Emerging heterocycles as bioactive compounds

G Li Petri, R Holl, V Spanò, M Barreca, I Sardo… - Frontiers in …, 2023 - frontiersin.org
The design and development of a drug is a very long process that generally takes many
years of research. The laborious and expensive drug development pipeline, still …

Quinazoline: An update on current status against convulsions

RS Cheke, SD Shinde, JP Ambhore… - Journal of Molecular …, 2022 - Elsevier
Epilepsy is one of the most frequent chronic neurological disorder extremely threatening the
life and good health. More than 70 million individuals suffering from epilepsy worldwide and …

[HTML][HTML] The pyrazolo [4, 3-c] pyrazole core as a novel and versatile scaffold for developing dual DYRK1A-CLK1 inhibitors targeting key processes of Alzheimer's …

VA Bakalakou, B Mavroidi, AD Kalampaliki… - European Journal of …, 2024 - Elsevier
In the current study, we designed, synthesized, and characterized a series of substituted
pyrazolo [4, 3-c] pyrazoles. These novel compounds were evaluated in vitro for their …

2-Oxabicyclo [2.2. 2] octane as a new bioisostere of the phenyl ring

VV Levterov, Y Panasiuk, K Sahun… - Nature …, 2023 - nature.com
The phenyl ring is a basic structural element in chemistry. Here, we show the design,
synthesis, and validation of its new saturated bioisostere with improved physicochemical …

Pyrimidine: An elite heterocyclic leitmotif in drug discovery‐synthesis and biological activity

S Nadar, T Khan - Chemical Biology & Drug Design, 2022 - Wiley Online Library
Heterocyclic compounds bearing the pyrimidine core are of tremendous interest as they
constitute an important class of natural and synthetic compounds exhibiting diverse useful …

Insights on Cancer Cell Inhibition, Subcellular Activities, and Kinase Profile of Phenylacetamides Pending 1H-Imidazol-5-One Variants

MT Khayat, AM Omar, F Ahmed, MI Khan… - Frontiers in …, 2022 - frontiersin.org
Structural changes of small-molecule drugs may bring interesting biological properties,
especially in the field of kinase inhibitors. We sought to study tirbanibulin, a first-in-class dual …

Natural isoquinoline alkaloids: Pharmacological features and multi-target potential for complex diseases

E Plazas, DR Muñoz - Pharmacological Research, 2022 - Elsevier
Complex diseases such as neurodegenerative disorders and cancer constitute a growing
public health problem due to the rising incidence and lack in effective therapies. Since …

Target discovery of acivicin in cancer cells elucidates its mechanism of growth inhibition

J Kreuzer, NC Bach, D Forler, SA Sieber - Chemical science, 2015 - pubs.rsc.org
Acivicin is a natural product with diverse biological activities. Several decades ago its
clinical application in cancer treatment was explored but failed due to unacceptable toxicity …

Pharmacophore-based synthesis of pyrazole analogues as artificial antibiotics targeting Salmonella Typhi

H Muniyasamy, MK Aravind, M Arunkumar… - Journal of Molecular …, 2024 - Elsevier
The pharmacological potential of the pyrazole moiety is demonstrated by their presence in a
wide range of therapeutic agents spanning various categories. Notable examples include …

Pyrazolone structural motif in medicinal chemistry: Retrospect and prospect

Z Zhao, X Dai, C Li, X Wang, J Tian, Y Feng… - European journal of …, 2020 - Elsevier
The pyrazolone structural motif is a critical element of drugs aimed at different biological end-
points. Medicinal chemistry researches have synthesized drug-like pyrazolone candidates …