ADMET profiling in drug discovery and development: perspectives of in silico, in vitro and integrated approaches

NEH Daoud, P Borah, PK Deb… - Current Drug …, 2021 - ingentaconnect.com
In the drug discovery setting, undesirable ADMET properties of a pharmacophore with good
predictive power obtained after a tedious drug discovery and development process may …

Thiazole derivatives in medicinal chemistry: Recent advancements in synthetic strategies, structure activity relationship and pharmacological outcomes

A Singh, D Malhotra, K Singh, R Chadha… - Journal of Molecular …, 2022 - Elsevier
Thiazole derivatives remains honored heterocycles in the field of medicinal chemistry. This
scaffold has been proven as a universal motif that is present in numerous pharmacologically …

Pyrazolo-benzothiazole hybrids: Synthesis, anticancer properties and evaluation of antiangiogenic activity using in vitro VEGFR-2 kinase and in vivo transgenic …

VG Reddy, TS Reddy, C Jadala, MS Reddy… - European journal of …, 2019 - Elsevier
A series of new pyrazolo-benzothiazole hybrids (7–26) were synthesised and screened for
their cytotoxic activity towards several cancer cell lines [colon (HT-29), prostate (PC-3), lung …

Comparison of the interactions of fanetizole with pepsin and trypsin: Spectroscopic and molecular docking approach

Y Yue, Q Tu, Y Guo, Y Wang, Y Xu, Y Zhang… - Journal of Molecular …, 2022 - Elsevier
In this work, the binding affinity of fanetizole with proteases pepsin and trypsin were
investigated by spectroscopy and molecular docking. As a thiazole derivative, the …

A synergistic investigation of azo-thiazole derivatives incorporating thiazole moieties: a comprehensive exploration of their synthesis, characterization, computational …

DM Aziz, SA Hassan, AAM Amin, K Qurbani, SB Aziz - RSC advances, 2023 - pubs.rsc.org
In the present study, a novel series of azo-thiazole derivatives (3a–c) containing a thiazole
moiety was successfully synthesized. The structure of these derivatives was examined by …

Design, synthesis, biological evaluation, QSAR analysis and molecular modelling of new thiazol-benzimidazoles as EGFR inhibitors

AM Srour, NS Ahmed, SS Abd El-Karim… - Bioorganic & Medicinal …, 2020 - Elsevier
Heterocyclic rings such as thiazole and benzimidazole are considered as privileged
structures, since they constitute several FDA-approved drugs for cancer treatment. In this …

Recent advances of thiazole hybrids in biological applications

M Gümüş, M Yakan, İ Koca - Future Medicinal Chemistry, 2019 - Taylor & Francis
Thiazoles have attracted much synthetic interest due to their wide variety of biological
properties and are important members of heterocyclic compounds. In recent years, studies …

Importance of fluorine in benzazole compounds

T Al-Harthy, W Zoghaib, R Abdel-Jalil - Molecules, 2020 - mdpi.com
Fluorine-containing heterocycles continue to receive considerable attention due to their
unique properties. In medicinal chemistry, the incorporation of fluorine in small molecules …

[HTML][HTML] Thiazole ring-the antimicrobial, anti-inflammatory, and anticancer active scaffold

S Hosseininezhad, A Ramazani - Arabian Journal of Chemistry, 2023 - Elsevier
Background Thiazole ring is one of the most important heterocycle scaffolds in organic and
medicinal chemistry due to this scaffold being the backbone of numerous drugs and their …

Synthesis and biological evaluation of novel benzothiazole derivatives as potential anticonvulsant agents

DC Liu, HJ Zhang, CM Jin, ZS Quan - Molecules, 2016 - mdpi.com
New benztriazoles with a mercapto-triazole and other heterocycle substituents were
synthesized and evaluated for their anticonvulsant activity and neurotoxicity by using the …