Current Bioactive Compounds - Online First
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21 - 26 of 26 results
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A Review of Newer Biologically Potent Pyridine Analogues
Available online: 04 December 2024More LessPyridine is a nitrogen-containing six-membered heterocycle that is used both independently and fused with other heterocyclic rings such as thiazole, thiophene, and most likely with imidazole having a wide range of biological applications. In this review, we report all possible applications of pyridine analogs for all possible diseases. Due to various medicinal applications, the pyridine scaffold has become a fascinating target for medicinal chemistry researchers globally. These particular properties like basicity, water solubility, hydrogen bond forming ability, stability, and small molecular size led researchers to pay more attention to the pyridine molecule with different geometries such as anticancer, antitubercular, anticonvulsant, fungal, bacterial, anti-inflammatory, antidepressant, antioxidant, anti-HIV, antidiabetic and against the COVID 19. This review encompasses all possible applications of pyridine analogs for various diseases.
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Synthesis, Crystal Structure, Spectroscopic Characterization, In Vitro and In Silico Molecular Docking Studies of Benzyl Tetrazole-N-Isobutyl Acetamide Hybrid
Authors: Selvaraj Geetha, Rajendran Sribalan and Srinivasakannan LakshmiAvailable online: 07 November 2024More LessBackgroundTetrazole-based compounds are of significant interest due to their potential pharmacological applications. The current study focuses on the synthesis and analysis of such a compound.
ObjectiveThis research aims to synthesize the title compound N-(3-methyl-1-phenyl-2-(1H-tetrazol-1-yl) butyl) acetamide, analyze its crystal structure, perform computational studies, and evaluate its potential pharmacological activities and it’s in silico and in vitro supports, specifically antidiabetic and anti-inflammatory properties.
MethodsThe title compound, C14H19N5O, was synthesized, and its crystal structure was confirmed using single-crystal X-ray diffraction analysis by default parameters. Density Functional Theory (DFT) calculations were performed using the Gaussian 09W software package with the B3LYP/6-311++G (d,p) method to optimize the compound's structure and calculate its HOMO-LUMO energy gap, Molecular Electrostatic Potential (MEP), and Mulliken charge distribution. In vitro, antidiabetic and anti-inflammatory activities were assessed and compared with standard drugs by using reported protocols. Additionally, molecular docking studies were conducted with enzymes related to diabetes and inflammation with default parameters, and Auto-Dock 4.2 software was used.
ResultsThe X-ray diffraction analysis confirmed the crystal structure, and the Density Functional Theory (DFT) calculations provided insights into the molecular properties of the compound. Molecular docking experiments with relevant enzymes further supported the significant antidiabetic and anti-inflammatory activities demonstrated in the in vitro tests.
ConclusionThe synthesized tetrazole-based compound exhibits promising antidiabetic and anti-inflammatory activities, supported by both experimental and theoretical studies, suggesting its potential for further pharmacological investigation.
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4-methyl-N-[5-[Phenylamino]Acetyl]-2-yl]Benzenesulfonamides: Synthesis, Characterization, and Preliminary Biological Evaluation
Available online: 17 October 2024More LessIntroductionOxazole and the compounds containing sulphonamides are utilized for various treatments of microbial disease as well as for diabetic patients. In the current study, the above moiety synthesizes the new molecule for the treatment of diabetes and microbial infection. The present work involved oxazole-based sulphonamide derivatives by the N-acylation and N-sulphonation. The synthesis was carried out by treating substituted anilines with chloroacetic chloride. The cycloaddition reaction was carried out using triethyl amine as a base catalyst. In the final steps, toluene sulphonyl chloride was used for sulphonation. The synthesized substance was confirmed viaIR, 1H NMR, ESI, Mass spectroscopy, and elemental investigation technique.
Material and MethodsEvery reagent and starting material used in the synthesis was pure enough to be used as a reagent. To provide an inert environment, the solvents were purified in accordance with conventional laboratory protocols under a nitrogen atmosphere. Melting points are expressed in degrees Celsius and are uncorrected. They were determined by the open capillary technique. KBr pellets and a Shimadzu 8201 PC FTIR spectrophotometer were used to obtain FTIR spectra. Using JEOL and Bruker 500 MHz NMR spectrometers, ~1H and ~13C NMR spectra were obtained in CDCl3 and DMSO-d6, with TMS serving as the internal reference. A Thermo-Finnigan mass spectrophotometer was used to determine the masses of the chemical using the ESI technique.
ResultThe present work involved oxazole-based sulphonamides derivatives by the N-acylation and N-sulphonation. The synthesis was carried out by treating substituted anilines with chloroacetic chloride. The cycloaddition reaction was carried out using triethyl amine as a base catalyst. In the final steps, toluene sulphonyl chloride was used for sulphonation. IR, 1HNMR, ESI, Mass spectroscopy and elemental analysis technique confirmed the synthesized compound.
