Facile 3-chloro-1H-indazole based 1,3,4-thiadiazole derivatives as novel thymidine phosphorylase and anti-diabetic inhibitors: Experimental, in-vitro and molecular modelling approaches.

A series of novel 3-chloro-1H-indazole-based 1,3,4-thiadiazole derivatives (1-15) were synthesized, characterized and evaluated for their inhibitory activity against thymidine phosphorylase and α-glucosidase. Several compounds showed potent dual inhibition, with compound 4 exhibiting the highest activity (IC = 4.70 ± 1.

Novel thiazole-thiadiazole as a potential anti-Alzheimer agent: synthesis and molecular interactions via an in silico study.

Aim: This study aimed to synthesize and evaluate a series of thiazole-derived thiadiazole-based Schiff base derivatives (1-16) for their potential anti-Alzheimer and antioxidant activities, with a focus on identifying promising drug-like candidates.

Materials & Methods: The synthesized compounds were structurally characterized using H-NMR, C-NMR, and mass spectrometry. Their biological potential was assessed via in vitro anti-Alzheimer assays (AChE and BuChE inhibition) and DPPH-based antioxidant screening.

Unveiling of the novel benzothiazole derived thiazolidinone derivatives: in vitro and in silico insights to design a promising agent for anti-Alzheimer's disease.

The present investigation explained various heterocyclic moieties particularly the thiazolidinone scaffold () which were synthesized from benzothiazole as promising anti-Alzheimer agent. In this, we have unveiled the synthetic path for generation of thiazolidinone scaffolds which was initiated benzothiazole having 2-amine moiety. These synthesized scaffolds were then inveterate through several analytical techniques including high-resolution electron impact mass spectrometry (HREI-MS), proton nuclear magnetic resonance (H NMR), and carbon-13 nuclear magnetic resonance (C NMR).

Novel oxazole based oxadiazole conjugates: Synthesis, DFT study and in silico confirmation as potent anti-diabetic agents.

In an approach to combat Diabetes mellitus (a severe metabolic disorder), novel oxazole derived oxadiazole derivatives (1-16) were synthesized having improved biological profile and minimal side effects. These compounds were screened for their biological potential against alpha-amylase and alpha-glucosidase in comparison to standard drug acarbose (4.50 ± 0.

Anti-Leukemic Profiling of Oxazole-Linked Oxadiazole Derivatives: A Computational and Kinetic Approach.

Leukemia is a common cancer that arises in both children and adults when bone marrow's hematopoietic stem cells proliferate unrestrained because of anomalies in normal cell regulatory systems. The present study focused on biological evaluation of oxazole-based oxadiazole scaffolds to evaluate the anti-proliferative effect on leukemic cancer cell lines. All novel oxazole-based oxadiazole scaffolds were synthesized and structurally characterized via C NMR, H NMR, and HREI-MS.

Insight the confirmation of benzothiazolidinone-derived thiadiazole scaffolds as promising antiurease and anti-Alzheimer agents: synthesis, , and investigations.

Alzheimer's disease is a serious neurological disorder, and traditional therapies for Alzheimer's, like radiation and surgical procedures, as well as chemotherapeutics, are usually linked with multiple negative consequences. Finding a novel therapeutic anti-Alzheimer agent with high efficacy and minimal side effects, we have designed and synthesized benzothiazolidinone-derived thiadiazole-based Schiff base derivatives (). Biological assessment of these compounds was carried out against acetylcholinesterase and butyrylcholinesterase, and all the derivatives showed varying degrees of inhibitory activity.

Comparison of Complications and Outcomes Following Transurethral Resection of the Prostate in Patients Presenting With and Without Acute Urinary Retention.

Objective: The objective of this study is to evaluate the outcomes and complications of transurethral resection of the prostate (TURP) in patients with and without acute urinary retention (AUR).

Methodology: This descriptive study was conducted in the Urology Department of the Institute of Kidney Diseases (IKD), Hayatabad Medical Complex (HMC), Peshawar, from 11th August 2023 to 11th February 2024. A total of 127 male patients aged over 40 years with prostate sizes between 40 and 80 grams on ultrasonography were included.

Insight into thymidine phosphorylase and molecular docking studies: identification of hybrid thiazole bearing Schiff base derivatives.

