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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 …
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 …
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 …
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 …
soluble drug candidates necessitating novel formulation technologies to provide dosage …
Alkaline phosphatase: a reliable endogenous partner for drug delivery and diagnostics
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 …
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 …
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 …
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
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 …
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 …
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 …
multidrug-resistant tuberculosis (MDR-TB). The mycobacterial enoyl reductase InhA is one …