A5047226472- Synthesis and Characterization of Heterocyclic Compounds
- Chemical Synthesis and Analysis
- Click Chemistry and Applications
- Crystallization and Solubility Studies
- X-ray Diffraction in Crystallography
- Synthesis and biological activity
- Chemical Synthesis and Reactions
- Synthesis of heterocyclic compounds
- Chemical Reaction Mechanisms
- Sulfur-Based Synthesis Techniques
- Synthesis of Tetrazole Derivatives
- Carbohydrate Chemistry and Synthesis
- Synthesis and Biological Evaluation
- Quinazolinone synthesis and applications
- Antimicrobial Peptides and Activities
- Multicomponent Synthesis of Heterocycles
- Enzyme Catalysis and Immobilization
- Chemistry and Chemical Engineering
- Nonlinear Optical Materials Research
- Innovative Teaching Methods
- Graphene research and applications
- Innovative Microfluidic and Catalytic Techniques Innovation
- Education and Critical Thinking Development
- Crystallography and molecular interactions
- Peptidase Inhibition and Analysis
University of KwaZulu-Natal
2017-2024
Academy of Scientific and Innovative Research
2024
Indian Institute of Chemical Technology
2023-2024
Indian Institute of Technology Patna
2023-2024
Guru Nanak Dev University
2024
Prince Sattam Bin Abdulaziz University
2022
University of Mysore
2013-2014
Solid-phase peptide synthesis (SPPS) is the method of choice for peptides research and production purposes. Despite having several positive features, it remains a challenge to reduce amount solvent waste generated during synthesis. We proposed 3-step protocol (in-situ Fmoc removal) where washing after coupling was eliminated. Here, in-situ removal optimized by adding an extra 4-methylpiperidine (4-MP) treatment ensure Fmoc. Additionally, second addition carbodiimide step performed form in...
Here, we described the synthesis of novel pyrazole-s-triazine derivatives via an easy one-pot procedure for reaction β-dicarbonyl compounds (ethylacetoacetate, 5,5-dimethyl-1,3-cyclohexadione or 1,3-cyclohexadionone) with N,N-dimethylformamide dimethylacetal, followed by addition 2-hydrazinyl-4,6-disubstituted-s-triazine either in ethanol-acetic acid neat acetic to afford a pyrazole and pyrazole-fused cycloalkanone systems. The synthetic protocol proved be efficient, shorter time high...
The study involves exploring the three orthogonal sites for aromatic nucleophilic substitution in cyanuric chloride (TCT). preferential order of incorporation different nucleophiles (such as alcohol, thiol, and amine) was addressed both experimentally theoretically. incorporating TCT found to be alcohol > thiol amine.
GVL is a green solvent used in Fmoc-based solid-phase peptide synthesis. It susceptible to ring opening the presence of bases such as piperidines, which are remove Fmoc protecting group. Here we studied formation corresponding acyl piperidides by time-dependent monitoring using NMR. The results, corroborated theoretical calculations, indicate that solution piperidines should be prepared daily for better removal.
A new class of compounds, which include s-triazine with pyrimidinetrione or thiopyrimidinedione moiety through a hydrazone linkage, were synthesized and characterized. The newly derivatives evaluated in vitro against four cancer cell lines: A549, HepG2, HCT-116, MCF-7. Several showed growth inhibition activity the low microgram range. results reveal that barbiturate poor to no activity, while thiobarbiturate better than analogues derivatives. substituents on have great effect...
A new series of thiobarbituric (thiopyrimidine trione) enamine derivatives and its analogues barbituric acid was synthesised, characterised, screen for in vitro evaluation α-glucosidase enzyme inhibition anti-glycation activity. This compounds were found to inhibit activity a reversible mixed-type manner with IC50 between 264.07 ± 1.87 448.63 2.46 µM. Molecular docking studies indicated that 3g, 3i, 3j, 5 are located close the active site α-glucosidase, which may cover pocket, thereby...
In-situ Fmoc removal leading to sustainable Solid Phase Peptide Synthesis (SPPS).
Two new disulfide-based protecting groups (SIT and MOT) are proposed for Cys thiol in the substitution of StBu, which is often difficult to remove. Both based on a secondary with branched point β-position an efficient modulation its lability and/or stability. This unique structure allows them be fully compatible Fmoc/tBu SPPS. At end synthesis, these removed straightforward manner dithiothreitol some H2O.
PolarClean, a green solvent prepared through the valorization of byproduct Nylon-66 manufacturing, shows an excellent capacity to dissolve all Fmoc-amino acids and key coupling reagents additives. It can also swell polystyrene ChemMatrix, two resins most widely used in solid-phase peptide synthesis. The synthesis model peptides has been carried out, rendering target as major component. performance PolarClean demonstrates its utility toolbox for Green Solid-Phase Peptide Synthesis.
An in silico study, using the GALAS algorithm available ACD/PhysChem Suite, was performed to calculate pKa(s) of various oximes with potential application as peptide coupling additives. Among known and predicted structures, OxymaPure is superior based on pKa values calculated, confirming results described literature validating this for further use that field. nondescribed oximes, calculation, ethyl 2-(hydroxyimino)-2-nitroacetate seems be a candidate used an additive during coupling.
A catalyst-free one-pot synthetic protocol is presented for the preparation of CF
Alzheimer’s disease (AD) lies in the category of those diseases which are still posing challenges to medicinal chemists, and search for super-effective drugs treatment AD is a work progress. The inhibition cholinesterase considered viable strategy enhance level acetylcholine brain. C-5 substituted derivative Meldrum’s acid was synthesized screened against acetylcholinesterase (AChE) butyrylcholinesterase (BChE) enzyme activity. simple unique structure 3 found be good dual both enzymes (AChE...
Abstract A series of urea and thiourea derivatives glutamic acid conjugated to 3‐(1‐piperazinyl)‐1,2‐benzisothiazole were synthesized, spectroscopically characterized, evaluated for their in vitro antiglycation urease inhibitory activities. Preliminary screening the synthesized compounds 1–35 showed significant results. Amongst these, 17 – 21 30 35 bearing fluoro methoxy substituents, respectively, exhibited potency greater than reference standards. Hence, they may serve as new lead further...
1,3,5-Triazines and pyrimidine-2,4,6-triones belong to that class of compounds which are well known in literature for possessing wide range biological activities. Here, we report a new family encompasses these two structures. The union both heterocycles was carried out through hydrazone moiety incorporated into an acetyl group at the position 5 1,3-dimethyl pyrimidine derivative. synthetic strategy adopted allowed preparation target with excellent yields good purities. synthesized were...