Piyush Trivedi

Publications of Piyush Trivedi

• Synthesis, in silico metabolic and toxicity prediction of some novel imidazolinones derivatives as potent anticonvulsant agents.

  Authors: N S Hari Narayana Moorthy, Vipin Saxena, C Karthikeyan, Piyush Trivedi

  Journal of enzyme inhibition and medicinal chemistry. 06/2011; 27(2):201-7.

  A series of 1,2,4-trisubstituted 5-imidazolinone derivatives were synthesized by Erlenmeyer condensation of benzoylglycine (hippuric acid) with different aldehydes in the presence of sodium acetateA series of 1,2,4-trisubstituted 5-imidazolinone derivatives were synthesized by Erlenmeyer condensation of benzoylglycine (hippuric acid) with different aldehydes in the presence of sodium acetate and acetic anhydride. The derivatives of the compounds were prepared by condensation of some known sulpha drugs with 5-oxazolone derivatives. The anticonvulsant activity of the compounds was determined by the protection of pentylenetetrazole-induced convulsions that was ranged from 10 to 60%. The compounds with p-OCH(3), p-OH and o-Cl substitutions in the phenyl ring on 4(th) position of the imidazolinone ring exhibited good anticonvulsant activity. In silico metabolic and toxicity studies showed that all the compounds in the series are not likely to exhibit toxicity except the compounds IIIa, IIIb, VIa and VIb, that is predicted to show 29% mutagenicity and 53% irritation in comparison to the other compounds. The predicted lethal effect and hERG toxicity of the compounds showed that IIa, IVa, Va and Vb might be toxic at higher concentrations. The results successfully establish the synthesized imidazolinone derivatives as novel compounds with anticonvulsant properties, low predicted cardiotoxicity and lethal effects thus can be promising leads for further development as novel anticonvulsants.

• Reduction in cisplatin genotoxicity (micronucleus formation) in non target cells of mice by protransfersome gel formulation used for management of cutaneous squamous cell carcinoma.

  Authors: Vandana Gupta, Ramesh Chandra Agrawal, Piyush Trivedi

  Acta pharmaceutica (Zagreb, Croatia). 03/2011; 61(1):63-71.

  Cisplatin-loaded protransfersome system was prepared and characterized for in vitro drug permeation, drug deposition and antitumor effect. A histopathological study and a genotoxicity study were alsoCisplatin-loaded protransfersome system was prepared and characterized for in vitro drug permeation, drug deposition and antitumor effect. A histopathological study and a genotoxicity study were also done. The skin permeation data of cisplatin from protransfersome gel formulation revealed 494.33 ± 11.87 μg cm-2, which was significantly higher than that from the control plain drug solution in 0.9 % NaCl (p < 0.001). Untreated group of animals showed invasive moderately differentiated keratinizing squamous cell carcinoma (malignant stage). However, with cisplatin loaded protransfersome gel system simple epithelial hyperplasia (pre-cancerous stage) with no cancerous growth was observed. Also, a significant induction in micronucleus formation was found in the group that was treated with injectable intraperitoneal cisplatin preparation in 0.9 % saline as compared to the group treated with topical protransfersome gel formulation. The findings of this research work appear to support improved, site-specific and localized drug action in the skin, thus providing a better option for dealing with skin related problems like squamous cell carcinoma.

• Synthesis of Some Coumarinyl Chalcones and their Antiproliferative Activity Against Breast Cancer Cell Lines

  Authors: Kuldeep Patel, Chandrabose Karthikeyan, Viswas Raja Solomon, N.S. Hari Narayana Moorthy, Hoyun Lee, Kapendra Sahu, Girdhar Singh Deora, Piyush Trivedi

  Letters in Drug Design &amp Discovery. 01/2011; 11(8):308.

