Posted by admin on May 31, 2020 in |
The reaction of 5- (2- chlorophenyl)- 7- nitro- 3H- 1, 4-benzodiazepin-2-thione (I) with glycine (A) by means of Na2CO3 in refluxing ethanol in water gives 2-carboxymethylamino-7-nitro-5-(2-chlorophenyl)-3H-1, 4-benzodiazepine(II), which is cyclized by means of dicyclohexylcarbodiimide in methylene chloride to afford 8-nitro-(2-chlorophenyl)-1,2-dihydro-1H,4H-imidazo[1, 2-a] [1, 4]benzodiazepin-1-one (III). The reaction of (III) with dimethylformamide diethylacetal (B) by means of triethylamine in benzene yields 8-nitro-2-(dimethylaminomethylene)-6-(2-chlorophenyl)-1,2-dihydro-1H, 4H-imidazo[1,2a] [1,4]benzodiazepin-1-one(IV), which is treated with N-methylpiperazine (C) in refluxing toluene result 8-nitro-(2-chlorophenyl)-2-(N-methylpiperazin-1- ylmethylene)- 1, 2- dihydro- 1H, 4H- imidazo[1,2a] [1,4] benzodiazepin-1-one (V). This compound is finally treated with methanesulfonic acid. The condensation of 6-(2-chlorophenyl)-1,2-dihydro-8-nitro-1H, 4H-imidazo [1,2-a] [1,4] benzodiazepin-1one, with 1(dimethoxymethyl)-4-methylpiperazine (II) gives the free base of Loprazolam Mesylate (III), which is then treated with methanesulfonic acid. 5-aryl-1, 3-di-hydro-7-substitued-2H-1,4-benzodiazepine-2-thiones were condensed with glycine in aqueous ethanol to give the previously unreported amino acid. Dicyclohexylcarbodiimide in dry methylenechloride cyclized. These acids to the imidazolobenzodiazepines which were found to oil unstable to hydrolytic...
Read More
Posted by admin on May 31, 2020 in |
Candesartan cilexetil is a novel, potent, and highly selective non-peptide angiotensin II type 1 receptor blocker. It is a hydrophobic drug that belongs to the BCS Class II drug. For enhancement, the bioavailability and quick systemic action of Candesartan cilexetil a novel formulation of buccal (effervescent) tablet, was designed. Preformulation is an important step in the rational formulation of an active pharmaceutical ingredient (API). Micromeritics properties: Bulk density (du), Tapped density (db), Compressibility Index (% C) and sieve analysis was performed in order to determine the best excipients to be used in the formulation development of Candesartan cilexetil (effervescent) tablets. Results show that Candesartan Cilexetil has a fair flow and compressibility properties (du 0.8 g/mL, db 0.7 g/mL, % C 12.5, and sieve analysis time 4.5 min. HPLC method for estimation of Candesartan cilexetil shows linearity ( R2 = 1) and specific with no interference of excipients. Solubility studies reveal that it soluble at pH 6.8 and 7.5 in phosphate buffer. The ability of a material to absorb water...
Read More
Posted by admin on May 31, 2020 in |
Even though numerous herbal preparations have been recommended in alternative systems of medicine against hepatic disorders, many of them cause severe toxicity upon prolonged use. Volvariella volvacea (Bull.: Fr.) Singer is a highly nutritious mushroom that can be incorporated into the regular diet without the fear of side effects. The protective effect of the aqueous ethanol extract of V. volvacea mycelia was evaluated against acetaminophen (APAP) induced hepatic damage in Wistar rats. A single dose of APAP (3 g/kg, p.o.) was used for inducing hepatic damage. The extract was administrated orally at doses of 250 and 500 mg/kg, once daily for 7 days. Treatment with APAP (3 g/kg) increased the activities of liver function enzymes serum glutamate oxaloacetate transaminase (SGOT), serum glutamate pyruvate transaminase (SGPT) and alkaline phosphatase (ALP). APAP also reduced the activities of superoxide dismutase (SOD), catalase (CAT), and glutathione peroxidase (GPx) and enhanced lipid peroxidation in liver tissue. Administration of V. volvacea extract (500 mg/kg, p.o.) decreased the activities of SGPT, SGOT, and ALP. It also...
Read More
Posted by admin on May 31, 2020 in |
The objectives were to observe the drug pattern of epileptic patients with their seizure type, to analyze the type of therapy received by the patients, to observe if epileptic patients are receiving an appropriate dose, to identify the side effects in epileptic patients associated with drug treatment and to observe the cost of conventional and newer antiepileptic drugs (AED’s). This was a cross-sectional observational study conducted in the Neurology department. A total of 150 patients were selected based on the inclusion and exclusion criteria. Demographic details and clinically relevant details such as therapy, dose of the drug, side effects experienced pertaining to the objectives of the study were collected using the self-prepared proforma. Symptomatic localization (64%) was the most commonly observed epilepsy syndrome. The commonly observed type of therapy among the patients was dual therapy. AED dose prescribed for most of the adult population was at a sub-optimal level, as explained by the daily defined dose/ prescribed daily dose (DDD/PDD) ratio (<1). Carbamazepine and oxcarbazepine were prescribed at a...
Read More
Posted by admin on May 31, 2020 in |
Schiff bases from chitosan and 5-nitro salicylaldehyde-aniline complexes represented the important structural subject in excess of biologically active molecules, including synthetic. The introduction of 5-nitro salicylaldehyde at C-2 nitrogen position and aniline at C-6 oxygen position of chitosan. The structure-activity relationship (SAR) of the double Schiff based chitosan, synthesized from the condensation reaction of equimolar amounts of 5-nitrosalicyl-aldehyde, chitosan, and aniline in DMSO. The chitin and the phenyl rings deviate from co-planarity with an inter and intra-molecular bond (–C2-N=CH–), (–C6–C=N–). The title compound C69H118N11O43 is not a planner, with a dihedral angle among the planes of the three aryl rings. The structure is a heterocyclic derivative constituting a stimulating class of compounds with synthetic flexibility and productive biological activities. The synthesized compound structurally categorized by FT-IR, 1H-NMR, GC-Mass spectra, and TG/DTA studies. The 1H-NMR spectroscopy used to determine the degree of acetylation in chitosan. The synthesized compound primarily parted for their in-vitro growth constraining activity against a different strain of bacterial and fungal. The in-vitro antioxidant activity of the...
Read More
