SYNTHESIS AND ANTIMICROBIAL ACTIVITY EVALUATION OF SOME SCHIFF BASES DERIVED FROM 2-AMINOTHIAZOLE DERIVATIVES

Various substituted acetophenones (1-5) on treatment with iodine and thiourea yielded 2-amino-4-(substituted-phenyl)-thiazole (1a-5a), which on further treatment with various substituted aldehydes to get N-(substitutedbenzylidene)-4-(substitutedphenyl) thiazol-2-amine (1b-5b). All the synthesized compounds were characterized by their respective FTIR, 1H NMR and mass data. Synthesized compounds (1b-5b) were subjected to investigation for their antibacterial and antifungal studies against Staphylococcus aureus, Escherichia coli, Pseudomonas aeruginosa, Candida albicans, Asperigillus flavus and Asperigillus fumigatus by disk diffusion method. Compound 5b was found to be most effective with largest zone of inhibition.Key words: thiazole, acetophenones, antibacterial, antifungal, substituted aldehydes

SYNTHESIS AND ANTIMICROBIAL ACTIVITY EVALUATION OF SOME SCHIFF BASES DERIVED FROM 2-AMINOTHIAZOLE DERIVATIVES

Various substituted acetophenones (1-5) on treatment with iodine and thiourea yielded 2-amino-4-(substituted-phenyl)thiazole (1a-5a), which on further treatment with various substituted aldehydes to get N-(substitutedbenzylidene)-4(substitutedphenyl)thiazol-2-amine (1b-5b). All the synthesized compounds were characterized by their respective FTIR, H NMR and Mass data. Synthesized compounds (1b-5b) were subjected to investigation for their antibacterial and antifungal studies against Staphylococcus aureus, Escherichia coli, Pseudomonas aeruginosa, Candida albicans, Asperigillus flavus and Asperigillus fumigatus by disk diffusion method. Compound 5b was found to be most effective with largest zone of inhibition

Synthesis and antibacterial profile of novel azomethine derivatives of β-phenylacrolein moiety

Purpose: To develop some novel molecules effective against antibiotic-resistant bacterial infections.Methods: A series of azomethines (SB-1 to SB-6) were synthesized from β-phenyl acrolein moiety. The structures of the synthesized compounds were confirmed on the basis of their UV ultra-violet (UV) spectroscopy (λmax: 200 - 400 nm), Fourier transform infra-red (FTIR, vibrational frequency: 500-4000 cm-1), 1H nuclear magnetic resonance (NMR, chemical shift: 0 - 10 ppm), 13C NMR (chemical shift: 0 - 200 ppm), mass spectrometry (m/z values: 0 - 500) and carbon hydrogen nitrogen (CHN) elemental analysis. The new compounds were screened for antibacterial activity by test-tube dilution and disc diffusion methods using gentamicin as reference standard.Results: The structures of azomethine were in full agreement with their spectral data. Among all the synthesized compounds, compounds SB-5 and SB-6 exhibited the highest minimum inhibitory concentration (MIC) of 62.5 μg/mL. At MIC of 250 μg/mL, all compounds SB-1 to SB-6 displayed significant antibacterial activity, compared to gentamycin (p < 0.05). SB-5 and SB-6 were active against S. aureus, P. aeruginosa and K. pneumoniae; SB-3 was active against B. subtilis and S. aureus. SB-4 was active against P. aeruginosa and S. aureus while SB-1 and SB-2 were active against S. aureus.Conclusion: The synthesized compounds possess antibacterial activities compared to those of gentamycin.Keywords: Acrolein, Imines, Azomethine, Antibacterial, Gentamycin, Minimum inhibitory concentratio

Deciphering Synsepalum dulcificum as an arising phytotherapy agent : background, phytochemical and pharmacological properties with associated molecular mechanisms

Medicinal plants with less side effects are paramount important for humankind to cure various ailments as compared to newly developed allopathic medicines. Synsepalum dulcificum Daniell (Sapotaceae), is well known as miracle fruits due to its distinctive taste-modifying property. This review aimed to discuss its recent reported pharmacological properties and associated molecular mechanisms as a novel phytotherapy agent. In addition, background, phytochemical analysis and toxicological studies were also discussed as the foundation and added values for this review. It was discovered that S. dulcificum is endowed with various classes of phytochemicals, such as flavonoids, tannins, alkaloids and saponins. This review ravelled that S. dulcificum is a potent medicinal plant associated with antioxidant, antidiabetic, antimicrobial, anticancer, anti-hyperuricemic, hepatoprotective, anti-hyperlipidaemic, and anticonvulsant activities, with less toxicity shown. Future research may explore further the corresponding phytochemicals, associated molecular mechanisms, toxicological and pharmacokinetic profile before subjecting to clinical testing

Evaluation of Antitumor Efficacy of Chitosan-Tamarind Gum Polysaccharide Polyelectrolyte Complex Stabilized Nanoparticles of Simvastatin