  Abstract: A series of coumarinyl chalcones derivatives were synthesized and evaluated for their antiproliferative activities on three different breast cancer cell lines (MDA-MB231, MDA-MB468, MCF7)Abstract: A series of coumarinyl chalcones derivatives were synthesized and evaluated for their antiproliferative activities on three different breast cancer cell lines (MDA-MB231, MDA-MB468, MCF7) and one non-cancer breast epithelial cell line (184B5). The coumarinyl derivatives exhibited anticancer activity against breast cancer cell lines at a micromolar range. A structure-activity relationship (SAR) analysis was performed by studying the effect of substituents on their antiproliferative activities. One of the compound 3i bearing methoxy substitutions at the R1, R2 and R3 positions of the phenyl ring showed comparable potency to the reference drug cisplatin as well as a two-fold higher selectivity for the breast cancer cell lines than 184B5 cells.

• Design, Synthesis and Biological Evaluation of Some Novel 3-Cinnamoyl-4-Hydroxy-2H-Chromen- 2- ones as Antimalarial Agents

  Authors: Kuldeep Patel, Karthikeyan Chandrabose, N.S. Hari Narayana Moorthy, Girdhar Singh Deora, Kapendra Sahu, Piyush Trivedi

  Medicinal Chemistry Research. 01/2011;

  A novel series of 3-cinnamoyl-4-hydroxy-2Hchromen-2-ones were designed, synthesized and screened for antiplasmodial activity. Eleven compounds of the series exhibited micromolar potency againstA novel series of 3-cinnamoyl-4-hydroxy-2Hchromen-2-ones were designed, synthesized and screened for antiplasmodial activity. Eleven compounds of the series exhibited micromolar potency against chloroquine sensitive and chloroquine resistant strains. The most potent compound 4-hydroxy-3-(3-(4-nitrophenyl) acryloyl) -2Hchromen- 2-one showed inhibitory potency (IC50) of 3.1 and 4 lg/ml against chloroquine sensitive and chloroquine resistant strains, respectively. A structure activity relationship study was performed by correlating the effect of substituents with the antimalarial activity of the title compounds. The novel 3-cinnamoyl-4-hydroxy-2H-chromen- 2-ones reported here should be good lead for further development of antimalarial agents that can overcome resistance.

• Coumarinyl Chalcones and their Antiproliferative Activity Against Breast Cancer Cell Lines

  Authors: Kuldeep Patel, Chandrabose Karthikeyan, Viswas Raja Solomon, N. S. Hari Narayana Moorthy, Hoyun Lee, Kapendra Sahu, Girdhar Singh Deora, Piyush Trivedi

  Letters in Drug Design &amp Discovery. 01/2011; 8:308.

  A series of coumarinyl chalcones derivatives were synthesized and evaluated for their antiproliferative activities on three different breast cancer cell lines (MDA-MB231, MDA-MB468, MCF7) and oneA series of coumarinyl chalcones derivatives were synthesized and evaluated for their antiproliferative activities on three different breast cancer cell lines (MDA-MB231, MDA-MB468, MCF7) and one non-cancer breast epithelial cell line (184B5). The coumarinyl derivatives exhibited anticancer activity against breast cancer cell lines at a micromolar range. A structure-activity relationship (SAR) analysis was performed by studying the effect of substituents on their antiproliferative activities. One of the compound 3i bearing methoxy substitutions at the R1, R2 and R3 positions of the phenyl ring showed comparable potency to the reference drug cisplatin as well as a two-fold higher selectivity for the breast cancer cell lines than 184B5 cells.

• Synthesis of Some Coumarinyl Chalcones and their Antiproliferative Activity against Breast Cancer Cell Lines

  Authors: Kuldeep Patel, Chandrabose Karthikeyan, Viswas Raja Solomon, N.S. Hari Narayana Moorthy, Hoyun Lee, Kapendra Sahu, Girdhar Singh Deora, Piyush Trivedi

  Letters in Drug Design & Discovery. 01/2011; 8:323-327.

