The 1, 2, 3-triazole ring as a bioisostere in medicinal chemistry

E Bonandi, MS Christodoulou, G Fumagalli… - Drug Discovery …, 2017 - Elsevier
Highlights•Triazoles mimic different functional groups, resulting optimal bioisosteres for the
synthesis of new active molecules.•Triazoles present a marked stability under hydrolytic …

[HTML][HTML] Mechanisms of biotin-regulated gene expression in microbes

J Satiaputra, KE Shearwin, GW Booker… - Synthetic and systems …, 2016 - Elsevier
Biotin is an essential micronutrient that acts as a co-factor for biotin-dependent metabolic
enzymes. In bacteria, the supply of biotin can be achieved by de novo synthesis or import …

Identification of Putative Vaccine and Drug Targets against the Methicillin-Resistant Staphylococcus aureus by Reverse Vaccinology and Subtractive Genomics …

RS Naorem, BD Pangabam, SS Bora, G Goswami… - Molecules, 2022 - mdpi.com
Methicillin-resistant Staphylococcus aureus (MRSA) is an opportunistic pathogen and
responsible for causing life-threatening infections. The emergence of hypervirulent and …

Antibacterial silver and gold complexes of imidazole and 1, 2, 4-triazole derived N-heterocyclic carbenes

JC Mather, JA Wyllie, A Hamilton, TPS da Costa… - Dalton …, 2022 - pubs.rsc.org
A series of gold (I)(4a–4h, 5a–5b) and silver (I)(3a–3h) complexes of 1, 2, 4-triazolylidene
and imidazolylidene based N-heterocyclic carbene ligands were prepared and the …

Towards novel herbicide modes of action by inhibiting lysine biosynthesis in plants

TPS da Costa, CJ Hall, S Panjikar, JA Wyllie… - Elife, 2021 - elifesciences.org
Weeds are becoming increasingly resistant to our current herbicides, posing a significant
threat to agricultural production. Therefore, new herbicides with novel modes of action are …

Synthesis, antimicrobial activity and molecular docking studies of spiroquinoline-indoline-dione and spiropyrazolo-indoline-dione derivatives

M Gul, E Turk Celikoglu, O Idil, G Tas, E Pelit - Scientific Reports, 2023 - nature.com
Abstract Spiro [benzo [h] quinoline-7, 3′-indoline] diones and spiro [indoline-3, 4′-
pyrazolo [3, 4-b] quinoline] diones were efficiently synthesized via one-pot multi-component …

Synthesis, antimicrobial activity and in-silico docking of two macrocycles based on pyrazole-tetrazole subunit

M Cherfi, T Harit, MI Yahyaoui, A Riahi… - Journal of Molecular …, 2022 - Elsevier
The design of two new macrocycles bearing two pyrazole-tetrazole subunits and a lateral
arm is presented. These macrocycles and the intermediate compounds are characterized by …

Synthesis of novel tetrazolic derivatives and evaluation of their antimicrobial activity

C Bourhou, H Benouda, R Bellaouchi… - Journal of Molecular …, 2023 - Elsevier
The microbial resistance to various anti-infective drugs remains a major worldwide health
problem. Therefore, the search for novel and effective antimicrobial agents is of paramount …

Kinetic target-guided synthesis in drug discovery and chemical biology: a comprehensive facts and figures survey

D Bosc, J Jakhlal, B Deprez… - Future Medicinal …, 2016 - Taylor & Francis
For the last 15 years, kinetic target-guided syntheses, including in situ click chemistry, have
been used as alternative methods to find ligands to therapeutically relevant proteins. In this …

Repurposed inhibitor of bacterial dihydrodipicolinate reductase exhibits effective herbicidal activity

ERR Mackie, AS Barrow, MC Giel, MD Hulett… - Communications …, 2023 - nature.com
Herbicide resistance represents one of the biggest threats to our natural environment and
agricultural sector. Thus, new herbicides are urgently needed to tackle the rise in herbicide …