Resistance to drugs is reaching alarming levels and is placing human health at risk. With the lack of new antimicrobials drugs, infectious diseases are becoming harder to treat. Hence, there is an increasing awareness of active phytochemicals with therapeutic functions. The tremendous research interest on the Cistus L. genus includes numerous plants used in traditional medicine by people living around the Mediterranean Sea, also resulted in some interesting discoveries and written literature. This review aimed at gathering scientific literature about Cistus species, describing phytochemical profiles and the various pharmacological activities. We also extensively reviewed the antimicrobial activities, including antiviral, antiparasitic, antifungal, and antibacterial potentials of Essential Oils (EO), raw extracts as well as isolated compounds. Mechanisms of action along with methods used are also investigated in this review. Considering the findings of the Cistus species extracts, this genus offers an adequate reserve of active phytochemicals since many have been used to create drugs. Therefore, this review work can serve society by providing a global view on Cistus L. sp. regarding pharmacological potentials and their chemical profiles.
6 November 2017 in European Journal of Organic Chemistry
A convenient and efficient synthetic route to C3-arylated 7-trifluoromethylpyrazolo[1,5-a]pyrimidin-5-one derivatives has been reported starting from 3-bromo-7-(trifluoromethyl)pyrazolo[1,5-a]pyrimidin-5-one through a Suzuki–Miyaura cross-coupling reaction. The arylation (heteroarylation) strategy can be performed using a wide variety of aryl and heteroaryl boronic acids and requiring a tandem catalyst XPhosPdG2/XPhos to avoid the debromination reaction. These optimized conditions were successfully extended to the synthesis of 7-, 8- and 9-arylated pyrimido[1,2-b]indazol-2-ones from their corresponding brominated starting materials. Furthermore, the second C-5 arylation of C3-arylated pyrazolo[1,5-a]pyrimidin-5-ones was achieved under standard Suzuki–Miyaura cross-coupling conditions, after activating the C–O bond of the lactam function with PyBroP, giving access to a small library of 3,5-diarylated 7-(trifluoromethyl)pyrazolo[1,5-a]pyrimidines in good to excellent yields. The interest of this approach has been highlighted by the synthesis of a known anti-inflammatory agent. Additionally, a preliminary biological evaluation has revealed that a number of derivatives display micromolar IC50 values against monoamine oxidase B, an important target in the field of neurodegenerative disorders.
Four diterpene alcohols were isolated from the neutral hexane extract of the cones of Cedrus atlantica, and their structures were confirmed after comparing their spectral data with literature values. These products exhibited significant antibacterial activity against gram (±) bacteria.
The C3 direct arylation of 1H-indazole and 1H-7-azaindazole has been a significant challenge due to the lack of the reactivity at this position. In this paper, we describe a mild and an efficient synthesis of new series of C3-aryled 1H-indazoles and C3-aryled 1H-7-azaindazoles via a C3 direct arylation using water as solvent. On water, PPh3 was effective as a ligand along with a lower charge of the catalyst Pd(OAc)2 (5 mol%) at 100 °C, leading to C3-aryled 1H-indazoles or C3-aryled 1H-7-azaindazoles in moderate to good yields.