Synthesis and biological evaluation of new 2-(6-alkyl-pyrazin-2-yl)-1H-benz[d]imidazoles as potent anti-inflammatory and antioxidant agents
Sign Up to like & getrecommendations! Published in 2017 at "Medicinal Chemistry Research"
DOI: 10.1007/s00044-017-1897-7
Abstract: A novel series of 2-(6-alkyl-pyrazin-2-yl)-1H-benzo[d]imidazole analogs (3a–3j) derived from 2-(6-chloropyrazin-2-yl)-1H-benzo[d]imidazole (2) by reacting with various substituted cyclic and acyclic secondary amines in presence of Pd-PEPPSI Mes catalyst by using Buchwald–Hartwig amination in excellent yield. The… read more here.
Keywords: anti inflammatory; potent anti; alkyl pyrazin; inflammatory ... See more keywords
Unlocking potent anti-tuberculosis natural products through structure–activity relationship analysis
Sign Up to like & getrecommendations! Published in 2025 at "Natural Products and Bioprospecting"
DOI: 10.1007/s13659-025-00529-4
Abstract: Tuberculosis (TB) remains a world health problem due to the high number of affected individuals, high mortality rates, prolonged treatment durations, and the increasing prevalence of resistance to commercial TB drugs. The emergence of resistance… read more here.
Keywords: natural products; potent anti; structure activity; tuberculosis ... See more keywords
Exploring the cycloheptathiophene-3-carboxamide scaffold to disrupt the interactions of the influenza polymerase subunits and obtain potent anti-influenza activity.
Sign Up to like & getrecommendations! Published in 2017 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2017.06.015
Abstract: With the aim to identify small molecules able to disrupt PA-PB1 subunits interaction of influenza virus (flu) RNA-dependent RNA polymerase, and based on previous structural and computational information, in this paper we have designed and… read more here.
Keywords: carboxamide scaffold; potent anti; exploring cycloheptathiophene; scaffold disrupt ... See more keywords
Peptidomimetic plasmepsin inhibitors with potent anti-malarial activity and selectivity against cathepsin D
Sign Up to like & getrecommendations! Published in 2019 at "European Journal of Medicinal Chemistry"
DOI: 10.1016/j.ejmech.2018.11.068
Abstract: Following up the open initiative of anti-malarial drug discovery, a GlaxoSmithKline (GSK) phenotypic screening hit was developed to generate hydroxyethylamine based plasmepsin (Plm) inhibitors exhibiting growth inhibition of the malaria parasite Plasmodium falciparum at nanomolar… read more here.
Keywords: potent anti; malarial activity; anti malarial; plasmepsin ... See more keywords
Identification of tetragocarbone C and sideroxylin as the most potent anti-inflammatory components of Syncarpia glomulifera.
Sign Up to like & getrecommendations! Published in 2021 at "Fitoterapia"
DOI: 10.1016/j.fitote.2021.104843
Abstract: In contrast to ancient Western and Asian cultures, medicinal plants of the Aboriginal and Torres Strait Islanders in Australia have not been as intensively studied for their molecular composition and molecular bioactivity. Syncarpia glomulifera subsp.… read more here.
Keywords: anti inflammatory; syncarpia glomulifera; tetragocarbone sideroxylin; potent anti ... See more keywords
Discovery of 2-Ethynylisoborneol as a Highly Potent Anti-seizure Agent.
Sign Up to like & getrecommendations! Published in 2025 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.5c00821
Abstract: Epilepsy is a type of severe neurological disorder that is caused by abnormal neuronal discharges. Natural D-(+)-borneol has been proven to attenuate epileptic seizures, while its potency and pharmacokinetic profiles remain improved. In this study,… read more here.
Keywords: anti seizure; seizure agent; potent anti; highly potent ... See more keywords
Pyridobenzothiazolones Exert Potent Anti-Dengue Activity by Hampering Multiple Functions of NS5 Polymerase.
Sign Up to like & getrecommendations! Published in 2020 at "ACS medicinal chemistry letters"
DOI: 10.1021/acsmedchemlett.9b00619
Abstract: Treatment of dengue virus (DENV) and other flavivirus infections is an unmet medical need. The highly conserved flaviviral NS5 RNA-dependent RNA polymerase (RdRp) is an attractive antiviral target that interacts with NS3 and viral RNA… read more here.
Keywords: anti dengue; potent anti; exert potent; polymerase ... See more keywords
The nuclear factor ID3 endows macrophages with a potent anti-tumour activity
Sign Up to like & getrecommendations! Published in 2024 at "Nature"
DOI: 10.1038/s41586-023-06950-4
Abstract: Macrophage activation is controlled by a balance between activating and inhibitory receptors1–7, which protect normal tissues from excessive damage during infection8,9 but promote tumour growth and metastasis in cancer7,10. Here we report that the Kupffer… read more here.
Keywords: id3; tumour; potent anti; factor id3 ... See more keywords
High-throughput identification of repurposable neuroactive drugs with potent anti-glioblastoma activity
Sign Up to like & getrecommendations! Published in 2024 at "Nature Medicine"
DOI: 10.1038/s41591-024-03224-y
Abstract: Glioblastoma, the most aggressive primary brain cancer, has a dismal prognosis, yet systemic treatment is limited to DNA-alkylating chemotherapies. New therapeutic strategies may emerge from exploring neurodevelopmental and neurophysiological vulnerabilities of glioblastoma. To this end,… read more here.
Keywords: neuroactive drugs; repurposable neuroactive; drugs potent; potent anti ... See more keywords
Identification of novel furo[2,3-d]pyrimidine based chalcones as potent anti-breast cancer agents: synthesis, in vitro and in vivo biological evaluation
Sign Up to like & getrecommendations! Published in 2022 at "RSC Advances"
DOI: 10.1039/d2ra00889k
Abstract: Various substituted synthetic chalcones demonstrated potent anti-cancer activities. In the current study a series of novel furo[2,3-d]pyrimidine based chalcones were synthesized as potential anticancer agents. Among the different substituted derivatives, two of the halogen bearing… read more here.
Keywords: novel furo; based chalcones; potent anti; pyrimidine based ... See more keywords
Virus-like particle display of HER2 induces potent anti-cancer responses
Sign Up to like & getrecommendations! Published in 2018 at "Oncoimmunology"
DOI: 10.1080/2162402x.2017.1408749
Abstract: ABSTRACT Overexpression of human epidermal growth factor receptor-2 (HER2) occurs in 20–30% of invasive breast cancers. Monoclonal antibody therapy is effective in treating HER2-driven mammary carcinomas, but its utility is limited by high costs, side… read more here.
Keywords: like particle; potent anti; virus like; cancer ... See more keywords