The expanding role of prodrugs in contemporary drug design and development

J Rautio, NA Meanwell, L Di… - Nature reviews drug …, 2018 - nature.com
Prodrugs are molecules with little or no pharmacological activity that are converted to the
active parent drug in vivo by enzymatic or chemical reactions or by a combination of the two …

Prodrugs: design and clinical applications

J Rautio, H Kumpulainen, T Heimbach… - Nature reviews Drug …, 2008 - nature.com
Prodrugs are bioreversible derivatives of drug molecules that undergo an enzymatic and/or
chemical transformation in vivo to release the active parent drug, which can then exert the …

Phosphine Oxides from a Medicinal Chemist's Perspective: Physicochemical and in Vitro Parameters Relevant for Drug Discovery

P Finkbeiner, JP Hehn, C Gnamm - Journal of Medicinal …, 2020 - ACS Publications
Phosphine oxides and related phosphorus-containing functional groups such as
phosphonates and phosphinates are established structural motifs that are still …

Supersaturating drug delivery systems: the answer to solubility-limited oral bioavailability?

J Brouwers, ME Brewster, P Augustijns - Journal of pharmaceutical …, 2009 - Elsevier
Contemporary pharmaceutical pipelines are often highly populated with poorly water-
soluble drug candidates necessitating novel formulation technologies to provide dosage …

Alkaline phosphatase: a reliable endogenous partner for drug delivery and diagnostics

B Le‐Vinh, ZB Akkuş‐Dağdeviren… - Advanced …, 2022 - Wiley Online Library
Since the 1960s the membrane‐bound enzyme alkaline phosphatase (ALP) has been
utilized in drug delivery. As it cleaves phosphate substructures from drugs, auxiliary agents …

Prodrug strategies to overcome poor water solubility

VJ Stella, KW Nti-Addae - Advanced drug delivery reviews, 2007 - Elsevier
Drug design in recent years has attempted to explore new chemical spaces resulting in
more complex, larger molecular weight molecules, often with limited water solubility. To …

Inhibitors of HIV-1 attachment: the discovery and development of temsavir and its prodrug fostemsavir

NA Meanwell, MR Krystal, B Nowicka-Sans… - 2018 - ACS Publications
Human immunodeficiency virus-1 (HIV-1) infection currently requires lifelong therapy with
drugs that are used in combination to control viremia. The indole-3-glyoxamide 6 was …

Bioinert, stealth or interactive: how surface chemistry of nanocarriers determines their fate in vivo

JD Friedl, V Nele, G De Rosa… - Advanced functional …, 2021 - Wiley Online Library
Nanocarriers (NCs) have emerged as powerful tools to improve drug solubility, to promote
drug transport across membranes, to protect their payload from premature degradation, and …

Geminal diheteroatomic motifs: some applications of acetals, ketals, and their sulfur and nitrogen homologues in medicinal chemistry and drug design

YJ Wu, NA Meanwell - Journal of Medicinal Chemistry, 2021 - ACS Publications
Acetals and ketals and their nitrogen and sulfur homologues are often considered to be
unconventional and potentially problematic scaffolding elements or pharmacophores for the …

Direct inhibitors of InhA are active against Mycobacterium tuberculosis

UH Manjunatha, SP S. Rao, RR Kondreddi… - Science translational …, 2015 - science.org
New chemotherapeutic agents are urgently required to combat the global spread of
multidrug-resistant tuberculosis (MDR-TB). The mycobacterial enoyl reductase InhA is one …