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Novel benzimidazole derivatives as effective inhibitors of prolyl oligopeptidase: synthesis, in vitro and in silico analysis
Novel benzimidazole derivatives as effective inhibitors of prolyl oligopeptidase: synthesis, in vitro and in silico analysis
Background: This research aims to discover novel derivatives having potential therapeutic applications in treating conditi...
In vitro cytotoxic investigation of some synthesized 1,6-disubstituted-1-azacoumarin derivatives as anticancer agents
In vitro cytotoxic investigation of some synthesized 1,6-disubstituted-1-azacoumarin derivatives as anticancer agents
Aims: In this study, novel synthesized 1,6-disubstituted-1-azacoumarin-3-carboxylic acid derivatives were designed, synthe...
New 3-amino-2-thioxothiazolidin-4-one-based inhibitors of acetyl- and butyryl-cholinesterase: synthesis and activity
New 3-amino-2-thioxothiazolidin-4-one-based inhibitors of acetyl- and butyryl-cholinesterase: synthesis and activity
Aim: 2-Thioxothiazolidin-4-one represents a versatile scaffold in drug development. The authors used it to prepare new pot...
Mucin glycosylation: a potential target for prostate cancer management
Mucin glycosylation: a potential target for prostate cancer management
The authors duly acknowledge the Research Grant from DST-SERB, India for supporting this work. P Prasher thanks DST-SERB f...
Kynomycin: a beacon of hope in the battle against antibiotic resistance
Kynomycin: a beacon of hope in the battle against antibiotic resistance
The authors have no financial involvement with any organization or entity with a financial interest in or financial confli...
Synthesis of 1,3,4-oxadiazoles with 4-methoxynaphthalene ring: discovering new compounds with antimicrobial activity
Synthesis of 1,3,4-oxadiazoles with 4-methoxynaphthalene ring: discovering new compounds with antimicrobial activity
Background: Paracoccidioidomycosis (PCM) is a systemic infection caused by Paracoccidioides spp. (Pb). PCM can be associat...
Novel amodiaquine analogues to treat cervical cancer and microbial infection in the future
Novel amodiaquine analogues to treat cervical cancer and microbial infection in the future
Aim: To synthesize and explore the therapeutic potential of amodiaquine analogues. Methodology: New promising analogues we...
Synthesis, biological evaluation and in silico studies of some new analogues of 3,5-disubstituted thiazolidin-2,4-dione
Synthesis, biological evaluation and in silico studies of some new analogues of 3,5-disubstituted thiazolidin-2,4-dione
Background: A new series of 3,5-disubstituted thiazolidin-2,4-dione molecules were derived and characterized using various...
Hydrazone–sulfonate hybrids as potential cholinesterase inhibitors: design, synthesis and molecular modeling simulation
Hydrazone–sulfonate hybrids as potential cholinesterase inhibitors: design, synthesis and molecular modeling simulation
Aim: Design and synthesis of a series of hydrazone–sulfonate hybrids, 5a–r. Methodology: The inhibitory properties of the ...
Norfloxacin derivatives as DNA gyrase and urease inhibitors: synthesis, biological evaluation and molecular docking
Norfloxacin derivatives as DNA gyrase and urease inhibitors: synthesis, biological evaluation and molecular docking
Background: DNA gyrase and urease enzymes are important targets for the treatment of gastroenteritis, appendicitis, tuberc...
Polyhydroquinoline derivatives for diabetic management: synthesis, in vitro and in silico approaches
Polyhydroquinoline derivatives for diabetic management: synthesis, in vitro and in silico approaches
Background: Medication used to treat Type 2 diabetes by decreasing the absorption of carbohydrates in the intestine consis...
Design and synthesis of novel pyrazolopyrimidine candidates as promising EGFR-T790M inhibitors and apoptosis inducers
Design and synthesis of novel pyrazolopyrimidine candidates as promising EGFR-T790M inhibitors and apoptosis inducers
Aim: Our objective was to design and synthesize a new range of pyrazolopyrimidines while maintaining the key pharmacophori...
Erlotinib-containing benzenesulfonamides as anti-Helicobacter pylori agents through carbonic anhydrase inhibition
Erlotinib-containing benzenesulfonamides as anti-Helicobacter pylori agents through carbonic anhydrase inhibition
Aim: Development of dual-acting antibacterial agents containing Erlotinib, a recognized EGFR inhibitor used as an anticanc...
Antimicrobial potential of quaternary phosphonium salt compounds: a review
Antimicrobial potential of quaternary phosphonium salt compounds: a review
Given that mitochondrial dysregulation is a biomarker of many cancers, cationic quaternary phosphonium salt (QPS) conjugat...
