Current strategies in design and synthesis of antifungals hybrid and chimeric diazine derivatives.

In the last decades fungal infections became a major threat to human health having an unacceptably occurrence, a high rate of mortality and the number of patients at risk for these infections continue to increase every year. An effective, modern and very useful strategy in antifungal therapy is represented by the use of chimeric and hybrid drugs, most of them being with azaheterocycle skeleton. In this review, we present an overview from the last five years of the most representative achievements in the field of chimeric and hybrid diazine derivatives with antifungal properties.

Ultrasound assisted synthesis of hybrid quinoline anchored with 4-R-benzenesulfonamide moiety with potential antimicrobial activity.

We present in this paper a direct and efficient study regarding synthesis and spectral characterization of three series of hybrid quinoline anchored with 4-R-benzenesulfonamide moiety, with potential antimicrobial activity, by using ultrasound (US) irradiation and conventional methods (CV). The synthesis pathway is efficient and direct, in two steps: an initial -acylation of 8-aminoquinoline followed by metal complexation with variously M metals (Cd, Co, Cu, Ni, Pd, Zn). For both type of reactions, -acylation and complexation, under US irradiations the synthesis have some undeniable advantages: the most relevant being the higher yields, a dramatically decrease for reaction time (with about 150 (one hundred fifty) folds for complexation) comparative with conventional methods (CV) (therefore the spent energy decrease in the same way), a decrease of the amount of used solvents.

Benzoquinoline Derivatives: An Attractive Approach to Newly Small Molecules with Anticancer Activity.

This study presents the synthesis, structural characterization, and in vitro evaluation of anticancer activity of some newly benzo[]quinoline derivatives. The synthesis is facile and efficient, involving two steps: quaternization of nitrogen heterocycle followed by a [3+2] dipolar cycloaddition reaction. The synthesized compounds were characterized by FTIR, NMR, and X-ray diffraction on monocrystal in the case of compounds and .

Hybrids Diazine: Recent Advancements in Modern Antimicrobial Therapy.

Nowadays, antimicrobial therapies have become a very challenging issue because of a large diversity of reasons such as antimicrobial resistance, over consumption and misuse of antimicrobial agents, . A modern, actual and very useful approach in antimicrobial therapy is represented by the use of hybrid drugs, especially combined five and six-membered ring azaheterocycles. In this review, we present an overview of the recent advanced data from the last five years in the field of hybrid diazine compounds with antimicrobial activity.

Quinoline-imidazole/benzimidazole derivatives as dual-/multi-targeting hybrids inhibitors with anticancer and antimicrobial activity.

Two new classes of hybrid quinoline-imidazole/benzimidazole derivatives (the hybrid QIBS salts and QIBC cycloadducts) were designed and synthesized to evaluate their anticancer and antimicrobial activity. The strategy adopted for synthesis is straight and efficient, in four steps: N-acylation, N-alkylation, quaternization and a Huisgen 3 + 2 cycloaddition. The in vitro single-dose anticancer assay of forty six hybrid quinoline-benzimidazole compounds reveal that one QIBS salt (11h), has an excellent quasi nonselective activity against all type of cancer cell with an excellent PGI in the area of 90-100% and very good lethality.

Ultrasound assisted synthesis of hybrid quinoline-imidazole derivatives: a green synthetic approach.

A green, straightforward and efficient study for obtaining hybrid quinoline-imidazole derivatives under ultrasound (US) irradiation as well as under conventional thermal heating (TH) has been presented. The reaction pathway involves only two steps: the -alkylation of imidazole ring and a Huisgen [3 + 2] dipolar cycloaddition reaction of ylides to dimethyl acetylenedicarboxylate (DMAD). For both types of reactions, a green workup procedure under US irradiation has been presented.

Hybrid Quinoline-Sulfonamide Complexes (M) Derivatives with Antimicrobial Activity.

Two new series of hybrid quinoline-sulfonamide complexes (M: Zn, Cu, Co and Cd) derivatives () were designed, synthesized and tested for their antimicrobial activity. The synthesis is straightforward and efficient, involving two steps: acylation of aminoquinoline followed by complexation with metal acetate (Cu, Co and Cd) or chloride (Zn). The synthesized compounds were characterized by FTIR and NMR spectroscopy and by X-ray diffraction on single crystal.