In pursuit of effective thymidine phosphorylase inhibitors, a series of hybrid analogs of thiazole-hydrazone derivatives (1-15) were synthesized and evaluated for their enzyme inhibitory potential using 7-deazaxanthine as a positive control. The goal was to determine these derivatives' effectiveness in suppressing thymidine phosphorylase activity, a target relevant to antitumor strategies due to the enzyme's role in angiogenesis and tumor growth. Biological evaluations indicated that all synthesized analogs displayed significant to moderate inhibitory activity, with IC values between 3.

and assessment of thiazole-thiazolidinone derivatives as selective inhibitors of urease and α-glucosidase.

Aims: Current research work aims to synthesize hybrid compounds with a thiazole-thiazolidinone structure, as potent inhibitors of urease and α-glucosidase enzymes.

Materials And Methods: These compounds were characterize throughHNMR,CNMR and HREI-MS techniques. These compounds were also evaluated for their potential to inhibit urease and α-glucosidase enzymes for the treatment of urinary tract infections (UTIs) and diabetes treatments.

Molecular modeling and synthesis of novel benzimidazole-derived thiazolidinone bearing chalcone derivatives: a promising approach to develop potential anti-diabetic agents.

Diabetes mellitus (DM) is a disorder which is raised at the alarming level and it is characterized by the hyperglycemia results from the impaired action of insulin, production of insulin or both of these simultaneously. Consequently, it causes problems or failure of different body organs such as kidneys, heart, eyes, nerve system. Since this disease cannot be completely cured until now, we aimed to design series of enzymes inhibitors and tested them for DM treatment.

Novel pyrrole based triazole moiety as therapeutic hybrid: synthesis, characterization and anti-Alzheimer potential with molecular mechanism of protein ligand profile.

As a springboard to explore novel potent inhibitors of cholinesterase enzymes (AChE and BChE) responsible for causing Alzheimer disorder, the current study was conducted to synthesize pyrrole derived triazole based Schiff base scaffolds by facile synthetic route. These compounds were validated by HNMR, CNMR and HREI-MS. All these scaffolds (1-16) were examined for their inhibitory activity against AChE and BChE in contrast to Donepezil (10.

Novel indole based fused triazole-thiadiazole derivatives as anti-diabetic agents: and approaches.

The current research presents novel library of indole derived fused triazole-thiadiazole derivatives (1-17) for treatment of diabetes mellitus. These compounds were synthesized by treating 2-(1H-indol-3-yl)acetic acid with hydrazinecarbothiohydrazide followed by treating the resultant compound with substituted benzoic acid. Structural validation was achieved spectroscopically (HNMR, CNMR and HREI-MS).

Harnessing the synergistic potential of TiO-CuSe composites for enhanced photocatalytic and antibacterial activities.

With growing environmental concerns, the removal of toxic industrial dyes from wastewater has become a critical global issue. In this study, TiO-CuSe composites were synthesized using a cost-effective and simple chemical method to determine the optimal concentration of CuSe for the efficient degradation of methylene blue (MB) under visible light. The TiO samples exhibited a mix of rutile and anatase phases, while CuSe formed in a hexagonal phase.

Synthesis, biological and computational evaluation of benzoxazole hybrid analogs as potential anti-Alzheimer's agents.

Current study aims exploration of -benzoxazole bearing -Schiff base scaffolds () as anti-Alzheimer's agents. 2-aminophenol is used as starting materials which react with different reagents in different step to give us -benzoxazole bearing -Schiff base analogs. NMR and HREI-MS techniques were used for characterization.

Facile synthesis of NiSe-ZnO nanocomposites for enhanced photocatalysis and wastewater remediation.

In this study, NiSe nanocubes, ZnO rods, and their composites were prepared by simple chemical methods to investigate their photocatalytic response and antibacterial activity. The optimal concentration of NiSe nanocubes was explored for enhanced photocatalytic performance by varying its percentage in the NiSe-ZnO composites. The findings suggested that the optical response of ZnO was significantly improved and shifted towards visible region by incorporating NiSe as a co-catalyst.

Electrophoretically deposited Asphaltum punjabianum (Shilajit) coatings on polyvinylalcohol/carboxymethylcellulose hydrogels.

