Benzopyrones are the club of compounds that can be coumarins or flavonoids. The hydroxyl derivatives of coumarins such as 4-hydroxycoumarins and 7-hydroxycoumarins have extensive biological activities which have employed for the synthesis of miscellaneous coumarin derivatives. These derivatives have exhibited impressive pharmacological and physiological activities such as anticoagulant, antibacterial, antiviral, antitumor, bactericidal, fungicidal, anti-inflammatory agents, and anti-HIV activity. This review comprised pharmacokinetic studies, including absorption, distribution, and metabolism of coumarin analogs along with toxicological studies. The studies of coumarins and their derivatives exhibiting immense pharmacological activity are also summarized in the current study.
Objective: A novel series of substituted 3,3-diphenyl propanamide derivatives (I-VIII) were synthesized by reacting 3,3-diphenyl propanoyl chloride with different amines/amino acids, and all the derivatives were investigated for anthelmintic, antibacterial, and antifungal activity.Methods: All the compounds were characterized by infrared (IR) and1H- nuclear magnetic resonance spectrometry data. The synthesized derivatives were investigated for their anthelmintic activity employing housefly worms method and earthworm species model. The antibacterial and antifungal activity was performed employing cup plate method.Results: The synthesized compounds (VII and VIII) exhibited maximum anthelmintic activity as compared with standard drug albendazole at doses of 50 and 100 mg/mL, due to minimal paralyzing and death time in both housefly and earthworm models. The compounds (IV, VII, and VIII) at 50 μg/mL exhibited maximum activity against Gram-negative bacterial strains, namely, Escherichia coli, Pseudomonas aeruginosa as compared with ciprofloxacin and same compounds exhibited maximum antifungal activity against Candida albicans and Aspergillus niger in comparison with standard drug griseofulvin at 50 μg/mL.Conclusion: The synthesized compounds bearing amino acid moiety in their structure (VII-VIII) exhibited impressive anthelmintic activity in comparison with albendazole. This suggests that amino acid/peptide derivative of diphenyl propanamides can act as great anthelmintic agents. Further, the research can be performed to design potent antimicrobial diphenyl propanamide derivatives.
Objective: The current study was projected to prepare a losartan potassium gastroretentive drug delivery system (GRDDS) of floating tablets was planned to enhance the gastric residence time, thus prolong the drug release.Methods: Effervescent floating matrix tablets of losartan potassium were prepared by direct compression technique using polymers like HPMC k4m, guar gum, and gum karaya, with lubricants magnesium stearate and talc. In the present study, sodium bicarbonate was incorporated as a gas generating agent. Total nine formulations were designed and evaluated for pre-compression parameters known as the angle of repose, bulk density, tapped density, Hausner’s ratio, compressibility index, and post-compression parameters are uniformity of weight, hardness, and drug content percentage, variability, in vitro buoyancy, dissolution studies, and Fourier transform infrared spectroscopy (FTIR).Results: An in vitro dissolution study was carried out by using buffer pH 1.2. From in vitro dissolution studies, it has been found that an increase in polymer concentration diminishes the drug release profile. The in vitro drug release percentage from F4-F9 formulations ranged from 60.28%-98.66% at the closing of 12 h and buoyancy found over 12 h.Conclusion: The in vitro drug release from F1-F3 and F7-F9 followed zero-order, F4 followed Higuchi order, F5 and F6 followed Hixon-Crowell release kinetics. The drug release mechanism was set up to be F1-F8 non-Fickian (anomalous behavior) and F9 having Fickian diffusion type.
Diabetes is a metabolic disorder which evolves from imperfect insulin action and secretion. 1 In congruence with the International Diabetes Federation, diabetes is among the utmost gigantic health hassles. The planetary preponderance of hyperglycemic patients is hypothesized to augment from 415 million in 2015 to 642 million by 2040, symbolizing the escalation of 35.5% in the next 25 years. 2 Diabetes inaugurates multiple organ ruination including eyes, kidneys, liver, heart, and blood vessels. 3 Conventionally, blood investigation is one of the screening proceedings to authenticate general health. Glucose, cholesterol, calcium, total protein, alkaline phosphates, uric acid, sodium, potassium, and chloride levels are indicative values for diabetes mellitus 4 and its associated diseases such as coronary artery disease, dyslipidemia, 5] diabetic nephropathy, 6 chronic hepatopathy, and liver disease. 7 Innumerable plants are affluent source of antidiabetic consequence and have been practiced in
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