DiscussionOxazoles are also related to compounds called 1,3-azoles[nitrogen and oxygen heteroatoms in a 5-membered ring]. Oxazole demonstrates aromaticity since Huckel's rule requires 6π electrons, which are provided by the delocalization of a single pair of electrons from the oxygen atom. It has a wide range of pharmacological aspects like anti-allergic, hypertension, inflammation, schizophrenia, and inflammation. Similarly, sulphonamides are also used as preventive and chemotherapeutic agents against various diseases such as antibacterial, antiprotozoal, antifungal, and translation initiation inhibitors.
ConclusionThe preliminary biological activity was performed on a preliminary level for the antimicrobial and antidiabetic profile. The disc diffusion approach was utilized to achieve the antibacterial activity; similarly diabetic activity was carried out by the induced method. Out of all the synthesized compounds N-[5-[2-[4-bromophenyl amino]acetyloxazole2 yl]-4methylo benzene sulphonamide [4a], N-[5-2[2-FLoro-5nitrophenyl amino]acetyloxazole2yl]-4methylo benzene sulfonamide [4b] show significant effect compared to standard drugs.
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Bakuchiol and their Derivatives: Unveiling its Chemistry, SAR, Pharmacological Marvels and Therapeutic Odyssey
Available online: 09 October 2024More LessBakuchiol, a meroterpene natural product found in various plants, exhibits diverse biological activities, notably anticancer properties. Researchers have synthesized numerous analogs targeting different positions, such as alcoholic OH, ethenyl, and isopropylidene groups within bakuchiol, aiming to enlighten potent therapeutic agents with enhanced pharmaceutical characteristics. The review aims to focus on the extensive potential of the bioactive molecule, bakuchiol describing SAR that may lead to the development of a variety of bakuchiol derivatives. Literature survey has been carried out to determine the potential of bakuchiol and its derivatives. This review comprehensively outlines the biosynthesis, isolation, patent, and clinical studies of bakuchiol, and pharmacological potential of bakuchiol derivatives documented to date. Additionally, it explores the structure-activity relationships observed in its derivatives. Collectively, findings from various studies underscore the significant potential of bakuchiol and its derivatives in the development of potent anticancer and other therapeutic agents. Ultimately, this review serves as a valuable resource for researchers interested in both the chemistry and biology of bakuchiol, offering insights into its multifaceted applications and paving the way for further exploration in this field.
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An Assessment of Antidepressant Activity of Etlingera elatior Alone and in Combination with Fluoxetine
Available online: 09 October 2024More LessAimPresent study deals to access the antidepressant activity of Etlingera elatior leaves extract in rodent.
BackgroundEtlingera elatior is a species of herbaceous perennial plant in the family Zingiberaceae; native to Indonesia, Thailand, Malaysia and New Guinea. Depression is one of the most common mental disorders affecting humans, pathological basis of which is not fully understood. The current antidepressant drugs have several adverse effects including their effects on cognition. Therefore, natural product are being evaluated for their antidepressant activities.
ObjectiveIn this study, Etlingera elatior leaf extracts are being evaluated for antidepressant activity in rodent models. A wide range of synthetic medicines that can be used to treat depression which may exerts various side effects such as dry mouth, gastrointestinal problems, nausea, respiratory problems, cardiac arrhythmias, drowsiness, anxiety etc. Hence, it becomes essential to discover new anti-depressant drug with more potency, efficacy and safety profile than those of marketed synthetic drugs.
MethodsUsing the forced swimming test, the tail suspension test, mouse 5-HTP-induced head twitches and estimation of brain lipid peroxidation modelsthe antidepressant efficacy of Etlingera elatior ethanolic extract was examined. Imipramine was used as reference standards.
ResultsAccording to our study, Etlingera elatior significantly (p 0.01) reduced immobility in tail suspension, forced swimming, and 5-HTP-induced head twitches in mice with depression that were comparable to imipramine.
ConclusionBased on the results obtained we can conclude that Etlingera elatior leaves extract possess significant antidepressant activity. The antidepressant effectiveness of Etlingera elatior leaves extract can be confirmed in the future by adding more models, and attempts can also be made to isolate and characterise the phytoconstituents responsible for the pharmacological action.
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A Review on Recent Synthesis and Diverse Biological Activities of Isoquinolone
Available online: 08 October 2024More LessIsoquinolone scaffolds are among the most important core structures of nitrogen heterocyclic compounds, which possess vital roles in biological and physiological activities such as anti-tumor, anti-microbial, anti-leukemic, anti-malaria, anti-dengue, anti-HIV and anti-bacterial. Over the years, multiple studies have been done to synthesize these isoquinolone derivatives, and several authors have reported on various methods and synthetic routes to produce the target skeletons of isoquinolones. Therefore, many scientific communities have developed these compounds as the intended structure and evaluated their biological activities. Thus, this review confers several information on isoquinolone analogue synthetic strategies and their biological effects on mosquito-borne diseases.
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Podophyllotoxin: Current Perspectives
Authors: Ying Qian Liu, Liu Yang and Xuan Tian
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