Rational design and synthesis of new tetralin-sulfonamide derivatives as potent anti-diabetics and DPP-4 inhibitors: 2D & 3D QSAR, in vivo radiolabeling and bio distribution studies

2018 ◽  
Vol 81 ◽  
pp. 481-493 ◽  
Author(s):  
Somaia S. Abd El-Karim ◽  
Manal M. Anwar ◽  
Yasmin M. Syam ◽  
Manal A. Nael ◽  
Hanan F. Ali ◽  
...  
Keyword(s):  
Rational Design ◽  
3D Qsar ◽  
Design And Synthesis ◽  
Distribution Studies

Design and Synthesis of IMR-23, an Oxime Derived from Nitroimidazole as an Immunomodulatory Molecule

2020 ◽  
Vol 17 (4) ◽  
pp. 324-332
Author(s):  
Esmeralda Sánchez-Pavón ◽  
Aracely López-Monteon ◽  
Delia Hernández-Romero ◽  
María de la Soledad Lagunes-Castro ◽  
Dxinegueela Yolanda Zanatta-García ◽  
...  
Keyword(s):  
Rational Design ◽  
Condensation Reaction ◽  
Vero Cells ◽  
Design And Synthesis ◽  
Cytokines And Chemokines ◽  
Sulforhodamine B ◽  
Sulforhodamine B Assay ◽  
Proper Balance

Background: Adjuvants have been obtained empirically by trial and error experiments and today, there is a tendency to the rational design of adjuvants candidates, which will increasingly achieve effective and safe products. The aim of this work was to design and evaluate the compound IMR-23 derived from nitroimidazole as an immunomodulatory molecule. Material and Methods: The IMR-23 molecule was obtained by a condensation reaction, cytotoxicity was tested by the sulforhodamine B assay. Adjuvanticity was evaluated in vivo and in vitro in J774A.1 cells and in the mouse model, respectively. Results: IMR-23 that did not show cytotoxicity on HeLa, Vero cells and macrophages J774A.1, was able to induce the production of molecules involved in the inflammatory process, such as cytokines and chemokines determined by ELISA, to induce the production of antibodies and to generate antigenspecific cells to ovalbumin and against the antigen GST-L1b. Conclusions: These results open the possibility of further studies to obtain a proper balance of immunogenicity- toxicity in the use of IMR-23 as an adjuvant molecule.

scholarly journals Rational Design and Synthesis of a Novel Membrane Binding NaV1.8 Selective Inhibitor with in vivo Activity in Pain Models

2016 ◽  
Vol 110 (3) ◽  
pp. 33a
Author(s):  
Christina I. Schroeder ◽  
Jennifer Deuis ◽  
Sonia Troeria Henriques ◽  
Zoltan Dekan ◽  
Marco Inserra ◽  
...  
Keyword(s):  
Rational Design ◽  
Membrane Binding ◽  
Selective Inhibitor ◽  
Design And Synthesis ◽  
Pain Models

Effects of Preloading of Stannous Compounds on the Distribution of 99mTc-Pertechnetate

1977 ◽  
Vol 16 (01) ◽  
pp. 26-29 ◽  
Author(s):  
D. D. Greenberg ◽  
P. Som ◽  
G. E. Meinken ◽  
D. F. Sacker ◽  
H. L. Atkins ◽  
...  
Keyword(s):  
Blood Cell ◽  
Red Blood Cell ◽  
Plasma Ratio ◽  
99Mtc Pertechnetate ◽  
Time Period ◽  
Stannous Ion ◽  
Distribution Studies

Summary 99mTc-pertechnetate distribution studies were performed in rabbits and mice following pretreatment between 5—336 hours with various routinely used stannous complexes (HSA, MAA, GHT, DTPA, PYPs) containing different amounts of Sn++ (0.17 —15.0 μ mg/kg). Beyond a concentration of 0.26 mg/kg of Sn++ an alteration in 99mTc-pertechnetate distribution was observed. The red blood cell was found to be the most prominent target. An in-vivo reduction of 99mTc-pertechnetate apparently occurred by the presence of stannous ion within the red blood cell. Preloading time period between 5—24 hours did not alter the uptake of RBC/plasma ratio. Beyond that period it decreased slowly and still persisted up to 2 weeks following pretreatment. RBC/ plasma ratio of 99mTcO4 - increased with increased Sn++ content of various commercially available pharmaceutical kits.

99mTc-Sn-Pyrophosphate Complexes, an Investigation of its Possible Structures

1974 ◽  
Vol 13 (03) ◽  
pp. 252-257 ◽  
Author(s):  
K. Rörvik - Schümichen ◽  
G. Hoffmann ◽  
C. Schümichen
Keyword(s):  
In Vivo Distribution ◽  
Low Concentrations ◽  
Distribution Studies

SummaryAt least two different 99mTc-Sn-pyrophosphate complexes are formed, as it is shown by comparative in vivo distribution studies: A 2 : 2 Sn : pyrophosphate complex is predominant at higher concentrations. Only this complex shows bone seeking properties. A 2 : 1 Sn : pyrophosphate complex exists only at low concentrations. This complex shows no deposition in bone but in the kidneys. Which complex is predominant depends on the pyrophosphate concentration in the equilibrium. Both complexes are rapidly excreted by the kidneys.

Design and Synthesis of Quinazolinone Derivatives as Anti-inflammatory Agents: Pharmacophore Modeling and 3D QSAR Studies

2014 ◽  
Vol 10 (7) ◽  
pp. 711-723 ◽  
Author(s):  
P. Chaitanya ◽  
G. Reddy ◽  
G. Varun ◽  
L.M. Srikanth ◽  
V.V.S.R. Prasad ◽  
...  
Keyword(s):  
3D Qsar ◽  
Pharmacophore Modeling ◽  
Qsar Studies ◽  
Design And Synthesis ◽  
Anti Inflammatory ◽  
Quinazolinone Derivatives

3D-QSAR Methodologies and Molecular Modeling in Bioinformatics for the Search of Novel Anti-HIV Therapies: Rational Design of Entry Inhibitors

2013 ◽  
Vol 8 (4) ◽  
pp. 452-464 ◽  
Author(s):  
Alejandro Speck-Planche ◽  
Valeria Kleandrova ◽  
Marcus Scotti ◽  
M. Cordeiro
Keyword(s):  
Molecular Modeling ◽  
Rational Design ◽  
3D Qsar ◽  
Entry Inhibitors ◽  
Anti Hiv
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