Mini Reviews in Medicinal Chemistry - Volume 16, Issue 11, 2016

Alkylresorcinols are compounds which belong to the family of phenolic lipids, and are usually found in numerous biological species. In the particular case of higher plants, alkylresorcinols have been found in various counterparts with chains of thirteen to twenty-seven carbon atoms containing several saturations. Due to the demonstrated antimicrobial properties of many naturally occurring members of the alkylresorcinols family, it is possible to conclude that these compounds act as defensive agents in plants. Previous studies led to the isolation and identification of 5-alkylresorcinols that cleave DNA. Additionally, in the literature, there are several other biological effects attributed to some resorcinol derivatives, namely, cytotoxic, anticarcinogenic, antiproliferative, antileishmanial and antioxidant properties. This mini-review intends to outline the biological activities of the most relevant alkylresorcinols isolated from plants and to propose future directions for subsequent studies regarding the effective biological effects of this class of compounds.

Culinary herbs are herbaceous (leafy) plants that add flavour and colour to all types of meals. There is a wide variety of herbs that are used for culinary purposes worldwide, which are also recognized for their beneficial health effects, and thus have also been used in folk medicine. Besides their nutritional value herbs are rich in many phytochemical components with bioactive effects, thus improving human health. The aim of the present work was to make a general overview of some of these herbs, including their gastronomic usage, their chemical composition in bioactive components and their reported health effects. This work showed that the health effects are very diverse and differ according to the herb in question. However, some of the most frequently citted biological activities include antioxidant, antimicrobial, and antiviral effects.

Neuregulin-1(NRG-1) has now been accepted to have therapeutic potential in cardiovascular disease. The preclinical and clinical researches of NRG-1 have demonstrated its advantage effects in cardiac function with multi-target cardiovascular biology and pathophysiology, but its influence on cardiac electrophysiology is rarely involved, which is a very important aspect and should not be ignored.

Platinum-based (Pt-based) anticancer drugs have been recognised as one of the most effective drugs for clinical treatment of malignant tumors due to its unique mechanism of action and broad range of anticancer spectrum. But, there are still some limitations such as side effects, drug resistance/cross resistance, no-specific targeting, becoming obstacles to restrict its expanding of clinical application. Targeted drug delivery system (TDDS) is a promising strategy for the research of novel Pt-based anticancer drugs. A variety of TDDS have been explored to improve the antitumor activity of Pt-based drugs such as nanoparticle drug systems, polymer-drug systems, drugs-macrocyclic compounds systems, etc. The review concentrates on recent development of various targeted drug delivery techniques, which could provide more opportunities for the development of Pt-based drugs with better efficiency, lower toxicity and less resistance.

Azaheterocyclic compounds are well-known to have diverse types of biological activity. Among them, azacyclopropanes, commonly referred as aziridines, occupy a prominent place in synthetic organic and medicinal chemistry due to its occurrence in natural resources, complexity involved in synthesis due to ring-strain, building blocks in organic synthesis, and its biological properties. Several novel compounds containing aziridine ring have been designed and synthesized recently by medicinal chemists for evaluating their biological profile. A number of compounds are reported as cysteine protease inhibitors, antibacterial, antifungal, anticancer, antileishmanial, and antimalarial agents. This review article summarizes the biological activity of such compounds. The preparation of such compounds is also described.

With unique optical properties and versatile surface chemistry, cadmium-containing quantum dots (Cd-QDs) have attracted extensive attention for drug delivery in the field of biomedicine. However, Cd-QDs applications are currently restricted in cells and small animals due to their uncertain biological fate and potential toxicity. Consequently, the long-term fate of Cd-QDs and their interaction with biological systems need to be explored for the development of the clinical applications of Cd-QDs as nanomedicines. This review succinctly described recent progress in functionalized Cd-QDs for the design as multifunctional drug delivery system and advanced findings on the interactions of Cd-QDs with biological systems at the level of living systems, cells and biomacromolecules. This knowledge could provide suggestions to improve the delivery performance and biocompatibility of Cd-QDs as well as better understand the potential side effects of Cd-QDs in in vivo applications. In addition, attention was laid on exploring the similarities and discrepancy of their toxicological results at the three levels to comprehensively interpret the potential carcinogenicity of Cd-QDs and deeply understand the associated mechanism.

Cerebral edema causes intracranial hypertension (ICH) which leads to severe outcome of patients in the clinical setting. Effective anti-edema therapy may significantly decrease the mortality in a variety of neurological conditions. At present drug treatment is a cornerstone in the management of cerebral edema. Osmotherapy has been the mainstay of pharmacologic therapy. Mannitol and hypertonic saline (HS) are the most commonly used osmotic agents. The relative safety and efficacy of HS and mannitol in the treatment of cerebral edema and reduction of enhanced ICP have been demonstrated in the past decades. Apart from its osmotic force, HS exerts anti-edema effects partly through inhibition of Na+-K+-2Cl- Cotransporter-1 (NKCC1) and aquaporin 4 (AQP4) expression in astrocytes. Melatonin may also reduce brain edema and exert neuroprotective effect on several central nervous system diseases through inhibition of inflammatory response. The inhibitors of Na/H exchanger, NKCC and AQP4 may attenuate brain edema formation through inhibition of excessive transportation of ion and water from blood into the cerebral tissue. In this review we survey some of the most recent findings in the drug treatment of brain edema focusing on the use of osmotherapy, melatonin and inhibitors of ion cotransporters and water channels. A better understanding of the molecular mechanism of these agents would help to improve in the clinical management of patients with brain edema.

The triazoles 3a-d underwent condensation reactions with 4-(piperidin-1-yl)-benzaldehyde to afford the chalcones 5a-d. Chalcone derivatives 5a-d were reacted with 2,3-diaminomaleonitrile, thiourea and hydrazine hydrate to afford the novel diazepine-dicarbonitrile derivatives 7a-d, the pyrimidine-2-thiol derivatives 9a-d and hydrazino-pyrimidines 10a-d respectively. Structures of the prepared compounds were elucidated by physical and spectral data like FT-IR, 1H NMR, 13C NMR, and mass spectroscopy. Some of the synthesized compounds were screened for their anticonvulsant activity and SAR.