The necessary nitrogen atom: a versatile high-impact design element for multiparameter optimization

LD Pennington, DT Moustakas - Journal of Medicinal Chemistry, 2017 - ACS Publications
There is a continued desire in biomedical research to reduce the number and duration of
design cycles required to optimize lead compounds into high-quality chemical probes or …

Practical strategies and concepts in GPCR allosteric modulator discovery: recent advances with metabotropic glutamate receptors

CW Lindsley, KA Emmitte, CR Hopkins… - Chemical …, 2016 - ACS Publications
Allosteric modulation of GPCRs has initiated a new era of basic and translational discovery,
filled with therapeutic promise yet fraught with caveats. Allosteric ligands stabilize unique …

Leveraging language model for advanced multiproperty molecular optimization via prompt engineering

Z Wu, O Zhang, X Wang, L Fu, H Zhao… - Nature Machine …, 2024 - nature.com
Optimizing a candidate molecule's physiochemical and functional properties has been a
critical task in drug and material design. Although the non-trivial task of balancing multiple …

Electrochemical synthesis of 1, 2, 4-triazole-fused heterocycles

Z Ye, M Ding, Y Wu, Y Li, W Hua, F Zhang - Green chemistry, 2018 - pubs.rsc.org
A reagent-free intramolecular dehydrogenative C–N cross-coupling reaction has been
developed under mild electrolytic conditions. In this atom-and step-economical one-pot …

International union of basic and clinical pharmacology. CXI. Pharmacology, signaling, and physiology of metabotropic glutamate receptors

KJ Gregory, C Goudet, EH Ohlstein - Pharmacological reviews, 2021 - Elsevier
Metabotropic glutamate (mGlu) receptors respond to glutamate, the major excitatory
neurotransmitter in the mammalian brain, mediating a modulatory role that is critical for …

Synthesis, crystal structure, herbicidal activities and 3D‐QSAR study of some novel 1,2,4‐triazolo[4,3‐a]pyridine derivatives

XH Liu, XY Xu, CX Tan, JQ Weng… - Pest Management …, 2015 - Wiley Online Library
Abstract BACKGROUND 1, 2, 4‐Triazolo [4, 3‐a] pyridine derivatives represent a new series
of compounds that possess good herbicidal activity against Echinochloa crusgalli (L.) …

[HTML][HTML] Triazolopyridine, a leitmotif of synthetic methods and pharmacological attributes: an extensive review

P Mohite, D Nahar, R Pawara, T Alqahtani… - Arabian Journal of …, 2023 - Elsevier
Background Famous synthetic pharmacophores like Filgotinib, Dapiprazole, and Trazodone
have Triazolopyridine as their primary building element. It has become more well-known in …

Pyridines and Imidazopyridines with medicinal significance

T LS Kishbaugh - Current Topics in Medicinal Chemistry, 2016 - ingentaconnect.com
Pyridine and pyridine-fused ring systems are ubiquitous in medicinal research and
demonstrate such diverse pharmacological benefits as anticonvulsant therapies, treatment …

Visible‐Light‐Induced nickel‐catalyzed negishi cross‐couplings by exogenous‐photosensitizer‐free photocatalysis

I Abdiaj, A Fontana, MV Gomez… - Angewandte Chemie …, 2018 - Wiley Online Library
The merging of photoredox and transition‐metal catalysis has become one of the most
attractive approaches for carbon–carbon bond formation. Such reactions require the use of …

Scaffold-hopping as a strategy to address metabolic liabilities of aromatic compounds

PR Lazzara, TW Moore - RSC Medicinal Chemistry, 2020 - pubs.rsc.org
Understanding and minimizing oxidative metabolism of aromatic compounds is a key hurdle
in lead optimization. Metabolic processes not only clear compounds from the body, but they …