Government Model Science College

Jabalpur, India

Government Model Science College

Jabalpur, India
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Agrawal R.,Government Model Science College | Jain P.,Government Model Science College | Dikshit S.N.,Government Model Science College
Mini-Reviews in Medicinal Chemistry | Year: 2012

Balaglitazone (DRF-2593) is a novel partial agonist of PPAR-gamma (γ), which is developed by Dr. Reddy's laboratories India. Balaglitazone is a second generation peroxisome proliferator-activated receptor (PPAR) gamma agonist with only partial agonistic properties. Balaglitazone is currently being evaluated in phase III clinical trial in United States and Europe. Selective PPAR-γ modulators bind in distinct manners to the ligand-binding pocket of PPAR-γ, leading to alternative receptor conformations, differential cofactor recruitment/displacement, differential gene expression, and ultimately differential biological responses. Based on this concept, new and improved novel antidiabetic agents are in current development. Clinical studies conducted with 409 subjects of randomized, double blind, parallel-group placeboand active comparator-controlled subject groups to determine the efficacy and safety of Balaglitazone. The study showed that the trial met its primary endpoint. Balaglitazone treated groups shown significantly reduce of HbA1c (%), FSG (mmol/L), postprandial glucose as comparison to pioglitazone. Phase III clinical studies data clearly shows that Balaglitazone provides robust glycemic control as an add-on to insulin therapy. Balaglitazone 10mg and 20mg show the similar magnitudes of the effects which comparable to the effects seen in the pioglitazone 45mg group. The incidence of fluid retention and fat accumulation fewer than those observed with pioglitazone 45mg. Hence, Balaglitazone is prominent candidate of new glitazone which requires fewer doses as comparison pioglitazone and shows better safety profile less incidence of special adverse effect like heart failure, peripheral oedema, and myocardial infarction. Unlike other marketed PPAR gamma agonists, Balaglitazone shows less fluid retention, less heart enlargement and no reduction of bone formation than full PPAR gamma agonists in preclinical studies. In present review, we have tried to cover classification PPARs various ligands, chemistry, physical properties, commercial synthesis, current patent status, polymorphic information, receptor interaction, pharmacophore rational, mechanism, adverse effect and clinical status of Balaglitazone, giving emphasis on medicinal chemistry aspect. © 2012 Bentham Science Publishers.

Dubey V.,Bhilai Institute of Technology | Tiwari N.,Government Model Science College
AIP Conference Proceedings | Year: 2016

Behavior displayed by europium doped AZrO3 phosphor which was synthesized by solid state reaction method. For synthesis of BaZrO3, SrZrO3 and CaZrO3 phosphor with fixed concentration of europium ion was calcination at 1000°C and sintered at 1300°C following intermediate grinding. Synthesized sample was characterized by X-ray diffraction analysis and crystallite sized was calculated by Scherer's formula. From PL spectra of prepared phosphors shows intense emission centred at 612nm (red emission) with high intensity for SrZrO3:Eu3+. For europium doped BaZrO3 and CaZrO3 (613nm) phosphor shows less intense PL spectra as compared to SrZrO3:Eu3+. The strong emission peak of AZrO3:Eu3+ phosphor is due to forced electric dipole transition of 5D0 to 7F2 centered at 612 and 613nm. It is characteristic red emission for europium ion. The excitation spectra of AZrO3:Eu3+ phosphor mainly consists of the charge transfer and (CTB) of Eu3+ located in 200-350nm centred at 254nm. The present phosphors can act as single host for red light emission in display devices. The CIE coordinates were calculated by Spectrophotometric method using the spectral energy distribution of the AZrO3:Eu3+ sample. © 2016 Author(s).

