A5066182006- Synthesis and biological activity
- Computational Drug Discovery Methods
- Cholinesterase and Neurodegenerative Diseases
- Click Chemistry and Applications
- Synthesis and Characterization of Heterocyclic Compounds
- Natural Antidiabetic Agents Studies
- Enzyme function and inhibition
- Biochemical and Molecular Research
- Enzyme Production and Characterization
- Microbial Applications in Construction Materials
- Cancer therapeutics and mechanisms
- Multicomponent Synthesis of Heterocycles
- Medicinal Plants and Neuroprotection
- Metal complexes synthesis and properties
- Chronic Lymphocytic Leukemia Research
- Psidium guajava Extracts and Applications
- Pharmacological Effects and Toxicity Studies
- Synthesis and Biological Evaluation
- Enzyme Catalysis and Immobilization
- Plant Pathogens and Fungal Diseases
- Galectins and Cancer Biology
- Plant Genetic and Mutation Studies
- Chromosomal and Genetic Variations
- Cutaneous lymphoproliferative disorders research
- Protein Tyrosine Phosphatases
COMSATS University Islamabad
2022-2025
Quaid-i-Azam University
2024
International Center for Chemical and Biological Sciences
2024
University of Karachi
2024
Latifa Hospital
2024
Khyber Medical University
2022
University of Illinois Urbana-Champaign
2019
University of Illinois Chicago
2019
Illinois College
2019
The current study has afforded twelve analogs (4a-l) of pyridine-derived bis-oxadiazole containing bis-schiff base and subsequently evaluated for their potential to inhibit thymidine phosphorylase(in vitro). All the synthesized were structurally elucidated using various spectroscopic tools including NMR HREIMS. scaffolds showed varied range inhibitory with IC50values ranging from 5.19 ± 1.10 36.18 4.60 μM in comparison 7-deazaxanthine (IC50 = 30.28 2.10 μM) as a standard drug. (except analog...
Alzheimer's dementia (AD), the most prevalent neurodegenerative disorder adversely affecting elderly citizens worldwide, is an incurable with no effective medication found till date. Taking into account seriousness of this issue, imidazopyridine-based benzothiazole-oxadiazole hybrid derivatives were synthesized as anti-Alzheimer's agents. The efficacy these scaffolds was compared standard Donepezil (IC50 = 14.47 ± 1.20 μM for AChE and 19.90 2.40 BuChE). All novel exhibited biological...
Abstract A series of fifteen hybrid analogs ( 1 – 15 ) based on benzimidazole bearing triazole skeleton were synthesized and evaluated for in vitro AChE BuChE inhibition profile. All the newly afforded scaffolds showed moderate to good activity having IC 50 values ranging from 0.40 ± 0.05 19.60 μM against 1.50 0.10 23.30 0.50 comparison Donepezil (IC = 0.016 0.12 AChE), 4.5 0.11 BuChE) as reference drug. It was concluded structure–activity relationship (SAR) studies that groups strong...
In this study, a stepwise reaction afforded thiazolidinone-based benzothiazole derivatives 1-15, and the synthesized were then screened for biological significance found to be leading candidates against α-amylase α-glucosidase enzymes. Almost all showed excellent good activity ranging α-amylase, IC50 = 2.10 ± 0.70 37.50 μM, α-glucosidase, 3.20 0.05 39.40 0.80 μM. Some analogues such as 4 (2.40 3.50 μM), 5 (2.30 4.80 0.10 6 (2.10 μM) with folds better than that of standard drug acarbose (9.10...
The 7-quinolinyl-bearing triazole analogs were synthesized (1d-19d) and further assessed in vitro for their inhibitory profile against α-amylase andα-glucosidase. entire showed a diverse range of activities having IC50 values between 0.80 ± 0.05 µM to 40.20 0.70 (α-amylase) 1.20 0.10 43.30 (α-glucosidase) under the positive control acarbose (IC50 = 10.30 0.20 µM) 9.80 as standard drug. Among scaffolds, seven scaffolds 12d, 10d, 8d, 9d, 11d, 5d, 14d excellent α-glucosidase potentials with...
Hybrid analogs containing molecules are always the choice of different synthetic researcher due to their diverse biological applications and significantly more efficient. Heterocyclic being a good inhibitors against varied disease most commonly used in drug designing development. The current study also addressed synthesis pyrimidine-based thiazolidinone derivatives (1-13) using stepwise processes structure was confirmed various characterization techniques such as 1HNMR, 13CNMR, HREI-MS....
A series of benzimidazole-based Schiff base derivatives (1-18) were synthesized and structurally elucidated through 1H NMR, 13C NMR HREI-MS analysis. Subsequently, these synthetic subjected to evaluation for their inhibitory capabilities against acetylcholinesterase (AChE) butyrylcholinesterase (BuChE). All showed significant inhibition AChE with an IC50 value in the range 123.9 ± 10.20 342.60 10.60 µM BuChE 131.30 9.70 375.80 12.80 comparison standard Donepezil, which has values 243.76 5.70...