• Synthesis of Some Coumarinyl Chalcones and their Antiproliferative Activity Against Breast Cancer Cell Lines

  Authors: Kuldeep Patel, Chandrabose Karthikeyan, Viswas Raja Solomon, N.S. Hari Narayana Moorthy, Moorthy, Hoyun Lee, Kapendra Sahu, Girdhar Singh Deora, Piyush Trivedi

  Letters in Drug Design & Discovery. 01/2011; 8:308-311.

  A series of coumarinyl chalcones derivatives were synthesized and evaluated for their antiproliferative activities on three different breast cancer cell lines (MDA-MB231, MDA-MB468, MCF7) and oneA series of coumarinyl chalcones derivatives were synthesized and evaluated for their antiproliferative activities on three different breast cancer cell lines (MDA-MB231, MDA-MB468, MCF7) and one non-cancer breast epithelial cell line (184B5). The coumarinyl derivatives exhibited anticancer activity against breast cancer cell lines at a micromolar range. A structure-activity relationship (SAR) analysis was performed by studying the effect of substituents on their anti-proliferative activities. One of the compound 3i bearing methoxy substitutions at the R1, R2 and R3 positions of the phenyl ring showed comparable potency to the reference drug cisplatin as well as a two-fold higher selectivity for the breast cancer cell lines than 184B5 cells.

• Modeling VEGFR kinase inhibition of aminopyrazolopyridine urea derivatives using topological and physicochemical descriptors: a quantitative structure activity analysis study

  Authors: Ashutosh Kumar Pandey, Omprakash Tanwar, Girdhar Singh Deora, Chandrabose Karthikeyan, N. S. Hari Narayana Moorthy, Piyush Trivedi

  Medicinal Chemistry Research. 01/2011;

  A QSAR study has been performed on a series of aminopyrazolopyridine urea derivatives with potent VEGFR kinase inhibitory activity. Structural features responsible for the activity of the compoundsA QSAR study has been performed on a series of aminopyrazolopyridine urea derivatives with potent VEGFR kinase inhibitory activity. Structural features responsible for the activity of the compounds were characterized by using physicochemical, topological, and electrotopological descriptors, calculated from the Molecular Design Suite software (V-life MDSTM 3.5). Correlations between the inhibitory activities (KDR and KDRcell) of aminopyrazolopyridine urea derivatives and the calculated descriptors were established through simulated annealing method. The best QSAR models generated from the study explain 89 and 88% of the variation in KDR and KDRcell inhibitory activities, respectively. Internal and external validation methods were used to evaluate the predictive capacity of the generated models. The significant cross-validated correlation coefficient (Q2[0.6) and other statistical parameters suggest that the models exhibited considerable predictivity. The generated QSAR models divulge that factors related to lipophilicity and topological state of atoms in the molecule influences KDR and KDRcell inhibitory activities of aminopyrazolopyridine urea derivatives.

• Preparation and evaluation of tubular micelles of pluronic lecithin organogel for transdermal delivery of sumatriptan.

  Authors: Varsha Agrawal, Vandana Gupta, Suman Ramteke, Piyush Trivedi

  AAPS PharmSciTech. 12/2010; 11(4):1718-25.

