(2<i>S</i>,3<i>R</i>,4<i>R</i>,5<i>S</i>,6<i>R</i>)-2-(3-(4-Ethoxybenzyl)-4-chlorophenyl)-6-hydroxymethyl-tetrahydro-2<i>H</i>-pyran-3,4,5-triol (dapagliflozin; BMS-512148) is a potent sodium-glucose cotransporter type II inhibitor in animals and humans currently under development for the treatment of 2 diabetes. The preclinical characterization dapagliflozin, to allow compound selection prediction pharmacological dispositional behavior clinic, involved Caco-2 cell permeability studies,...

Macromolecule bactericides present challenges such as low biocompatibility and not being biodegradable, so broad-spectrum without accumulated bacteria resistance are now in urgent demand all over the world. Lysozyme, a kind of wide-spread natural enzyme easily extracted from nature, has become attractive for agriculture medicine use. However, Gram-negative bacterial strains highly resistant to lysozymes, which limits their practical application. In this study, rather than directly modifying...

A bio-inspired proteinosome-based material showed programmed mutual interaction with <italic>E. coli</italic> by controlling the temperature and ionic strength.

Fluopyram is a highly effective agricultural fungicide targeting succinate dehydrogenase (SDH). Twenty-six novel amide derivatives containing azetidine were designed and synthesized with fluopyram as the lead, their biological activities tested. The results showed that some compounds had obvious antifungal against Phomopsis sp., among them, EC50 value of compound C24 was 5.7 mg/L, which significantly better than (105.4 mg/L). curative protective on kiwi fruit infected sp. 42.2 52.9 %, (30.4...

Xanthomonas oryzae pv. (Xoo) is often considered one of the most destructive bacterial pathogens causing leaf blight (BLB), resulting in significant yield and cost losses rice. In this study, a series novel derivatives containing isopropanolamine moiety linked to various substituted phenols piperazines were designed, synthesized screened.

In this study, we investigate the effect of ecological environment near a firm's operations on its green innovation. Using detailed data city parks, find that when firms are surrounded by better environments, as indicated presence and density parks within 500-meter radius headquarters, they have higher levels corporate Our findings hold across various patent measures alternative model specifications. Firms with greater exposure to spaces at time their initial public offering, those led...

To develop antibacterial agents with a novel mechanism of action, series sulfone compounds containing 1,2,4-triazolo[4,3-a]pyridine were designed and synthesized by progressive molecular structure optimization. The activities some derivatives against the four plant pathogens Xanthomonas oryzae pv. (Xoo), oryzicola (Xoc), axonopodis citri (Xac), Pseudomonas syringae actinidiae (Psa) evaluated. Among them, compound K3 demonstrated significant Xoo, Xoc, Xac, EC50 values 1.5, 1.7, 4.9 mg/L,...

1,2,4-Thiadiazole derivatives containing a sulfone moiety were designed and synthesized via scaffold hopping to facilitate the discovery of novel antibacterial agents. Most compounds exhibited excellent activity against three plant pathogenic bacteria. The half-maximal effective concentrations (EC50) compound B7 for Xanthomonas oryzae pv (Xoo) X. oryzicola (Xoc) 0.4 1.0 mg/L, respectively. In addition, EC50 values B1 B24 Xoo, Xoc, Pseudomonas syringae actinidiae (Psa) less than 5 mg/L...

To develop antibacterial agents with novel mechanisms of action, a series 1,2,4-thiadiazole derivatives containing amide structures were designed and synthesized. The activities against Xanthomonas oryzae pv. oryzicola (Xoc), (Xoo), Pseudomonas syringae actinidiae (Psa) evaluated, all exhibited excellent activities. Among them, compound Z4 demonstrated significant Xoo, Xoc, Psa, EC50 values 0.32, 0.43, 11.06 mg/L, respectively. Compound protective activity 49.42% curative 44.93% rice...

This study investigated the potential anti-inflammatory and analgesic effects of rutin-chitooligosaccharide (R-COS) complex both in vitro vivo. Initially, cytotoxicity R-COS was assessed RAW 264.7 cells using an MTT assay. Subsequently, inflammatory conducted where demonstrated a significant reduction various pro-inflammatory factors (nitric oxide [NO], prostaglandin E2, tumor necrosis factor-α, interleukin-6, interleukin-1, inducible nitric synthase [iNOS], cyclooxygenase [COX-2])...

Abstract BACKGROUND Plant bacterial diseases have severely affected the yield and quality of agricultural products, among which kiwifruit canker wilt disease, caused by Pseudomonas syringae pv. actinidiae ( Psa ) Ralstonia solanacearum Rs ), respectively, seriously restrict development related industry. However, there are few effective green agents available to target these diseases. RESULTS Herein, we synthesized 41 novel derivatives natural product tryptanthrin, partial compounds showed...

