A5077790644- Synthesis and biological activity
- Malaria Research and Control
- Computational Drug Discovery Methods
- Phenothiazines and Benzothiazines Synthesis and Activities
- Phytochemicals and Antioxidant Activities
- Parasites and Host Interactions
- Synthesis and Characterization of Heterocyclic Compounds
- Amoebic Infections and Treatments
- Essential Oils and Antimicrobial Activity
- Microbial Metabolism and Applications
- Genomics, phytochemicals, and oxidative stress
- Synthesis and Biological Evaluation
- Cancer therapeutics and mechanisms
- HIV/AIDS drug development and treatment
- Monoclonal and Polyclonal Antibodies Research
- HIV Research and Treatment
- Protein Interaction Studies and Fluorescence Analysis
- Helminth infection and control
- Click Chemistry and Applications
- Pharmaceutical and Antibiotic Environmental Impacts
- Parasitic Infections and Diagnostics
- Pharmacological Effects of Natural Compounds
- Multicomponent Synthesis of Heterocycles
- Diagnosis and treatment of tuberculosis
- Bioactive Compounds and Antitumor Agents
Jamia Millia Islamia
2010-2024
Microtubule affinity-regulating kinase 4 (MARK4) is a serine-threonine that phosphorylates microtubule-associated proteins (MAPs) and increases the microtubule dynamics. Due to its direct involvement in initiation, cell division, progression, cancer metastasis, MARK4 considered potential therapeutic target. Here, we designed, synthesized, characterized vanillin-isatin hybrids evaluated their inhibitory potential. All of compounds strongly bind interact closely with active site residues....
Methionine aminopeptidases (MetAPs) are attractive drug targets due to their essential role in eukaryotes as well prokaryotic cells. In this study, biochemical assays were performed on newly synthesized Isatin-pyrazole hydrazones (PS1–14) identify potent and selective bacterial MetAPs inhibitors. Compound PS9 inhibited MetAPs, i.e., MtMetAP1c, EfMetAP1a SpMetAP1a with Ki values of 0.31, 6.93 0.37 µM, respectively. Interestingly, the human analogue HsMetAP1b (631.7 µM) about ten thousand-fold...
The rapid emergence of resistance to existing frontline antimalarial drugs emphasizes a need for the development target-oriented molecules with novel modes action. Given importance plant-like Calcium-Dependent Protein Kinase 1 (PfCDPK1) as stand-alone multistage signalling regulator P. falciparum, we designed and synthesized 7-chloroquinoline-indole-chalcones tethered triazole (CQTrICh-analogs 7 (a–s) 9) directed towards PfCDPK1. This was accomplished by reacting substituted...
A series of natural alcohols motif containing novel substituted cinnamates were developed and screened against five bacterial strains namely, Enterococcus faecal (E. faecalis), Escherichia coli coli), Bacillus subtilis (B. subtilis), Pseudomonas aeruginosa (P. aeruginosa) Klebsiella pneumonieae (K. pneumonieae). Among all cinnamates, YS17 was identified with 100% growth inhibition across the panel, except in E. faecalis MIC values 0.25 mg/mL B. P. whereas 0.125, 0.5 1 coli, K. faecalis,...
Abstract Novel drug like chloroquinoline‐benzylamine hybrids were synthesized and subjected to comprehensive antibacterial evaluation in the present investigation. The pharmacological comprises determination of minimum inhibitory concentration (MIC), disk diffusion assay, hemolysis combination assays against both Gram‐negative ( Pseudomonas aeruginosa ) Gram‐positive Bacillus subtilis, Enterococcus faecalis , Staphylococcus aureus bacterial strains. Among all, 7‐chloroquinoline‐benzylamine...
A series of pyrazolines and metal complexes 3-(furyl)-2-pyrazoline were design, synthesized their structures provided by FT-IR, 1 H-NMR, 13 C-NMR, ESI-MS elemental analysis.These compounds assessed for in-vitro anti-amoebic activity against HMI:IMSS strain Entamoeba histolytica compared with standard drug metronidazole.Pyrazolines showed better in comparison to its mannich base, but the is much more promising than pyrazolines.The docking ADMET studies also conducted investigate probable mode...
Microtubule affinity-regulating kinase 4 (MARK4) is a potential therapeutic target for cancer therapy; as it plays crucial role in division and metastasis. Vanillin key ingredient of vanilla bean extract, has several pharmacological activities including high inhibitory properties towards MARK4. This study aimed to synthesize vanillin-triazole derivatives develop MARK4-specific inhibitors. We emplyed experimental theoretical approaches investigate the potentials synthesized vanillin-triazoles...
Abstract In this investigation, we synthesized substituted 1,2,4‐oxadiazole‐sulfonamide conjugates ( 8 a – l ) through multistep synthetic approach. These compounds were then evaluated against six bacterial strains, consisting of three Gram‐positive and Gram‐negative strains. Among them, compound d displayed notable inhibitory activity, with minimum concentration (MIC) values 64 μg/mL observed the bacteria Staphylococcus aureus Enterococcus faecalis . Notably, in disk diffusion assay,...
Abstract ChemInform is a weekly Abstracting Service, delivering concise information at glance that was extracted from about 100 leading journals. To access of an article which published elsewhere, please select “Full Text” option. The original trackable via the “References”
Abstract To combat the emergence of drug resistance against existing antimalarials, novel side chain containing 7-chloroquinoline-indole-chalcones tethered with a triazole (CQTrICh-analogs 7 (a-s) and 9) were designed synthesized by reacting substituted 1-phenyl-3-(1-(prop-2-yn-1- yl)-1H-indol-3-yl) prop-2-en-1-one 1-(prop-2-yn-1-yl)-1H-indole-3-carbaldehyde 4- azido-7-chloroquinoline, respectively via ‘click’ reaction. The selected CQTrICh-analogs: 7l 7r inhibited chloroquine-sensitive...