  The present work focuses on the preparation and evaluation of lecithin organogel system of thermoreversible polymer pluronic F127, which would enhance the stability and absorption of sumatriptanThe present work focuses on the preparation and evaluation of lecithin organogel system of thermoreversible polymer pluronic F127, which would enhance the stability and absorption of sumatriptan succinate across the skin. Formulations were developed with and without co-surfactant (pluronic F127). The prepared organogels were evaluated for its appearance, organoleptic characteristics, and feel upon application, homogeneity, occlusivenes, washability, pH, viscosity, spreadability, gel transition temperature of formulations. The formulations were also evaluated for drug content, in vitro drug diffusion properties and skin irritation testing. In vivo evaluation of formulations was carried out by hot plate and writhing test method, and finally the optimized formulation was subjected to stability studies. The developed formulations were easily washable, smooth in feel, and showed no clogging which indicate superior texture of system. Formulation, containing pluronic showed greater spreadability and higher drug diffusion rate as compared to pluronic free organogel. Drug content of organogel formulations was in the range of 94-97%. The pH of the formulations was 6.48 ± 0.5 and 6.98 ± 0.1, reflecting no risk of skin irritation. Pluronic not only enhances the stability of organogel by increasing the viscosity (from 6,541 ± 234.76 to 7,826 ± 155.65 poise) but also increases the release of drug from 67.39 ± 1.53% to 74.21 ± 1.7%. The sumatriptan exhibits higher and long lasting antinociceptive effect as indicated by the persistent increase in reaction time in hot plate and inhibited abdominal contraction in acetic acid-induced writhing test (p < 0.05). The prepared optimized formulation was found to be stable without any significant changes at room temperature.

• 3D QSAR of aminophenyl benzamide derivatives as histone deacetylase inhibitors.

  Authors: Mahipal, Om Prakash Tanwar, C Karthikeyan, N S Hari Narayana Moorthy, Piyush Trivedi

  Medicinal chemistry (Shāriqah (United Arab Emirates)). 10/2010; 6(5):277-85.

  The article describes the development of a robust pharmacophore model and the investigation of structure activity relationship analysis of 48 aminophenyl benzamide derivatives reported for HistoneThe article describes the development of a robust pharmacophore model and the investigation of structure activity relationship analysis of 48 aminophenyl benzamide derivatives reported for Histone Deacetylase (HDAC) inhibition using PHASE module of Schrodinger software. A five point pharmacophore model consisting of two aromatic rings (R), two hydrogen bond donors (D) and one hydrogen bond acceptor (A) with discrete geometries as pharmacophoric features was developed and the generated pharmacophore model was used to derive a predictive atom-based 3D QSAR model for the studied dataset. The obtained 3D QSAR model has an excellent correlation coefficient value (r(2)=0.99) along with good statistical significance as shown by high Fisher ratio (F=631.80). The model also exhibits good predictive power confirmed by the high value of cross validated correlation coefficient (q(2) = 0.85). The QSAR model suggests that hydrophobic character is crucial for the HDAC inhibitory activity exhibited by these compounds and inclusion of hydrophobic substituents will enhance the HDAC inhibition. In addition to the hydrophobic character, hydrogen bond donating groups positively contributes to the HDAC inhibition whereas electron withdrawing groups has a negative influence in HDAC inhibitory potency. The findings of the QSAR study provide a set of guidelines for designing compounds with better HDAC inhibitory potency.

• A new approach for PEGylation of dendrimers.

  Authors: Hemant Khambete, Surya P Gautam, C Karthikeyan, Suman Ramteke, N S Hari Narayana Moorthy, Piyush Trivedi

  Bioorganic & medicinal chemistry letters. 07/2010; 20(14):4279-81.

  Dendrimers have emerged as one of the most interesting themes for researchers as a result of unique functional architecture and macromolecular characteristics. The reported methods of PEGylation areDendrimers have emerged as one of the most interesting themes for researchers as a result of unique functional architecture and macromolecular characteristics. The reported methods of PEGylation are very time consuming and required multisteps for synthesis. In present work we have synthesized PEGylated polyamidoamine (PAMAM) dendrimers using epichlorohydrin as a linker. The PEGylated dendrimers were evaluated for color reaction UV, IR and NMR studies and compared with standard data.

• Design, synthesis, cytotoxic evaluation, and QSAR study of some 6H-indolo[2,3-b]quinoxaline derivatives.

  Authors: N S Hari Narayana Moorthy, C Karthikeyan, Piyush Trivedi

  Journal of enzyme inhibition and medicinal chemistry. 03/2010; 25(3):394-405.

