A5101451724- Enzyme function and inhibition
- Cholinesterase and Neurodegenerative Diseases
- Synthesis and Catalytic Reactions
- Synthesis and biological activity
- Computational Drug Discovery Methods
- Click Chemistry and Applications
- Cancer therapeutics and mechanisms
- Chemical Synthesis and Analysis
- Phenothiazines and Benzothiazines Synthesis and Activities
- Synthesis and Characterization of Heterocyclic Compounds
- Alzheimer's disease research and treatments
- Quinazolinone synthesis and applications
- Cell death mechanisms and regulation
- ATP Synthase and ATPases Research
- Health disparities and outcomes
- Biological and pharmacological studies of plants
- Phytochemicals and Medicinal Plants
- Phytochemistry and biological activities of Ficus species
- Cancer-related Molecular Pathways
- Autophagy in Disease and Therapy
- Chemical Reactions and Mechanisms
- Biochemical and Molecular Research
- Natural Antidiabetic Agents Studies
- Aging and Gerontology Research
- Synthesis and Biological Evaluation
University of Toledo
2021-2024
Yale University
2024
Virginia Tech
2024
University of Nebraska Medical Center
2020-2023
Banaras Hindu University
2023
Nebraska Medical Center
2020-2023
Indian Institute of Technology BHU
2023
Indian Institute of Information Technology Design and Manufacturing Jabalpur
2023
Bhupendra Narayan Mandal University
2023
Dr. Rajendra Prasad Central Agriculture University
2023
We report two series of novel benzenesulfonamide derivatives acting as effective carbonic anhydrase (CA, EC 4.2.1.1) inhibitors. The synthesized compounds were tested against human (h) isoforms hCA I, II, VII, and XII. first compounds, 4-(3-(2-(4-substitued piperazin-1-yl)ethyl)ureido)benzenesulfonamides, showed low nanomolar inhibitory action being less the other isoforms. second series, 2-(4-substitued piperazin-1-yl)-N-(4-sulfamoylphenyl)acetamide derivatives, activity II involved in...
Lung cancer is a type of deadly and leading cause associated death worldwide. BCL-2 protein considered as an imperative target for the treatment due to their significant involvement in cell survival death. A carbazole-piperazine hybrid molecule ECPU-0001 was designed synthesized potent targeting agent with effective anticancer activity. Interaction ECPU-001 has been assessed by docking, molecular dynamics (MD) simulation, thermal shift assay. Further, vitro vivo activity executed...
Abstract Inhibition of specific carbonic anhydrase (CA) enzymes is a validated strategy for the development agents to target cancer. The CA isoforms IX and XII are overexpressed in various human solid tumors wherein they play critical role regulating extracellular tumor acidification, proliferation, progression. A series novel sulfonamides based on coumarin scaffold were designed, synthesized characterized as potent selective inhibitors. Selected compounds show significant activity...
Two series of novel benzenesulfonamide derivatives were synthesized and evaluated for their human carbonic anhydrase (CA, EC 4.2.1.1) inhibitory activity against four isoforms, hCA I, II, VII, IX. It was found that compounds both showed low to medium nanomolar potential all isoforms. Some these displayed selective inhibition the epileptogenesis related isoforms II within range. These potent VII inhibitors as anticonvulsant agents MES sc-PTZ induced convulsions. sulfonamides effectively...
Two sets of benzenesulfonamide-based effective human carbonic anhydrase (hCA) inhibitors have been developed using the tail approach. The inhibitory action these novel molecules was examined against four isoforms: hCA I, II, VII, and XII. Most disclosed low to medium nanomolar range inhibition all tested isoforms. Some synthesized derivatives selectively inhibited epilepsy-involved isoforms II showing affinity. anticonvulsant activity selected sulfonamides assessed maximal electroshock...
A series of N-(5-methyl-isoxazol-3-yl/1,3,4-thiadiazol-2-yl)-4-(3-substitutedphenylureido) benzenesulfonamide derivatives has been designed, synthesized and screened for their in vitro human carbonic anhydrase (hCA; EC 4.2.1.1) inhibition potential. These newly sulfonamide compounds were assessed against isoforms hCA I, II, VII XII, with acetazolamide (AAZ) as a reference compound. The majority these found quite weak inhibitor all tested isoforms. Compound 15 showed modest potency I (Ki =...
A series of pyrazolo[3,4-<italic>d</italic>]pyrimidine and urea hybrids have been designed, synthesized evaluated for their anticancer activity<italic>in vitro</italic>and<italic>in vivo</italic>cancer models.
A protocol for the synthesis of 1,4-disubstituted 1,2,3-triazoles <italic>via</italic> three-component reaction by a water soluble copper(<sc>i</sc>) complex has been developed.
A novel small molecule based on benzothiazole-piperazine has been identified as an effective multi-target-directed ligand (MTDL) against Alzheimer's disease (AD). Employing a medicinal chemistry approach, combined with molecular docking, MD simulation, and binding free energy estimation, compound 1 emerged potent MTDL AD. Notably, demonstrated efficient to both AChE Aβ1–42, involving crucial interactions within their active sites. It displayed (ΔGbind) −18.64± 0.16 −16.10 ± 0.18 kcal/mol...