Design, synthesis, and biological evaluations of 5-aryl-pyrazole-3-carboxamide derivatives as selective CB2 receptor agonists for the treatment of colitis.

Synthetic CB2 receptor agonists exhibit great potential in the treatment of neurodegenerative diseases, chronic and neuropathic pain, cancer, and inflammation-associated pathologies while avoiding adverse psychoactive effects caused by interactions with CB1 receptors. Herein, a class of 5-aryl-pyrazole-3-carboxamide derivatives was thus designed, synthesized, and biologically evaluated. Among the compounds tested, compound 33, one of the most potent leads, showed a remarkably high potency and selectivity at the CB2 receptor (EC = 16.

DNA intercalation makes possible superior-gain organic photoelectrochemical transistor detection.

DNA intercalation has increasingly been studied for various scenario implementations due to the diverse functions of DNA/intercalators. Nascent organic photoelectrochemical transistor (OPECT) biosensing taking place in organic electronics and photoelectrochemical bioanalysis represents a promising technological frontier in the arena. In this work, we first devise DNA intercalation-enabled OPECT for miRNA detection with a superior gain up to 17100.

Polymer Dot-Gated Accumulation-Type Organic Photoelectrochemical Transistor for Urea Biosensing.

Organic photoelectrochemical transistor (OPECT) biosensing represents a new platform interfacing optoelectronics and biological systems with essential amplification, which, nevertheless, are concentrated on depletion-type operation to date. Here, a polymer dot (Pdot)-gated accumulation-type OPECT biosensor is devised and applied for sensitive urea detection. In such a device, the as-designed Pdot/poly[bis(4-phenyl)(2,4,6-trimethylphenyl)amine] (PTAA) is validated as a superior gating module against the diethylenetriamine (DETA) de-doped poly(3,4-ethylenedioxythiophene):poly(styrene sulfonate) (PEDOT:PSS) channel, and the urea-dependent status of Pdots has been shown to be sensitively correlated with the device's response.

Design, synthesis, and biological evaluations of phenylpropiolic acid derivatives as novel GPR40 agonists.

GPR40, also known as free fatty acid receptor 1 (FFAR1), is a member of G protein-coupled receptors (GPCR) family and has emerged as an attractive target for the treatment of type 2 diabetes mellitus. So far, most of the synthetic GPR40 agonists, including several drug candidates discontinued in clinical trials, were derived from the phenylpropionic acid scaffold. For discovering novel GPR40 agonists with diverse chemical structures, a series of phenylpropiolic acid derivatives were designed, synthesized, and evaluated under a battery of bioassays.

Identification of Novel Coumestan Derivatives as Polyketide Synthase 13 Inhibitors against Mycobacterium tuberculosis.

Inhibition of the mycolic acid pathway has proven a viable strategy in antitubercular drug discovery. The AccA3/AccD4/FadD32/Pks13 complex of Mycobacterium tuberculosis constitutes an essential biosynthetic mechanism for mycolic acids. Small molecules targeting the thioesterase domain of Pks13 have been reported, including a benzofuran-based compound whose X-ray cocrystal structure has been very recently solved.

[Spatial Heterogeneity of Soil Respiration in a Planted Larch Forest in Shanxi Plateau].

Based on the data from a planted larch forest in Panquangou Natural Reserve of Shanxi Province, at three sampling scales (4, 2, and 1 m, respectively), soil respiration (Rs) and its affecting factors including soil temperature at 5 cm (T5), 10 cm (T10), and 15 cm (T15) depths, soil water content (Ws), litter mass (Lw), litter moisture (Lm), soil total carbon (C), and soil total nitrogen ( N) were determined. The spatial heterogeneities of Rs and the environmental factors were further analyzed and their intrinsic correlations were established. The results of traditional statistics showed that the spatial variations of Rs and the all measured factors were in the middle range; Rs were highly significantly positively correlated with T10, T15, and N (P < 0.