  In the pathway of anticancer drug development, we designed and synthesized some 6H-indolo[2,3-b]quinoxaline derivatives (which act as DNA intercalators) by structural modification. The structure ofIn the pathway of anticancer drug development, we designed and synthesized some 6H-indolo[2,3-b]quinoxaline derivatives (which act as DNA intercalators) by structural modification. The structure of the 6H-indolo[2,3-b]quinoxaline derivatives was confirmed by IR, NMR, Mass and elemental analysis. The compounds (IDQ-5, IDQ-10, IDQ-11, IDQ-13, and IDQ-14) exhibited significant in vitro activity against a human leukemia (HL-60) cell line. The QSAR derived for modeling the cytotoxic activity of 6H-indolo[2,3-b]quinoxaline derivatives suggests that candidate structures for increased cytotoxic potency should incorporate cyclic substituents or substituents with primary carbon atoms.

• 2D QSAR modeling of 1, 3, 4-oxadiazole derivatives as novel inhibitors of Glycogen synthase kinase-3β

  Authors: Girdhar Singh Deora, Blessy Joseph, C. Karthikeyan, Piyush Trivedi

  National conference on Cellular and Molecular Medicine, Bhopal, India; 01/2010

  A QSAR analysis of 1, 3, 4-oxadiazole derivative S derivatives has been performed to establish mathematical/functional relationship between the chosen activity and selected properties of theA QSAR analysis of 1, 3, 4-oxadiazole derivative S derivatives has been performed to establish mathematical/functional relationship between the chosen activity and selected properties of the congeneric series of compounds. This study would further help in designing of new inhibitors of glycogen synthase kinase-3β.

• RP-HPLC Method for Estimation and Stability Study of Drotaverine HCl as per ICH Guidelines

  Authors: Prafull Tailor, Kapendra Sahu, Kuldeep Patel, C Karthekeyan, N.S. Hari Narayana Moorthy, Mahipal, Blessy Joseph, Piyush Trivedi

  Latin American journal of pharmacy. 01/2010;

• Design,synthesis,biological evaluation and molecular modelling studies of some coumarin based antimalarial agents

  Authors: Kuldeep patel.c.karthikeyan, N S Hari Narayana moorthy, Girdhar singh Deora, Piyush Trivedi

  4th International conference on Recent advances in cardiovascular sciences, DIPSAR, NEW DELHI; 01/2010

• Development of a validated stability indicating ultra-performance liquid chromatographic assay method for Gemcitabine hydrochloride according to ICH guidelines

  Authors: Blessy Joseph, C. Karthikeyan, Girdhar Singh Deora, Pratibha Patel, Kapendra Sahu, Piyush Trivedi

  Recent Advances in Cardiovascular Sciences, New Delhi; 01/2010

• Development and Validation of a RP-HPLC Method for Determination of Citicoline Monosodium in Human Plasma

  Authors: Shailendra Kumar Bindaiya, Kapendra Sahu, Kuldeep Patel, C. Karthikeyan, Farhad Firoze Mehta, Piyush Trivedi

  Latin American journal of pharmacy. 01/2010;

• Development and validation of stability indicating assay method for Salmeterol by UPLC

  Authors: Pratibha Patel, Kapendra Sahu, Kuldeep Patel, Blessy Joseph, C. Kartikeyan, Piyush Trivedi

  Latin American journal of pharmacy. 01/2010;

• Study of Forced Degradation Behaviour of Eprosartan Mesylate and Development of Validated Stability Indicating Assay Method by UPLC

  Authors: Pratibha Patel, Kapendra Sahu, Kuldeep Patel, C. Kartikeyan, Piyush Trivedi

  Latin American journal of pharmacy. 01/2010;

• QSAR Analysis of Some Amino Substituted Pyrido[3,2b]pyrazinones as Potent and Selective PDE-5 Inhibitors

  Authors: Omprakash Tanwer, Kuldeep Patel, N.S H N Moorthy, Piyush Trivedi

  International journal of Pure and Applied Chemistry. 01/2010; 5(4):269-276.