The present study aims to develop Asphaltum punjabianum (namely Shilajit) coated Polyvinyl alcohol (PVA)/Carboxymethyl cellulose (CMC) hydrogels and examine their structural, morphological, degradation, and biological properties. Hydrogels were produced at two different concentrations: 70:30 PVA/CMC and 90:10 PVA/CMC. Following that, Shilajit was applied to the synthesized hydrogels using electrophoretic deposition for a duration of 3 min at 30 V.

Discovery of Novel and Selective Schiff Base Inhibitors as a Key for Drug Synthesis, Molecular Docking, and Pharmacological Evaluation.

Diabetes mellitus (DM) is a chronic disorder and still a challenge throughout the world, and therefore the search for safe and effective inhibitors for α-amylase and αglucosidase is increasing day by day. In this work, we try to carry out the synthesis, modification, and computer-aided results of and biological research on thiadiazole-based Schiff base derivatives and evaluate their α-amylase and αglucosidase inhibitory potential (-). In the current series, all of the synthesized analogues were shown to have potential inhibitory effects on targeted enzymes.

molecular modeling and biological screening of novel benzimidazole-based piperazine derivatives as potential acetylcholinesterase and butyrylcholinesterase inhibitors.

New series of benzimidazole incorporating piperazine moieties in single molecular framework has been reported. The structures of the synthesized derivatives were assigned by H-NMR, C-NMR, and HR-MS techniques. The hybrid derivatives were evaluated for their acetylcholinesterase and butyrylcholinesterase inhibition effect.

Synthesis of modified Schiff base appended 1,2,4-triazole hybrids scaffolds: elucidating the and α-amylase and α-glucosidase inhibitors potential.

The current study involves the synthesis of Schiff bases based on 1,2,4-triazoles skeleton and assessing their α-amylase and α-glucosidase profile. Furthermore, the precise structures of the synthesized derivatives were elucidated using various spectroscopic methods such as H-NMR, C-NMR and HREI-MS. Using glimepiride as the reference standard, the α-glucosidase and α-amylase inhibitory activities of the synthesized compounds were evaluated in order to determine their potential anti-diabetic properties.

Identification of novel benzothiazole-thiadiazole-based thiazolidinone derivative: and approaches to develop promising anti-Alzheimer's agents.

The present study describes benzothiazole derived thiazolidinone based thiadiazole derivatives () as anti-Alzheimer agents. Synthesis of benzothiazole derived thiazolidinone based thiadiazole derivatives was achieved using the benzothiazole bearing 2-amine moiety. These synthesized compounds were confirmed via spectroscopic techniques (H NMR, C NMR and HREI-MS).

Recent development and strategies towards target interactions: Synthesis, characterization and in silico analysis of benzimidazole based thiadiazole as potential anti-Alzheimer agents.

In the current research study, we aim to design and synthesize highly potent hybrid analogs of benzimidazole derived thiadiazole based Schiff base derivatives which can combat the cholinesterase enzymes (acetylcholinesterase and butyrylcholinesterase) accountable for developing Alzheimer's disease. In this context, we have synthesized 15 analogs of benzimidazole based thiadiazole derivatives, which were subsequently confirmed through spectroscopic techniques including H NMR, C NMR and HREI-MS. Biological investigation of all the analogs revealed their varied acetylcholinesterase inhibitory potency covering a range between 3.

Facile benzothiazole-triazole based thiazole derivatives as novel thymidine phosphorylase and α-glucosidase inhibitors: Experimental and computational approaches.

The present study reports the new thiazole (A-L) derivatives based on benzothiazole fused triazole which were synthesized and assessed against thymidine phosphorylase and α-glucosidase enzymes. Several compounds with the same basic structure but different substituents were found to have high activity against the targeted enzymes, while others with the same basic skeleton but different substituents were found to have medium to low activity among the members of tested series. These analogs showed a varied range of inhibition in both case thymidine phosphorylase and alpha glucosidase, A (IC = 7.

Synthesis, In Vitro Biological Evaluation and Molecular Modeling of Benzimidazole-Based Pyrrole/Piperidine Hybrids Derivatives as Potential Anti-Alzheimer Agents.

Benzimidazole-based pyrrole/piperidine analogs (-) were synthesized and then screened for their acetylcholinesterase and butyrylcholinesterase activities. All the analogs showed good to moderate cholinesterase activities. Synthesized compounds (-) were screened in cholinesterase enzyme inhibition assays and showed AChE activities in the range of IC = 19.