsevier
Integrating lipid conjugation strategies into the design of nucleoside monophosphate and
monophosphonate prodrugs is a well-established approach for discovering potential …