Purpose: The present study was intended to fabricate chitosan (Ch)-tamarind gum polysaccharide (TGP) polyelectrolyte complex stabilized cubic nanoparticles of simvastatin and evaluate their potential against human breast cancer cell lines. Materials and Methods: The antisolvent precipitation method was used for formulation of nanoparticles. Factorial design (32 ) was utilized as a tool to analyze the effect of Ch and TGP concentration on particle size and entrapment efficiency of nanoparticles. Results: Formulated nanoparticles showed high entrapment efficiency (67.19±0.42–83.36 ±0.23%) and small size (53.3–383.1 nm). The present investigation involved utilization of two biological membranes (egg and tomato) as biological barriers for drug release. The study revealed that drug release from tomato membranes was retarded (as compared to egg membranes) but the release pattern matched that of egg membranes. All formulations followed the Baker–Lansdale model of drug release irrespective of the two different biological barriers. Stability studies were carried out for 45 days and exhibited less variation in particle size as well as a reduction in entrapment efficiency. Simvastatin loaded PEC stabilized nanoparticles exhibited better control on growth of human breast cancer cell lines than simple simvastatin. An unusual anticancer effect of simvastatin nanoparticles is also supported by several other research studies. Conclusion: The present study involves first-time synthesis of Ch-TGP polyelectrolyte complex stabilized nanoparticles of simvastatin against MCF-7 cells. It recommends that, in future, theoretical modeling and IVIVC should be carried out for perfect designing of delivery systems

Deciphering synsepalum dulcificum as an arising phytotherapy agent: Background, phytochemical and pharmacological properties with associated molecular mechanisms

Medicinal plants with less side effects are paramount important for humankind to cure various ailments as compared to newly developed allopathic medicines. Synsepalum dulcificum Daniell (Sapotaceae), is well known as miracle fruits due to its distinctive taste-modifying property. This review aimed to discuss its recent reported pharmacological properties and associated molecular mechanisms as a novel phytotherapy agent. In addition, background, phytochemical analysis and toxicological studies were also discussed as the foundation and added values for this review. It was discovered that S. dulcificum is endowed with various classes of phytochemicals, such as flavonoids, tannins, alkaloids and saponins. This review ravelled that S. dulcificum is a potent medicinal plant associated with antioxidant, antidiabetic, antimicrobial, anticancer, anti-hyperuricemic, hepatoprotective, anti-hyperlipidaemic, and anticonvulsant activities, with less toxicity shown. Future research may explore further the corresponding phytochemicals, associated molecular mechanisms, toxicological and pharmacokinetic profile before subjecting to clinical testing

Fabrication of Tizanidine Loaded Patches Using Flaxseed Oil and Coriander Oil as a Penetration Enhancer for Transdermal Delivery

Transdermal drug delivery is important to maintain plasma drug concentrations for therapeutic efficacy. The current study reports the design, formulation, and evaluation of tizanidine transdermal patches formulated using chitosan and thiolated chitosan, ethyl cellulose (EC), polyvinylpyrrolidone (PVP), and Eudragit RL100 in different ratios. The tizanidine patches were formulated using flaxseed oil and coriander oil in the concentrations of 1% v/w, 2% v/w, 3% v/w, 4% v/w, 5% v/w, and 10% v/w. The patches were subjected to characterization of physicochemical property (thickness, weight uniformity, drug content, efficiency, percentage moisture uptake/loss), in vitro drug release and drug permeation, skin irritation, in vivo application, pharmacokinetics analysis, and stability studies. The results indicate that the interaction of thiolated chitosan with the negative charges of the skin opens the tight junctions of the skin, whereas flaxseed and coriander oils change the conformational domain of the skin. The novelty of this study is in the use of flaxseed and coriander oils as skin permeation enhancers for the formulation of tizanidine transdermal patches. The formulations follow non-Fickian drug release kinetics. The FTZNE23, FTZNE36 and FTZNE54, with 5% v/w flaxseed oil loaded formulations, exhibited higher flux through rabbit skin compared with FTZNE30, FTZNE35, FTZNE42, and FTZNE47, formulations loaded with 10% v/w coriander oil. The study concludes that flaxseed oil is a better choice for formulating tizanidine patches, offering optimal plasma concentration and therapeutic efficacy, and recommends the use of flaxseed and coriander oil based patches as a novel transdermal delivery system for tizanidine and related classes of drugs

Determination of Temperature-Dependent Coefficients of Viscosity and Surface Tension of Tamarind Seeds (Tamarindus indica L.) Polymer

The rheological properties of tamarind seed polymer are characterized for its possible commercialization in the food and pharmaceutical industry. Seed polymer was extracted using water as a solvent and ethyl alcohol as a precipitating agent. The temperature’s effect on the rheological behavior of the polymeric solution was studied. In addition to this, the temperature coefficient, viscosity, surface tension, activation energy, Gibbs free energy, Reynolds number, and entropy of fusion were calculated by using the Arrhenius, Gibbs–Helmholtz, Frenkel–Eyring, and Eotvos equations, respectively. The activation energy of the gum was found to be 20.46 ± 1.06 kJ/mol. Changes in entropy and enthalpy were found to be 23.66 ± 0.97 and −0.10 ± 0.01 kJ/mol, respectively. The calculated amount of entropy of fusion was found to be 0.88 kJ/mol. A considerable decrease in apparent viscosity and surface tension was produced when the temperature was raised. The present study concludes that the tamarind seed polymer solution is less sensitive to temperature change in comparison to Albzia lebbac gum, Ficus glumosa gum and A. marcocarpa gum. This study also concludes that the attainment of the transition state of viscous flow for tamarind seed gum is accompanied by bond breaking. The excellent physicochemical properties of tamarind seed polymers make them promising excipients for future drug formulation and make their application in the food and cosmetics industry possibl