The 1, 2, 3-triazole 'all-in-one'ring system in drug discovery: A good bioisostere, a good pharmacophore, a good linker, and a versatile synthetic tool

D Lengerli, K Ibis, Y Nural… - Expert opinion on drug …, 2022 - Taylor & Francis
ABSTRACT Introduction The 1, 2, 3-triazole ring occupies an important space in medicinal
chemistry due to its unique structural properties, synthetic versatility and pharmacological …

1, 2, 3-Triazoles as biomimetics in peptide science

N Agouram, EM El Hadrami, A Bentama - Molecules, 2021 - mdpi.com
Natural peptides are an important class of chemical mediators, essential for most vital
processes. What limits the potential of the use of peptides as drugs is their low bioavailability …

Design and synthesis of new 1, 4, 5-trisubstituted triazole-bearing benzenesulphonamide moiety as selective COX-2 inhibitors

MS Bekheit, HA Mohamed, BF Abdel-Wahab… - Medicinal Chemistry …, 2021 - Springer
Abstract A new series of 1, 4, 5-trisubstituted triazole-bearing benzenesulphonamide moiety,
COX-2 pharmacophore, was designed and synthesized. The synthetic pathway for …

Synthesis and antibacterial activity of benzothiazole and benzoxazole-appended substituted 1, 2, 3-triazoles

CP Kaushik, M Chahal - Journal of Chemical Sciences, 2020 - Springer
A series of benzothiazole and benzoxazole linked 1, 4-disubstituted 1, 2, 3-triazoles was
synthesized through copper (I) catalyzed azide-alkyne cycloaddition reaction. FTIR, 1 H, 13 …

Exploring acetaminophen prodrugs and hybrids: a review

VV Kouznetsov - RSC advances, 2024 - pubs.rsc.org
This critical review highlights the advances in developing new molecules for treating pain
syndrome, an important issue for human health. Acetaminophen (APAP, known as …

Average Electron Density: A Quantitative Tool for Evaluating Non-Classical Bioisosteres of Amides

AMA Osman, AA Arabi - ACS omega, 2024 - ACS Publications
Bioisosterism is strategically used in drug design to enhance the pharmacokinetic and
pharmacodynamic properties of therapeutic molecules. The average electron density (AED) …

Synthesis and Characterization of New Functionalized 1, 2, 3-Triazole-Based Acetaminophen Derivatives via Click Chemistry from Expired Commercial …

VV Kouznetsov, D Calderón Lamus, CE Puerto Galvis - Reactions, 2023 - mdpi.com
We hereby describe an efficient method for the preparation of a series of new 1-substituted
1, 2, 3-triazole-based acetaminophen derivatives through a clean, good-yielding, simple …

Transcriptomic signature, bioactivity and safety of a non-hepatotoxic analgesic generating AM404 in the midbrain PAG region

HA Bazan, S Bhattacharjee, MM Reid, B Jun, C Polk… - Scientific Reports, 2024 - nature.com
Safe and effective pain management is a critical healthcare and societal need. The potential
for acute liver injury from paracetamol (ApAP) overdose; nephrotoxicity and gastrointestinal …

Bioisosteric Replacement through 1, 2, 3-triazolyl Linkage Significantly Potentiate Biological Activity in Lidocaine and Etidocaine Analogs: Rational Design and Local …

A Sahu, RK Agrawal - Current Organic Chemistry, 2023 - ingentaconnect.com
Cytochrome P450 3A4, the most abundant form of isoenzyme, in combination with several
other isoforms, metabolizes lignocaine into mono-ethylglycine xylidide (MEGX) and …

Antimalarial and antibacterial activities of ether linked 1, 4-disubstituted 1, 2, 3-triazoles.

R Luxmi, CP Kaushik - Chemistry & Biology Interface, 2020 - search.ebscohost.com
A series of twenty seven ether linked 1, 4-disubstituted 1, 2, 3-triazoles was assessed for in
vitro antimalarial activity against Plasmodium falciparum, while antibacterial activity against …