Different research synthetic methods have been developed recently for the synthesis of bis-benzimidazole analogs to investigate various biological significances. In this present study, an attempt was made synthesize a new series in fast and efficient method. A variety spectroscopic techniques, including 13C NMR, 1H HREI-MS, were used establish existence every synthesized scaffold. Molecular docking profiles also carried out ascertain binding interactions compounds. All derivatives (1–18)...
The present work described the synthetic procedure adopted for synthesis of bis-indole-based triazine derivatives via a series reactions. All compounds were synthesized through stepwise reaction. After being confirmation thin-layer chromatography (TLC) these characterized various spectroscopic techniques including 1HNMR, 13CNMR and HREI-MS evaluated against beta-glucuronidase in presence standard drug D-saccharic acid 1,4 lactone (IC50 = 31.2 ± 1.0 µM). Most found with better to good...
Alzheimer's disease (AD) is a progressive neurological illness that distinguished clinically by cognitive and memory decline adversely affects the people of old age. The treatments for this gained much attention have prompted increased interest among researchers in field. As springboard to explore new anti-Alzheimer's chemical prototypes, present study was carried out synthesis benzoxazole-oxadiazole analogues as effective inhibitors. In research work, we focused our efforts synthesize...
Twenty-one analogs were synthesized based on benzimidazole, incorporating a substituted benzaldehyde moiety (1–21). These then screened for their acetylcholinesterase and butyrylcholinesterase inhibition profiles. All the derivatives except 13, 14, 20 showed various inhibitory potentials, ranging from IC50 values of 0.050 ± 0.001 µM to 25.30 0.40 against acetylcholinesterase, 0.080 25.80 butyrylcholinesterase, when compared with standard drug donepezil (0.016 0.12 0.30 0.010 µM,...
Aim: Recently, thiadiazole-containing drugs have gained greater clinical relevance and are being explored for the development of new antidiabetic, antiurease antimicrobial agents that target drug resistance. Methods & results: The authors disclose synthesis N-(5-[4-(trifluoromethyl)phenyl]-1,3,4-thiadiazol-2-yl)methanimine derivatives starting from 4-(trifluoromethyl)benzoic acid. All synthesized were evaluated their biological potential in order to investigate inhibitory activity against...
Abstract In the current era, a potent drug is still needed on market for treatment of various diseases worldwide. Researchers mainly focus those enzymes that cause these diseases. One major caused by an enzyme called urease, which increases concentration ammonia in body upon hydrolysis. across globe have keen interest to synthesize inhibitor this conversion. From perspective, hybrid analogs imidazopyridine and oxadiazole ( 1–20 ) were designed efficiently synthesized followed characterizing...
The current study addressed the synthesis of thiazole-based thiazolidinone derivatives (1–18) using stepwise reaction processes, and their structure was confirmed various characterization techniques such as 1HNMR, 13CNMR, HREI-MS. Furthermore, biological features these analogues anti-cancer drugs against human cancer cell lines (HCC78 H3122) were identified. Their inhibitory potentials determined half-maximal concentration (MIC50) in presence standard Tetrandrineb (IC50 = 10.70 ± 0.30 µM),...
A new series of thiazole derivatives (4a-p) incorporating imidazopyridine moiety was synthesized and assessed for their in vitro potential α-glucosidase potency using acarbose as a reference drug. The obtained results suggested that compounds 4a (docking score = −13.45), 4g −12.87), 4o −12.15), 4p −11.25) remarkably showed superior activity against the targeted enzyme, with IC50 values 5.57 ± 3.45, 8.85 2.18, 7.16 1.40, 10.48 2.20, respectively. Upon further investigation binding mode...
In the present work, a concise library of benzothiazole-derived pyrazoline-based thiazole (1-17) was designed and synthesized by employing multistep reaction strategy. The newly compounds were screened for their α-glucosidase urease inhibitory activities. scaffolds characterized using combination several spectroscopic techniques, including FT-IR, 1H-NMR, 13C-NMR, EI-MS. majority demonstrated notable potency against enzymes. These analogues disclosed varying degrees activities, with IC50...
The present work describes the synthetic procedure of 1,2,4-triazole derivatives (1–14) synthesized efficiently in a single step reaction. Basic skeleton confirmation was achieved through different characterization approaches, such as nuclear magnetic resonance(1HNMR and13CNMR) and high-resolution electron ionization mass spectrometry(HREI-MS). In vitro biological assessment these scaffolds anti-urease anti-cancer agents analyzed presence their standard compounds thiourea (IC50 = 9.30 ± 0.20...