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Discovery of novel pyrazole and pyrazolo[1,5-a]pyrimidine derivatives as cyclooxygenase inhibitors (COX-1 and COX-2) using molecular modeling simulation

期刊: ARCHIV DER PHARMAZIE, 2023; 356 (2)

Searching for effective and selective anti-inflammatory agents, our study involved designing and synthesizing new pyrazole and pyrazolo[1,5-a]pyrimidi......

1,2,4-Triazole and benzimidazole fused dihydropyrimidine derivatives: Design, green synthesis, antibacterial, antitubercular, and antimalarial activities

期刊: ARCHIV DER PHARMAZIE, 2023; 356 (4)

This study reports the design and synthesis of novel 1,2,4-triazolo/benzimidazolo-pyrimidine linked 1-benzyl-4-[(p-tolyloxy)methyl]-1,2,3-triazole der......

Zinc(II) complexation strategy for ultra-sensitive fluorimetric estimation of molnupiravir: Applications and greenness evaluation

期刊: ARCHIV DER PHARMAZIE, 2023; 356 (6)

The endemicity of the pandemic coronavirus disease 2019 (COVID-19) infection proved to be transitional only. Spikes are forming again in 2023, and hig......

Synthesis, computational and antimicrobial evaluation of some new pyridine derivatives

期刊: ARCHIV DER PHARMAZIE, 2023; 356 (3)

A series of pyridine compounds were prepared by using 3-(dimethylamino)-1-(pyridin-4-yl)prop-2-en-1-one (14) as a precursor. The reaction of 14 with d......

Design, synthesis, and biological evaluation of a potent PLK4 inhibitor WY29 with 1H-pyrazolo[3,4-d]pyrimidine scaffold

期刊: ARCHIV DER PHARMAZIE, 2023; 356 (3)

Centriole duplication occurs once per cell cycle and is regulated by Polo-like kinase 4 (PLK4). Overexpression of PLK4 in somatic cells can lead to th......

Design, synthesis, molecular docking, and biological evaluation of coumarin-thymidine analogs as potent anti-TB agents

期刊: ARCHIV DER PHARMAZIE, 2023; 356 (5)

With the intent to discover new antituberculosis (TB) compounds, coumarin-thymidine analogs were synthesized using second-order nucleophilic substitut......

Discovery of novel potent PI3K/mTOR dual-target inhibitors based on scaffold hopping: Design, synthesis, and antiproliferative activity

期刊: ARCHIV DER PHARMAZIE, 2023; 356 (12)

The PI3K/AKT/mTOR pathway is one of the most common dysregulated signaling cascade responses in human cancers, playing a crucial role in cell prolifer......

Inhibitory effects of 190 compounds against SARS-CoV-2 Mpro protein: Molecular docking interactions

期刊: ARCHIV DER PHARMAZIE, 2023; 356 (8)

COVID-19 has caused many deaths since the first outbreak in 2019. The burden on healthcare systems around the world has been reduced by the success of......

Targeting Mycobacterium tuberculosis: Synthesis, in vitro and in silico evaluation of novel N1-(benzo[d]oxazol-2-yl)-N4-arylidine compounds

期刊: ARCHIV DER PHARMAZIE, 2023; 356 (8)

The development of novel antimycobacterial agents is an urgent challenge to eradicate the increasing emergence and rapid spread of multidrug-resistant......

Melatonin-vorinostat hybrid ligands show higher histone deacetylase and cancer cell growth inhibition than vorinostat

期刊: ARCHIV DER PHARMAZIE, 2023; 356 (9)

Anticancer drug conjugates are an emerging approach for future cancer treatment. Here, we report a series of hybrid ligands merging the neurohormone m......

Development of 1-(2-aminophenyl)pyrrole-based amides acting as human topoisomerase I inhibitors

期刊: ARCHIV DER PHARMAZIE, 2023; 356 (10)

Topoisomerases are ubiquitous enzymes in the human body, particularly involved in cancer development and progression. Topoisomerase I (topoI) performs......

Synthesis, characterization, biochemical, and molecular modeling studies of carvacrol-based new thiosemicarbazide and 1,3,4-thiadiazole derivatives

期刊: ARCHIV DER PHARMAZIE, 2023; 356 (12)

A series of carvacrol-based thiosemicarbazide (3a-e) and 1,3,4-thiadiazole-2-amine (4a-e) were designed and synthesized for the first time. The struct......

Phthalimide-tethered isatins as novel poly(ADP-ribose) polymerase inhibitors: Design, synthesis, biological evaluations, and molecular modeling investigations

期刊: ARCHIV DER PHARMAZIE, 2023; ()

Humanity is currently facing various diseases with significant mortality rates, particularly those associated with malignancies. Numerous enzymes and ......

Tail approach synthesis of triazolylthiazolotriazole bearing benzenesulfonamides as carbonic anhydrase inhibitors capable of inducing apoptosis

期刊: ARCHIV DER PHARMAZIE, 2023; 356 (2)

Inhibition of human carbonic anhydrase (hCA) isoform IX with concurrent induction of apoptosis is a promising approach for targeting cancer in humans.......

Anticryptococcal activity and mechanistic studies of short amphipathic peptides

期刊: ARCHIV DER PHARMAZIE, 2023; 356 (4)

Cryptococcus neoformans, an opportunistic fungal pathogen, causes cryptococcosis in immunocompromised persons. A series of modified L-histidines-conta......

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