New Oligoethylene Ester Derivatives of 5‐iodo‐2′‐deoxyuridine as Dermal Prodrugs: Synthesis, Physicochemical Properties, and Skin Permeation Studies

2002 ◽  
Vol 91 (1) ◽  
pp. 171-179 ◽  
Author(s):  
Francesco Paolo Bonina ◽  
Maria Grazia Rimoli ◽  
Lucia Avallone ◽  
Francesco Barbato ◽  
Marzia Amato ◽  
...  
Keyword(s):  
Physicochemical Properties ◽  
Skin Permeation ◽  
Permeation Studies ◽  
Derivatives Of

Synthesis and Physicochemical Properties of Energetic 1,2,4,5‐Tetrazinyl Derivatives of 5‐Nitro‐2,4‐dihydro‐1,2,4‐triazol‐3‐one

2021 ◽  
Vol 6 (30) ◽  
pp. 7654-7662
Author(s):  
Gennady F. Rudakov ◽  
Ivan B. Kozlov ◽  
Nikolay V. Boev ◽  
Svetlana S. Zinchenko ◽  
Lyudmila Ya. Melnikova ◽  
...  
Keyword(s):  
Physicochemical Properties ◽  
Derivatives Of

Chemical modification and Physicochemical properties of new derivatives 5-(thiophen-3-ilmethyl)-4-R1-1,2,4-triazole-3-thiol

2021 ◽  
pp. 4621-4629
Author(s):  
O.A. Bihdan ◽  
V.V. Parchenko
Keyword(s):  
Physicochemical Properties ◽  
High Reactivity ◽  
Biologically Active Compounds ◽  
Biologically Active ◽  
Active Compounds ◽  
Triazole Derivatives ◽  
Pharmaceutical Ingredients ◽  
Current Trends ◽  
Wide Range ◽  
Derivatives Of

Current trends in the search for new biologically active compounds among synthetic molecules have arguably proved a priority in studies of the heterocyclic 1,2,4-triazole system. For many years, 1,2,4-triazole derivatives remain the object of close attention of scientists of various scientific fields. The unique properties of 1,2,4-triazole derivatives include high reactivity, which allows different modification of this system, practical absence of toxicity of these derivatives and the presence of a wide range of biological, pharmacological properties, which in the complex provides the prerequisites for the creation of new biologically active compounds, and in the future, active pharmaceutical ingredients (AFI). The aim of our work is to investigate some transformations in a number of derivatives of 5-(thiophen-3-ylmethyl) -4-R1-1,2,4-triazole-3-thiol, to study the physicochemical properties of the new synthesized compounds. A well-known fact remains the successful attempt of many scientists involved in the study of the heterocyclic 1,2,4-triazole system to synthesize potential biologically active compounds. The process of creating new molecules is very painstaking and requires considerable effort. The chemical approaches for the synthesis of the starting compounds required for further transformations are well known and described. Therefore, we used the corresponding N-R1-2 as intermediates for the synthesis of new 5-(thiophen-3-ylmethyl) -4-R1-1,2,4-triazole-3-thiols appropriate ones were used N-R1-2-(2-(thiophen-3-yl) acetyl) hydrazinocarbothioamide.

scholarly journals The synthesis and physicochemical properties of new derivatives of 5-r-phenylamino-2-mercapto-1,3,4-thiadiazole

2016 ◽  
Vol 0 (1(85)) ◽  
pp. 24-28
Author(s):  
I. V. Sych ◽  
L. O. Perekhoda ◽  
Z. G. Ieromina ◽  
L. O. Grinevich ◽  
N. P. Kobzar ◽  
...  
Keyword(s):  
Physicochemical Properties ◽  
Derivatives Of

scholarly journals Penetration of Chlorhexidine into Human Skin

2008 ◽  
Vol 52 (10) ◽  
pp. 3633-3636 ◽  
Author(s):  
T. J. Karpanen ◽  
T. Worthington ◽  
B. R. Conway ◽  
A. C. Hilton ◽  
T. S. J. Elliott ◽  
...  
Keyword(s):  
Human Skin ◽  
High Performance ◽  
Skin Permeation ◽  
Full Thickness ◽  
Alternative Strategies ◽  
Thickness Skin ◽  
Skin Antisepsis ◽  
Permeation Studies ◽  
Franz Diffusion Cells

ABSTRACT This study evaluated a model of skin permeation to determine the depth of delivery of chlorhexidine into full-thickness excised human skin following topical application of 2% (wt/vol) aqueous chlorhexidine digluconate. Skin permeation studies were performed on full-thickness human skin using Franz diffusion cells with exposure to chlorhexidine for 2 min, 30 min, and 24 h. The concentration of chlorhexidine extracted from skin sections was determined to a depth of 1,500 μm following serial sectioning of the skin using a microtome and analysis by high-performance liquid chromatography. Poor penetration of chlorhexidine into skin following 2-min and 30-min exposures to chlorhexidine was observed (0.157 ± 0.047 and 0.077 ± 0.015 μg/mg tissue within the top 100 μm), and levels of chlorhexidine were minimal at deeper skin depths (less than 0.002 μg/mg tissue below 300 μm). After 24 h of exposure, there was more chlorhexidine within the upper 100-μm sections (7.88 ± 1.37 μg/mg tissue); however, the levels remained low (less than 1 μg/mg tissue) at depths below 300 μm. There was no detectable penetration through the full-thickness skin. The model presented in this study can be used to assess the permeation of antiseptic agents through various layers of skin in vitro. Aqueous chlorhexidine demonstrated poor permeation into the deeper layers of the skin, which may restrict the efficacy of skin antisepsis with this agent. This study lays the foundation for further research in adopting alternative strategies for enhanced skin antisepsis in clinical practice.

scholarly journals Human Skin Permeation Studies with PPARγ Agonist to Improve Its Permeability and Efficacy in Inflammatory Processes

2017 ◽  
Vol 18 (12) ◽  
pp. 2548 ◽  
Author(s):  
Marcelle Silva-Abreu ◽  
Lupe Espinoza ◽  
María Rodríguez-Lagunas ◽  
María-José Fábrega ◽  
Marta Espina ◽  
...  
Keyword(s):  
Human Skin ◽  
Skin Permeation ◽  
Pparγ Agonist ◽  
Inflammatory Processes ◽  
Permeation Studies

Emulgels Containing Carbopol 934P and Different Vegetable Oils for Topical Propolis Delivery: Bioadhesion, Drug Release Profile, and Ex Vivo Skin Permeation Studies

2020 ◽  
Vol 21 (6) ◽  
Author(s):  
Rafaela Said dos Santos ◽  
Camila Félix Vecchi ◽  
Hélen Cássia Rosseto ◽  
Jéssica Bassi da Silva ◽  
Maria Eduarda Lima Dano ◽  
...  
Keyword(s):  
Drug Release ◽  
Vegetable Oils ◽  
Ex Vivo ◽  
Skin Permeation ◽  
Release Profile ◽  
Drug Release Profile ◽  
Permeation Studies ◽  
Carbopol 934P
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