Sulfonic acid: key drug design elements with potent, broad-ranging pharmacological activities
Sulfonic acid: key drug design elements with potent, broad-ranging pharmacological activities
*Author for correspondence: E-mail Address: liuchuanfeng214@163.comDepartment of Medicinal Chemistry, Key Laboratory of Ch...
Treatment of rheumatoid arthritis with curcumin analog 3,5-bis(arylidene)-4-piperidone
Treatment of rheumatoid arthritis with curcumin analog 3,5-bis(arylidene)-4-piperidone
Rheumatoid arthritis (RA) is an inflammatory disease. Curcumin can inhibit NF-κB and reduce the expression of inflammation...
Unveiling innovative anti-influenza agents through modern medicinal chemistry approaches (2019–2023 updates)
Unveiling innovative anti-influenza agents through modern medicinal chemistry approaches (2019–2023 updates)
Department of Medicinal Chemistry, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sc...
Indole–pyridine carbonitriles: multicomponent reaction synthesis and bio-evaluation as potential hits against diabetes mellitus
Indole–pyridine carbonitriles: multicomponent reaction synthesis and bio-evaluation as potential hits against diabetes mellitus
Background: Diabetes mellitus is a significant health disorder; therefore, researchers should focus on discovering new dru...
Biological and computational investigation of transition metal(II) complexes of 2-phenoxyaniline-based ligands
Biological and computational investigation of transition metal(II) complexes of 2-phenoxyaniline-based ligands
Aim: In the 21st century, we are witness of continuous onslaughts of various pathogen deformities which are a major cause ...
G-quadruplex ligands as therapeutic agents against cancer, neurological disorders and viral infections
G-quadruplex ligands as therapeutic agents against cancer, neurological disorders and viral infections
G-quadruplexes (G4s) within the human genome have undergone extensive molecular investigation, with a strong focus on telo...
Pyrazole: an emerging privileged scaffold in drug discovery
Pyrazole: an emerging privileged scaffold in drug discovery
Pyrazole or 1H-pyrazole, a five-membered 1,2-diazole, is found in several approved drugs and some bioactive natural produc...
Chemical and biological versatility of pyrazolo[3,4-d]pyrimidines: one scaffold, multiple modes of action
Chemical and biological versatility of pyrazolo[3,4-d]pyrimidines: one scaffold, multiple modes of action
Plain language summary Pyrazolo[3,4-d]pyrimidines are chemical compounds possessing remarkable versatility and significanc...
Artificial intelligence-guided approach for efficient virtual screening of hits against Schistosoma mansoni
Artificial intelligence-guided approach for efficient virtual screening of hits against Schistosoma mansoni
Background: The impact of schistosomiasis, which affects over 230 million people, emphasizes the urgency of developing new...
Design, synthesis and bioevaluation of novel trifluoromethylquinoline derivatives as tubulin polymerization inhibitors
Design, synthesis and bioevaluation of novel trifluoromethylquinoline derivatives as tubulin polymerization inhibitors
Aim: A series of novel trifluoromethylquinoline derivatives were designed, synthesized and evaluated for antitumor activit...
Discovery of new VEGFR-2 inhibitors and apoptosis inducer-based thieno[2,3-d]pyrimidine
Discovery of new VEGFR-2 inhibitors and apoptosis inducer-based thieno[2,3-d]pyrimidine
Background: VEGFR-2 is a key regulator of cancer cell proliferation, migration and angiogenesis. Aim: Development of thien...
Virtual screening approach for the discovery of selective 5α-reductase type II inhibitors for benign prostatic hyperplasia treatment
Virtual screening approach for the discovery of selective 5α-reductase type II inhibitors for benign prostatic hyperplasia treatment
Background: 5α-Reductase type II (5αR2) inhibition is a promising strategy for benign prostatic hyperplasia treatment. A c...
New horizons in lung cancer management through ATR/CHK1 pathway modulation
New horizons in lung cancer management through ATR/CHK1 pathway modulation
Lung cancer is the leading cause of cancer-related deaths worldwide. Molecular profiling has contributed to a new classifi...
N-Pyrazinylhydroxybenzamides as biologically active compounds: a hit-expansion study and antimicrobial evaluation
N-Pyrazinylhydroxybenzamides as biologically active compounds: a hit-expansion study and antimicrobial evaluation
Background: The development of novel antimicrobial drugs is an essential part of combatting the uprising of antimicrobial ...