scholarly journals The Lisbon Supramolecular Green Story: Mechanochemistry towards New Forms of Pharmaceuticals

Molecules ◽  
2020 ◽  
Vol 25 (11) ◽  
pp. 2705
Author(s):  
João Luís Ferreira da Silva ◽  
M. Fátima Minas da Piedade ◽  
Vânia André ◽  
Sofia Domingos ◽  
Inês C. B. Martins ◽  
...  

This short review presents and highlights the work performed by the Lisbon Group on the mechanochemical synthesis of active pharmaceutical ingredients (APIs) multicomponent compounds. Here, we show some of our most relevant contributions on the synthesis of supramolecular derivatives of well-known commercial used drugs and the corresponding improvement on their physicochemical properties. The study reflects, not only our pursuit of using crystal engineering principles for the search of supramolecular entities, but also our aim to correlate them with the desired properties. The work also covers our results on polymorphic screening and describes our proposed alternatives to induce and maintain specific polymorphic forms, and our approach to avoid polymorphism using APIs as ionic liquids. We want to stress that all the work was performed using mechanochemistry, a green advantageous synthetic technique.

Author(s):  
O.A. Bihdan ◽  
V.V. Parchenko

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.


MedChemComm ◽  
2013 ◽  
Vol 4 (3) ◽  
pp. 559 ◽  
Author(s):  
O. Andreea Cojocaru ◽  
Katharina Bica ◽  
Gabriela Gurau ◽  
Asako Narita ◽  
Parker D. McCrary ◽  
...  

INDIAN DRUGS ◽  
2016 ◽  
Vol 53 (09) ◽  
pp. 5-11
Author(s):  
S. S Pekamwar ◽  
◽  
D. D. Gadade ◽  
G. K. Kale

Physicochemical characteristics of active pharmaceutical compounds, including solubility and flow properties, are crucial in the development of drug formulation. The physical form of compound and formulation has potential effect on biopharmaceutical parameters of the drug. The crystal engineering approach can be employed for modification of physicochemical properties of the active pharmaceutical ingredients whilst maintaining the intrinsic activity of the drug molecule. This article covers the advantages of co-crystals over salts, solvates (hydrates), solid dispersions and polymorphs, mechanism of formation of co-crystals, methods of preparation of co-crystals and application of co-crystals to modify physicochemical characteristics of active pharmaceutical ingredients along with case studies.


CrystEngComm ◽  
2018 ◽  
Vol 20 (24) ◽  
pp. 3428-3434
Author(s):  
Colin C. Seaton ◽  
Rayan R. Thomas ◽  
Eman A. A. Essifaow ◽  
Elisa Nauha ◽  
Tasnim Munshi ◽  
...  

The creation of salts is a frequently used approach to modify physicochemical properties of active pharmaceutical ingredients. This work prepares a collection of sulfathiazole salts to probe the influence of counterion structure on crystal packing.


ChemMedChem ◽  
2011 ◽  
Vol 6 (6) ◽  
pp. 975-985 ◽  
Author(s):  
Ricardo Ferraz ◽  
Luís C. Branco ◽  
Cristina Prudêncio ◽  
João Paulo Noronha ◽  
Željko Petrovski

2007 ◽  
Vol 31 (8) ◽  
pp. 1429 ◽  
Author(s):  
Whitney L. Hough ◽  
Marcin Smiglak ◽  
Héctor Rodríguez ◽  
Richard P. Swatloski ◽  
Scott K. Spear ◽  
...  

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