Considering the chemical and pharmacological properties of semicarbazones, an interdisciplinary didactic sequence was developed to be applied in experimental classes of undergraduate courses in Pharmacy, Chemistry and related areas. This didactic sequence was planned in three steps, starting from the planning of the target molecule, a semicarbazone derived from helional, to its synthesis, physicochemical characterization (CCD, melting point, FTIR and UV-Vis) and in silico tests of its pharmacokinetic properties using the free software ADMETlab 2.0. The proposed target molecule has as molecular scaffold the 1,3-benzodiaxole nucleus and the semicarbazone function, aiming to obtain a molecule with promising anticonvulsant action and that can be obtained by a low cost and easy to execute methodology, which makes it attractive for use in experimental classes. Thus, the application of this didactic sequence aims to provide undergraduate students the opportunity to experience the process of drug development, applying techniques for planning, synthesis, characterization, and pharmacokinetic evaluation in silico. Besides reinforcing the interdisciplinary teaching of Medicinal Chemistry, applying in an integrated way the theoretical and practical knowledge of the disciplines of Organic Chemistry, Physical Chemistry, Pharmacology and Computational Chemistry.

Theranostic can be used to define therapeutic and imaging agents in a system. It is consisting of four components: signal emitter, therapeutic agent, targeting ligand and carrier. Naphthoimidazole and naphthoxazole are extended aromatic systems, and can participate in theranostic systems (TS) acting as a therapeutic agent and/or a signal emitter considering of their broad spectrum of biological activities and their optical properties of fluorescence emission. This systematic review investigated the applicability of the naphthoimidazole and naphthoxazole nuclei as constituents of TS and shows the synthesis methodologies described in the articles selected. Among the scientific articles suitable for the criteria of the systematic review, more than 35% described the evaluation of biological activities, mainly the naphthoimidazole derivatives, and approximately 18% explored the fluorescence emission of naphthoxazole derivatives and their applicability in biological systems. Among the selected articles 53% and 44% show synthetic routes for the preparation of naphthoxazoles and naphthoimidazoles, respectively. It was observed that both nuclei can be synthesized from various reagents, such as naphthoquinones, naphthols, naphthoic acids, aminonaphthoquinones and cyanophthalides. The results of this study suggests that naphthoimidazole and naphthoxazole derivatives are promising for application as components of TS, and there are various synthetic possibilities for obtaining these heterocycles.

Multicomponent reactions are attractive for the development of bioactive substances, being a one-pot synthesis allows a quick and efficient synthesis, and allows the construction of a diversity of privileged structures. The Debus-Radziszewski reaction, a classic example of a multicomponent reaction for obtaining 2,4,5-tri-substituted imidazole, was used to compose a didactic sequence to be applied in undergraduate courses in the following disciplines: Organic Chemistry, Experimental Chemistry, Pharmaceutical Chemistry and Medicinal Chemistry. Thus, the classes were planned and applied, one theoretical and two experimental, the synthesis of lofin (2,4,5-triphenyl-1H-imidazole) and the characterization of the product. The Debus-Radziszewski reaction for the preparation the lofin, proved to be suitable for practical class of multicomponent reactions, as it uses accessible reagents and equipment, it is easy to do and the students can follow the progress of the reaction visually. In addition, the didactic sequence inserts students in a contextualized and interdisciplinary way in the practical chemistry procedures, employing a classic reaction, but with current perspectives of Organic and Medicinal Chemistry, such as the synthesis of the privileged fragments of bioactive compounds.

Skin cancer is a frequent neoplasm in Brazil and this, is observed the importance of the development of new sunscreens using simple methodologies capable of reducing production costs. In this context, six symmetric acyclic azines were synthesized and characterized, with reaction yields between 54 and 84%, short reaction times (5 to 10 min), and manual grinding as an energy source. Sunscreens 10 %(m/m) of these compounds were produced for the in vitro determination of the solar protection factor UVB (SPF-UVB), of the the six formulations containing the synthesized azines, four showed higher photoprotective capacity in the UVB region (AZN-BZD, AZN-2OH, AZN-4OH and AZN-CIN), with SPF-UVB equivalent or higher than benzophenone-3 (BZF) and at the octylmethoxycinnamate (OMC), commercial chemical filters. The AZN-VAN and AZN-4DAB formulations presented high photoprotective capacity in the UVA region, resulting in lower SPF-UVB when compared to the other synthesized azines, but were still superior to the BZF and equivalent to the OMC. All the azines synthesized showed superior FPS-UVB to their precursor aldehydes, evidencing the increase of the photoprotective capacity due to the insertion of the azine group.

In Brazil, the development of new chemical entities (NEQ) is still limited to small advances in the academic and public research sectors, the authors understand that this is a sector of the pharmaceutical industry that needs encouragement. Accepting that education transforms society, educate students in the development of bioactive molecules, it’s a way to stimulate the national pharmaceutical industry to invest in the sector. Thus, this work brings a didactic sequence, applicable in undergraduate courses, which exemplifies some stages of development of the NEQ through its rational planning. The synthesis of a 1,3,4-oxadiazole heterocycle was planned and its potentiality assessed through the Lipinski’s Rule of Five (RO5), using the ChemSpider® database. Once in accordance with RO5, the heterocycle was prepared using a simple and accessible methodology, using microwaves for domestic use as heating source. The 2-phenyl-5-(pyridin-4-yl)-1,3,4-oxadiazole was synthesized by oxidative cyclization of acylhydrazone and an overall yield of 90%. So was possible to demonstrate in a practical way some steps for the development of a substance with potential biological activity and thus to attract greater interest of undergraduate students by this follow-up of the Medicinal Chemistry.

<p>Medicinal Chemistry is a multidisciplinary discipline and the discovery of new bioactive molecules is one of its objectives. Molecular Hybridization (MH) is a strategy of rational design of new prototypes, where the lead compound is produced through an adequate fusion of pharmacophoric sub-unities. Undergraduate laboratory experiments for Medicinal Chemistry education with a focus on MH are scarce. Therefore, the present paper describes a practice class for some undergraduate courses (Pharmacy, Chemistry and/or Chemical Engineering) involving drug development and MH that can be performed at low cost. In this work, alternative materials such as paracetamol and sulfadiazine tablets were used to engage student's attention and to contextualize important concepts of MH. The experiment describes the synthesis of a new compound involving the azo coupling between an aromatic amine (sulfadiazine) and a phenol (paracetamol) to show undergraduate students a practical example of MH. In this case, SciFinder^® - a search website of the American Chemical Society - was also demonstrated and utilized as a search tool in the proposed experimental class.</p>