Department of Pharmacy
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Item Phytochemical screening, total phenol estimation, antioxidant activity of Blainville camellia leaf and stem successive extracts(2014) Jadhav, Hemant R.The aim of present work was to investigate antioxidant potential of different extracts of Blainvillea acmella leaf and stem. The successive extraction of individual plant part was carried out using solvents of different polarity viz. n-hexane, ethyl acetate, methanol and water. Preliminary phytochemical screening of all the extracts was done. The present total phenolic contents were estimated by Folin-Ciocalteu reagent method and expressed as µg/mg of gallic acid equivalent. The antioxidant potential and reducing power of all the prepared extracts were measured against DPPH, as compared to standard ascorbic acid, and BHA respectively. The result data indicate that the phenolic contents were higher in methanolic extracts of leaf (73.67±0.38 mg/g) followed by ethyl acetate (29.08±0.38 mg/g), aqueous (21.50±0.28 mg/g), and n-Hexane (9.29±0.38 mg/g); gallic acid equivalent. The similar pattern in stem part was also observed ie methanolic extracts (41.90±0.45 mg/g), ethyl acetate (21.92±0.28 mg/g), aqueous (15.13±0.18 mg/g), and n-Hexane (3.69±0.28 mg/g). The antioxidant capacity of methanolic extract of both the part ie leaf and stem was found to be maximum, as IC50 values were 226.49±0.16, 402.05±1.10 respectively. The reducing power was also highest in methanol extract of both parts. The result data conclude that the higher antioxidant as well as reducing power may be due to present phenolic contentsItem Design, synthesis and evaluation of acridin-9-yl hydrazide derivatives as BACE-1 inhibitors(Springer, 2016-04) Jadhav, Hemant R.BACE-1, an aspartyl protease is implicated in Alzheimer’s disease. In this paper, we report BACE-1 inhibitory potential of acridin-9-yl hydrazide derivatives, known to inhibit other aspartyl proteases. The derivatives were designed based on the docking study, synthesized and assessed for BACE-1 inhibition in vitro. Docking simulation predicted the binding of prototype acridin-9-yl hydrazide at BACE-1 active site. The enzyme–inhibitor complex was primarily stabilized by hydrogen bonds between the hydrazide part of the inhibitor and side chain of Gly11, which is important amino acid of 10s loop. The acridinyl moiety showed π–π stacking with Tyr71 while the phenyl ring was buried in S1 cavity. Enzyme inhibition experiments showed that the synthesized compounds had moderate activity with compound AA-13 having 54.54 % inhibition at 10 µM concentration.Item Synthesis and Biological Evaluation of N-(4-Fluorophenyl)-6-Methyl-2-Oxo-1, 2, 3, 4-Tetrahydropyrimidine-5-Carboxamides as HIV Integrase Strand Transfer Inhibitors(2018) Jadhav, Hemant R.HIV-1 integrase (IN) catalyzes chromosomal integration of synthesized viral DNA into host DNA by performing two independent reactions, 3′-processing (3′-P) and strand transfer (ST). In the present study, we report synthesis and evaluation of N-(4-fluorophenyl)-6-methyl-2-oxo-4-substituted phenyl-1,2,3,4-tetrahydropyrimidine-5-carboxamides for IN inhibitory activity. All the derivatives were found to inhibit strand transfer reaction in vitro in isolated enzyme assay and most active compound (13e) showed IC50 value of 0.65 μM. Docking studies were also done to justify the IN inhibition and in vitro-in silico correlation was drawn. However, these compounds did not show HIV-1 and HIV-2 inhibition below their cytotoxic concentration in cell culture assay indicating that these compounds cannot be used as lead for anti-HIV activity.Item Synthesis and Evaluation of 3-(1,3-dioxoisoindolin-2-yl)-N-substituted Phenyl Benzamide Analogues as HIV Integrase Strand Transfer Inhibitors(Bentham Science, 2019) Jadhav, Hemant R.A series of novel 3-(1,3-dioxoisoindolin-2-yl)-N-substituted phenyl benzamide derivatives was synthesized and tested in vitro against human immunodeficiency virus type-1 Integrase (HIV-1 IN).Item Small Molecular Inhibitors for the Treatment of Rheumatoid Arthritis: Progress so Far(Bentham Science, 2015) Jadhav, Hemant R.Rheumatoid Arthritis (RA) is an autoimmune disease characterized by persistent inflammation and joint damage. The main aim of RA treatment is to control the disease progress. Despite the success of biologicals like Adalimumab, Atlizumab, infliximab, etc. in treatment of RA, the high cost and associated immunological adverse effects have triggered discovery of small molecules targeting RA. This review describes the last 15 years of small molecular drug discovery in RA, focused mainly on preclinical and clinical studiesItem QSAR and Docking Studies of N-hydroxy Urea Derivatives as Flap Endonuclease-1 Inhibitors(Bentham Science, 2015) Jadhav, Hemant R.Flap endonuclease-I (FEN-1) is involved in DNA repair and considered to be a novel target for the development of anticancer agents. N-hydroxy urea derivatives have been reported as FEN-1 inhibitors. To derive in vitro and in silico correlation, we have performed 2D-quantitative structure activity relationship (QSAR) analysis and docking studies on these compounds. 