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.
Agrawal R.,Government Model Science College |
Jain P.,Government Model Science College |
Dikshit S.N.,Government Model Science College
Current Drug Targets | Year: 2012
Apixaban (BMS-562247-01) is a compound being investigated as an anticoagulant. Apixaban molecule is developed in a joint venture by Pfizer and Bristol-Myers Squibb. Apixaban, a coagulation factor Xa inhibitor, approved in the E.U. in 2011 for the prevention of venous thromboembolic events in adult patients, who have undergone elective hip or knee replacement. The Apixaban based drug will be marketed under the brand name Eliquis® and is expected to rack up annual sales of over $2.5 billion. Apixaban is expected to provide stiff competition to warfarin, a popular blood thinner used in Europe. Warfarin is known to cause some serious side effects in patients. Apixaban, as compared with aspirin, reduced the risk of stroke or systemic embolism in patients experiencing atrial fibrillation by more than 50% (from 3.7% per annum with aspirin to 1.6% per annum with apixaban). Apixaban exhibits superiority to enoxaparin in preventing thrombosis in patients undergoing elective hip replacement surgery with similar bleeding rates. Apixaban is a highly selective and potent Factor Xa Inhibitor with Ki=0 8nM to both free as well as prothrombinase bound FXa. In X-ray crystal structure studies indicate that the pyrazole N-2 nitrogen atom interacts with backbone of Gln192 and the carbonyl oxygen of carboxamide interacts with NH of Gly216. The orientation of phenyllactum in the S4 region indiacates an edge to face interaction with Trp215, which is positioned between the Tyr99 and Phe174. In the present review, we have tried to cover comparative study of various FXa-inhibitors and point out apixaban in the various aspect including molecular chemistry, physical properties, commercial synthesis, current patent status, crystalline polymorphic forms, molecular receptor interaction, pharmacophore rational, mechanism of action, clinical studies, preclinical, adverse effect, available formulation, dose regimen and co-therapy, thus giving emphasis on 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.
Bajpai A.,Government Model Science College |
Tripathi N.,Government Model Science College
Procedia Engineering | Year: 2014
The hybrid nanocomposite was prepared by in situ intercalative polymerization of acrylamide in a fine dispersion of the sugarcane bagasse, chitin and fuller's earth by microwave irradiation. The product was very efficient as an adsorbent for metal ions and organic dye. It was mechanically stable in wet condition, resistant to fast microbial attack and released no leachates. © 2013 The Authors. Published by Elsevier Ltd.
Tiwari R.K.,Government Model Science College |
Singh R.,Government Model Science College
International Journal of Theoretical Physics | Year: 2015
We have analyzed a new class of spatially homogeneous and anisotropic Bianchi type-V cosmological models with perfect fluid distribution in presence of time varying cosmological and gravitational constants in the framework of general relativity. Exact solutions of Einstein’s field equations are obtained for two types of cosmologies viz. m ≠ 3 and m = 3 respectively. We propose an alternate variation law in which the anisotropy (σ/θ) per unit expansion scalar (θ) is proportional to a function of scale factor R i.e. (Formula presented.) (where σ is a shear scalar) Tiwari (The African Review of Physics, 8, 437–447 2013). Physical properties of the models are discussed in detail. The models isotropize at late times. Some cosmological distance parameters for both the models have also been presented. We also discussed state finder parameters and observe that our solutions favor ΛCDM model. © 2014, Springer Science+Business Media New York.