Agrawal R.,Government Model Science College | Bahare R.S.,Birla Institute of Technology | Jain P.,Government Model Science College | Dikshit S.N.,Government Model Science College | Ganguly S.,Birla Institute of Technology
Mini-Reviews in Medicinal Chemistry | Year: 2012

Alogliptin (codenamed SYR-322) is a recently approved anti-diabetic drug in Japan, which has been under clinical development phase III in USA and Europe. Alogliptin has been developed by Takeda under the brand name "Nesina". Alogliptin is a highly selective (> 10,000-time selectivity, potent, reversible and durable serine protease dipeptidyl peptidase IV enzyme is compared to DPP-8 and DPP-9) inhibitor, which has been developed as an alternative second-line to metformin in place of a sulphonylurea. Alogliptin has been observed to increase and prolong the action of incretin hormone by inhibiting the DPP-IV enzyme activity. Alogliptin has been observed to well absorb and show low plasma protein binding, which displays slow-binding properties to DPP-IV enzyme. The X-ray crystallography studies have been revealed that Alogliptin binds to DPP-IV active site by non-covalently and provides sustained reduction of plasma DPP-IV activity as well as lowering of blood glucose, in drug-naive patients with T2DM and inadequate glycemic control, once daily oral dosing regimen with varying levels of doses ranging from 25-800 mg. Alogliptin is approved as monotherapy and in combination with alpha-glucosidase & thiazolidinediones. The 26 week clinical study of Alogliptin revealed that Alogliptin doesn't increase the weight and well tolerated. In the present review, we have tried to cover biology of DPP-IV, molecular chemistry, chemical characterization, crystal polymorphic information, interaction studies, commercial synthesis, current patent status, adverse effects and clinical status of Alogliptin giving emphasis on the medicinal chemistry aspect. © 2012 Bentham Science Publishers.

Kumar S.,Jamia Hamdard University | Agrawal R.,Government Model Science College
Recent Patents on Anti-Cancer Drug Discovery | Year: 2014

Afatinib is a recently introduced new tyrosine kinase inhibitor, approved by the USFDA on July 12, 2013. Afatinib is marketed under the trade name Gilotrif and developed by Boehringer Ingelheim GmbH. It is indicated for the first-line treatment of patients with metastatic non-small cell lung cancer (NSCLC) carrying EGFR exon 19 deletions or exon 21 (L858R) mutations. Afatinib is a covalent, irreversible inhibitor of epidermal growth factor receptor (EGFR), human epidermal growth factor receptor 2 (HER2) and HER4. Chemically afatinib is a 4-anilinoquinazoline derivative, having an acrylamide warhead. Gilotrif is the formulation of Afatinib di-meleate salt. Presently, afatinib has been approved in the USA, the European Union, Taiwan and Mexico. In this review, we have summarized the chemical characterization of afatinib, its synthesis, patent status, marketed formulation, available crystalline form and current clinical trials. © 2014 Bentham Science Publishers.

Agrawal R.,Government Model Science College
Current Drug Targets | Year: 2014

The new chemical entity (NCE) has been knocked as novel antidiabetic agent, e.g. Saroglitazar. Saroglitazar is a drug for the treatment of Type II diabetes. Saroglitazar is marketed under the trade name Lipaglyn, developed by the Zydus Cadila. Lipaglyn is the first indigenously developed NCE by any Indian pharmaceutical company, ever. Lipaglyn has been approved for the treatment of Type II diabetes by the Drug Controller General of India in June 2013. Lipaglyn is indicated for the patients suffering from diabetes dyslipidemia. It also provides the option of a once-daily oral therapy. Saroglitazar regulates the lipid parameters as well as glycemic control. The present article describes Saroglitazar with its chemical synthesis and patent status with its summary of clinical studies. © 2014 Bentham Science Publishers.

Thomas V.,Trinity College Dublin | Bajpai M.,Government Model Science College | Bajpai S.K.,Government Model Science College
Journal of Industrial Textiles | Year: 2011

This work involves chemical modification of cotton fabrics by natural, biocompatible, and biodegradable polysaccharide - chitosan - followed by incorporating silver nanoparticles in the fabrics. The excellent chelating property of chitosan binds the silver metal ions that are later on reduced to nanoparticles giving rise to chitosan-attached nanosilver-loaded fabrics. The silver nanoparticles-loaded chitosan-attached fabric has been characterized by surface plasmon resonance, transmission electron microscopy, energy dispersive X-ray analysis, and X-ray diffraction analysis. These chitosan-attached nanosilver-loaded fabrics exhibit excellent antibacterial action against model bacteria E. coli. © The Author(s), 2011.