2D-QSAR models were developed using multiple linear regression (MLR) analysis and cross-validation using leave one out (LOO) method. The best model displayed R2 of 0.806 and Q2 of 0.607. Docking study revealed key interactions with desired amino acids and compare well with the in vitro potency of the reported compounds. Both studies reveal a link between FEN-1 inhibition and physicochemical descriptors or interactions with amino acids in active site. The information generated is first of its kind and may be helpful in the design of novel FEN-1 inhibitors.Item Fast Dissolving Oral Films(Bentham Science, 2017) Jadhav, Hemant R.Ease of administration and patient compliance makes the oral route as the most popular route of administration, but difficulty in swallowing or dysphagia may limit the use of oral route in special populations like paediatrics, geriatrics, psychotics, cancer patients, etc. Unavailability of water and episodic attack of allergy also contributes to difficulties in swallowing tablets and capsules. Here the novel fast dissolving oral film (FDOF) technology gives new hope to overcome these problems. Oral films made from active ingredient and hydrophilic polymers are capable of rapidly dissolution/disintegration in the buccal cavity. A part of the drug is absorbed from buccal route providing the advantages of quicker onset, bypassing first pass effect and reducing gastric degradation or metabolism. These qualities have made oral film a very popular and convenient dosage form for paediatric, geriatric as well as adult populations. This chapter describes formulation aspects, preparation technologies and some important patents of FDOFs.Item A Proposed Methodology for In Vitro Evaluation of Bitterness in Drug Solutions and In Vitro Drug Release Samples(Springer, 2014-04) Jadhav, Hemant R.Ethical and safety concerns, paediatric taste panels and predictivity in early drug development for strategic decisions are some of the reasons for seeking in vitro methods of bitterness evaluation for drugs and drug products. In this study, taste panel studies and in vitro drug release studies have been performed, correlated to each other and proposed as an analytical tool for evaluation of bitterness.Item Bitterness Score and its Correlation to Drug Concentration: An Approach for Estimating Bitterness Suppression in a Marketed Product of Ofloxacin(Bentham Science, 2015) Jadhav, Hemant R.In vitro approaches for assessing taste characteristics of taste masked drug and drug products are useful in reducing reliance on human panel tests. In this study, taste panel studies were used to determine bitterness threshold and bitterness score of various solutions of ofloxacin followed by correlation and the application of this approach in estimating bitterness suppression. Bitterness scores for different solutions of ofloxacin were estimated by trained human volunteers of a taste panel. Bitterness scores were correlated to ofloxacin concentration followed by determination of bitterness scores for various dissolution samples obtained from in vitro drug release study of ofloxacin taste masked drug product. Concentration of 80 µg/ml and below was perceived bitterless by all the volunteers of taste panel. A third order polynomial equation (y=13.51x3-91.08x2+206.7x-156.6; R2 = 0.973) was derived as a relationship between bitterness score (y) and log ofloxacin concentration (x). Marketed taste masked product achieved concentrations below bitterness threshold in in vitro drug release studies performed in pharmacopoeial apparatus at initial time points (0-5 min). Bitterness threshold and bitterness scores are helpful in estimating bitterness of ofloxacin solutions provided suitable correlation has been found between them. The suggested approach, which is applicable to any bitter or objectionable tasting drug, has potential to be used as analytical tool in formulation development and quality control.Item Design, Synthesis and In Vitro Evaluation of Piperazine Incorporated Novel Anticancer Agents(Bentham Science, 2018) Jadhav, Hemant R.Novel 4-(3-(4-ethylpiperazin-1-yl)propoxy)-N-phenylbenzamide derivatives (C-1 to C-10) and (4-(3-(4-ethylpiperazin-1-yl)propoxy)phenyl)(4-(2-methoxyphenyl)piperazin-1- yl)ethanone derivatives (C-11 to C-16) were designed and synthesized by pharmacophore approach.
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