From DC18 to MR07: A Metabolically Stable 4,4′‐Oxybisbenzoyl Amide as a Low‐Nanomolar Growth Inhibitor of P. falciparum
Sign Up to like & getrecommendations! Published in 2022 at "Chemmedchem"
DOI: 10.1002/cmdc.202200355
Abstract: To improve the metabolic stability of a 4,4′‐oxybisbenzoyl‐based novel and potent (nanomolar‐range IC50) antiplasmodial agent previously described by us, in silico‐guided structure‐activity relationship (SAR) campaigns have been conducted to substitute its peptide decorations with more… read more here.
Keywords: oxybisbenzoyl amide; metabolically stable; mr07 metabolically; dc18 mr07 ... See more keywords
Discovery of NLX-266, an Orally Available and Metabolically Stable ERK1/2-Biased 5-HT1AR Agonist with Superior Antidepressant and Antiparkinsonian Activity
Sign Up to like & getrecommendations! Published in 2025 at "Journal of Medicinal Chemistry"
DOI: 10.1021/acs.jmedchem.5c00484
Abstract: We report the discovery of NLX-266 (31), an orally available and metabolically stable ERK1/2-biased 5-HT1A receptor agonist, which demonstrates both enhanced antidepressant and antiparkinsonian-like activities. A new series of 1-(1-benzoylpiperidin-4-yl)methanamine derivatives were synthesized and screened… read more here.
Keywords: 266 orally; orally available; available metabolically; nlx 266 ... See more keywords
A metabolically stable apelin-17 analog decreases AVP-induced antidiuresis and improves hyponatremia
Sign Up to like & getrecommendations! Published in 2021 at "Nature Communications"
DOI: 10.1038/s41467-020-20560-y
Abstract: Apelin and arginine-vasopressin (AVP) are conversely regulated by osmotic stimuli. We therefore hypothesized that activating the apelin receptor (apelin-R) with LIT01-196, a metabolically stable apelin-17 analog, may be beneficial for treating the Syndrome of Inappropriate… read more here.
Keywords: stable apelin; apelin analog; apelin; metabolically stable ... See more keywords
Expanding the toolbox of metabolically stable lipid prodrug strategies
Sign Up to like & getrecommendations! Published in 2023 at "Frontiers in Pharmacology"
DOI: 10.3389/fphar.2022.1083284
Abstract: Nucleoside- and nucleotide-based therapeutics are indispensable treatment options for patients suffering from malignant and viral diseases. These agents are most commonly administered to patients as prodrugs to maximize bioavailability and efficacy. While the literature provides… read more here.
Keywords: toolbox metabolically; expanding toolbox; metabolically stable; prodrug ... See more keywords
Toward Structurally Novel and Metabolically Stable HIV-1 Capsid-Targeting Small Molecules
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DOI: 10.3390/v12040452
Abstract: HIV-1 capsid protein (CA) plays an important role in many steps of viral replication and represents an appealing antiviral target. Several CA-targeting small molecules of various chemotypes have been studied, but the peptidomimetic PF74 has… read more here.
Keywords: structurally novel; novel metabolically; metabolically stable; hiv capsid ... See more keywords