Posted by admin on Jul 31, 2022 in |
As per the ICH guidelines and regulatory authorities’ worldwide, it has become mandatory to establish a stability-indicating assay method (SIAM) for the drug substance (DS) and drug product (DP) to generate the stability data. It was undertaken to develop a precise, accurate, reliable, rapid, simple and specific method for estimating Teneligliptin free of interference from its probable degradation products. The present investigation has exploited the high-performance liquid chromatography (HPLC) technique. The retention time of Teneligliptin under optimized chromatographic conditions was found to be 5.71 ±0.02 min with a sharp, symmetrical peak (asymmetry of 0.66 ± 0.02). In the system suitability, the drug was found to adequately retain at 5.71 ±0.02 min with a sharp, symmetrical peak and high theoretical plate value of 4808, indicating high column efficiency. The solutions were observed to undergo hydrolysis in 0.1 N HCl and 0.1 N NaOH at room temperature and reflux. Teneligliptin was also found to be susceptible to rapid oxidation. Photolytic stress study indicates that drug in solid-state upon exposure to sunlight...
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Posted by admin on Jul 31, 2022 in |
Background: The current study used computational approaches to investigate the molecular, physicochemical and drug-like properties of some 4-(10-acetyl-10H-phenothiazines-3-yl)-1-phenylazetidin-2-one derivatives. Methods: The structures of the compounds were drawn using Chemdraw ultra12 and smiles were generated using ACD chem sketch software. The physicochemical and molecular properties were calculated using the OSIRIS data warrior, and Toxicity potential, pharmacokinetic profile and medicinal chemistry aspects were determined by Swiss ADME tools. The docking analysis was carried out by mCule for the antimicrobial and anti-inflammatory profiles. The compounds were targeted for beta-lactamase, peptidoglycan hydroxylase, Cyclo-oxygenase-1 and 2 inhibitions. Result: All the compounds exhibited moderate to good drug likeliness and pharmacokinetic potential. The molecules showed good bioactivity scores against enzyme receptors. The ADMET prediction showed PGP and CYP-inhibitory effects with the least toxic profile. The docking analysis showed good binding affinity toward beta-lactamase, peptidoglycan hydroxylase and cycloxygenase-1 enzymes. Conclusion: The compounds showed good drug likeliness properties along with good toxicity potential and pharmacokinetic profiles. From docking analysis, it was found that all the molecules had a good...
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Posted by admin on Jul 31, 2022 in |
Background: In the Unani System of Medicine, Sandal safed (Sandalwood) is used in many cardiac problems as it possesses Mufarreh (exhilarant) and Muqawwi Qalb (cardiotonic) activities. The present study was designed to evaluate the cardioprotective effect of Sandal safed in Isoproterenol-induced Myocardial Infarction. Methods: Male Wistar rats, weighing 150-200gm, divided into five groups of ten in each. Group I and III rats were given 5% gum acacia (vehicle) and Sandalwood powder in the dose of 800 mg/kg body weight, orally once daily for seven days, followed by subcutaneous administration of normal saline on the 8th and 9th day. Group II, IV & V were administered 5% gum acacia, test drug in the dose of 600 & 800mg/kg body weight, orally once daily for seven days, respectively, followed by isoproterenol hydrochloride (50 mg/ kg body weight) subcutaneously, twice at an interval of 24 h on 8th and 9th day. On 10th day, animals were sacrificed, heart and adrenal glands were weighed, and serum cardiac enzymes and lipid profile were analysed....
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Posted by admin on Jun 30, 2022 in |
A series of novel N10 -substituted 2,4-Dimethoxy acridones were synthesized as potent cytotoxic agents. DNA-binding studies of the synthesized compounds were carried out by the HPLC method using Calf thymus DNA (CT – DNA) based on their affinity or intercalation with CT-DNA, measured by binding percentage. The compound 12 bearing planar dimethoxy tricyclic ring linked with butyl pyrazole side chain showed the highest percentage of binding (90.78%) with CT-DNA and showed binding affinity of -6.08 Kcal/mol with the lipophilicity value of 3.33. Compound 8 showed the highest lipophilicity value of 5.09 with a binding affinity of -6.04 Kcal/mol and a percentage of drug binding (80.93%). Compound 5 showed high binding affinity of 7.01 Kcal/mol with percentage of drug binding (66.94%) and lipophilicity value of 3.72. The Binding affinity and percentage of drug binding showed favorable results. The docking outcome was in good agreement with DNA-binding results confirming the DNA binding activity of compounds. The lipophilicity and binding ability of the acridones with CT-DNA showed poor...
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Posted by admin on Jun 30, 2022 in |
Chikungunya is a mosquito-borne infection of the genus alphavirus. It is vaccines, medications, and other treatments difficult to produce. The CHIK-Virus is carried thru the mosquito, which functions as a vector for the disease. Vaccines, therefore, provide alternate preventative techniques for the spread of viral infection. Structural proteins of CHIK-Virus with T and B cells had been used for immuno-informatic approach. The identification of epitopes is a critical step in the development of vaccines against infectious illnesses. The author of this research work used scientific forte databases to choose the binding interactions of the epitopes PLVPRNAEL and RNEATDGTL have been created for a vaccine that contained non-toxic, non-allergenic, however tremendously antigenic determined in Asia, Africa, and Central South America. As a result of it’s far a high-quality feel polymer virus. The replication of CHIKV in the host results in genome mutation, making T-cells from CHIKV. Finally, epitopes acknowledged thru molecular docking research can be wont to supply huge spectrum vaccines, which might be powerful in opposition to numerous lines...
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