Agrawal R.,Government model science college | Jain P.,Government model science college | Dikshit S.N.,Government model science college
Current Drug Targets | Year: 2012

Chemically, methylxanthine nucleus based Linagliptin (BI-1356, BI-1356-BS) is a dipeptidyl peptidase-IV inhibitor, which has been developed by Boehringer Ingelheim in association with Lilly for the treatment of Type-II Diabetes. Linagliptin was marketed by Lilly under the trade name Tradjenta and Trajenta. Linagliptin was approved as the once-daily dose by USFDA on 2 May 2011, for the treatment of Type-II Diabetes. Linagliptin 5mg once daily dose was approved based on a clinical trial program, which was conducted on approximately 4,000 adults with Type-II Diabetes. Linagliptin demonstrated statistically significant mean difference in HbA1c from placebo of up to 0.72 percent, when it was used monotherapically. In patients, who were not adequately controlled on metformin or metformin plus sulphonylurea, the addition of Linagliptin resulted in a statistically significant mean difference in HbA1c from placebo of -0.6 percent. Linagliptin was observed to produce significant reduction in fasting plasma glucose (FPG) compared to placebo, when used as a monotherapy in combination with metformin, sulfonylurea and/or pioglitazone. Linagliptin demonstrated significant reduction post-prandial glucose (PPG) levels in two hours as compared with placebo in monotherapy as well as in combination with metformin. In vitro assays also anticipated that Linagliptin is a potent DPPIV inhibitor as well as it exhibits good selectivity for DPP-IV as compared with other DPPs. The in-vivo studies also demonstrated same anticipation with respect to Linagliptin. Consequently, increasing the GLP-1 levels so far improved glucose tolerance in both healthy animals. X-ray crystallography anticipates that Linagliptin complexes with human DPPIV enzyme, e.g. butynyl substituent occupies the S1 hydrophobic pocket of the enzyme; the aminopiperidine substituent in the xanthine scaffold occupies the S2 subsite and its primary amine interacts with the key amino acid residues, which involves in the recognition of peptide substrates. In the present review, we have tried to cover comparative study of DPPIV inhibitors, chemistry, physical properties, commercial synthesis, patent portfolio, crystalline polymorphic forms of Linagliptin and its receptor interaction, Pharmacophore rational, mechanism, clinical studies, preclinical, adverse effect, available formulations, dose regimen, co-therapy of Linagliptin, giving emphasis on the medicinal chemistry aspects. © 2012 Bentham Science Publishers.

Sharma V.,Government Model Science College
Russian Journal of Herpetology | Year: 2014

The distribution of Elachistodon westermanni, Indian Egg Eater is expanded by adding of two more localities in currently known distribution. Occurrence in Punjab extends its northernmost point with first record for the state. © 2014 Folium Publishing Company.

Pandey S.K.,Government Model Science College
Indian Journal of Physics | Year: 2012

An extension of the theory of optical emission spectra due to exciton-exciton collisions (in bulk GaAs at nonzero temperatures) for GaAs/AlGaAs quantum well systems has been attempted to understand the physics associated with the optical spectra due to excitonic scattering processes in these novel systems. The four typical processes have been considered to give different spectral shape, peak position, and temperature dependence of the emission spectra. The intensity of emitted light in quantum well systems varies inversely to the square of temperature, whereas in case of bulk materials it simply decreases with the temperature. The results arrived at are purely qualitative in nature. © 2012 IACS.

Awasthi S.K.,Government Model Science College | Bajpai S.K.,Government Model Science College | Dubey A.,Government Model Science College
Polymer - Plastics Technology and Engineering | Year: 2012

The solution cast technique for the preparation of polymer blends of poly(ethylmethacrylate) (PEMA) and poly(ethylene oxide)(PEO) is described. Polymer blends of poly(ethylmethacrylate) (PEMA) and poly(ethylene oxide) (PEO) with different weight percentage ratio of the two polymers have been prepared. Effect of thermal pretreatments like annealing and quenching on the mechanical properties of polymer blends of PEMA and PEO have been reported using Vicker's microhardness testing. The thermal pretreatment produces morphological changes in the blend system investigated. These thermal pretreatments results in hardening and softening of blend systems under investigation. © 2012 Copyright Taylor and Francis Group, LLC.

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