Herein, we synthesized 34 novel tryptanthrin derivatives, among which T7NHCO-series compounds showed great antibacterial activity againstXanthomonas axonopodis pv. citri,Pseudomonas syringae actinidiae, andRalstonia solanacearum with EC50 values ranging from 0.26 to 0.56 μg/mL. Meanwhile, these exhibited low cytotoxicity against HEK-293. Additionally, compound T7NHCO can inhibit biofilm formation, damage bacterial morphology, downregulate the expression of chemotaxis-related proteins, cause...

Abstract BACKGROUND The pine wilt disease (PWD) caused by Bursaphelenchus xylophilus is considered the ‘cancer’ of trees, and protecting forests from destructive impact nematode remains a significant challenge. Chemical control one most effective methods for managing plant nematodes. Developing new nematicides an strategy urgent need management. RESULTS Amide derivatives containing 1,2,4‐oxadiazole were designed synthesized through scaffold‐hopping strategy. Some target compounds exhibited...

Plant bacterial diseases have seriously affected the yield and quality of crops, among which rice leaf blight (BLB), caused by Xanthomonas oryzae pv. has rice. As plant-pathogenic bacteria gradually become resistant to existing bactericides, it is necessary find effective bactericides with novel structures.Herein, a series compounds containing quinazolin-4(3H)-one disulfide moieties were designed synthesized using facile synthetic method. The bioassay results revealed that most target...

Xanthomonas axonopodis pv. citri (Xac) belongs to the Gram-negative species, causing citrus canker that seriously affects fruit yield and quality of many rutaceae plants. Herein, we found compound 2-(butyldisulfanyl) quinazolin-4(3H)-one exhibited remarkable anti-Xac activity in vitro with a half effective concentration (EC50) 2.6 μg/mL, while positive controls thiodiazole-copper 57 μg/mL bismerthiazol 68 this showed great anti-citrus vivo. This active also was confirmed reduce biofilm...

A series of indazole derivatives were designed and synthesized by molecular hybridization strategy, these compounds evaluated the inhibitory activities against human cancer cell lines lung (A549), chronic myeloid leukemia (K562), prostate (PC-3), hepatoma (Hep-G2) methyl thiazolyl tetrazolium (MTT) colorimetric assay. Among these, compound 6o exhibited a promising effect K562 line with IC50 (50% inhibition concentration) value 5.15 µM, this showed great selectivity for normal (HEK-293, =...

Rice bacterial leaf blight is a destructive disease caused by Xanthomonas oryzae pv. (Xoo) that seriously threatens crop yields and their associated economic benefits. In this study, series of improved dissolubility 7-aliphatic amine tryptanthrin derivatives was designed synthesized, potency in antibacterial applications investigated. Notably, compound 6e exhibited excellent activity against Xoo, with an EC50 value 2.55 μg/mL, compared the positive control bismerthiazol (EC50 = 35.0 μg/mL)...

Abstract A series of new sorafenib derivatives was designed and synthesized. The antiproliferative activity the synthesized compounds against human lung cancer cell (A549), pancreatic (PC‐3), leukemia (K562), hepatoma (SMMC‐7721) evaluated by MTT assay. results revealed that several displayed more significant antitumor activities than commercial anticancer agent SMMC‐7721. In addition, 7a , 7g 7l 7m 7p represented obvious growth inhibition with IC 50 values 1‐9 μM four lines, demonstrating...

A series of novel quinazoline derivatives containing piperazine analogs are synthesized via substitution reactions with 6,7-disubstituted 4-chloroquinazoline and benzyl (amido piperazine). Potent antiproliferative activities observed against A549, HepG2, K562, PC-3 N-(3-chlorophenyl)-2-(4-(7-methoxy-6-(3-morpholino-propoxy)quinazoline-4-yl)piperazine-1-yl)acetamidename C9 showing excellent activity. This active derivative was screened for cell migration ability, proliferation effects,...

An ethanol extract of the dried aerial Pedicularis densispica Franch (Scrophulariaceae) afforded a new lignan, densispicoside (1), and two iridoids, densispicnin C D (14, 15), together with four lignans, (+)-isolarisiresinol 3a-O-β -D-glucopyranoside (2), (-)-pinoresinol-β - D-glucopyranoside (3), syringaresinol mono-β (4), longifloroside B (5), eight phenylpropanoids, 4-O-β -D-glucopyranosyl-sinapic acid methyl ester (6), 3-(4-hydroxy-3-methoxyphenyl)- 1,2,3-propantriol (7), citrusin (8),...

Abstract The neuroprotective agent 3-hydroxymorphinan (3-HM) is a well-documented and highly safe therapeutic intervention for the inflammatory-related effects of Parkinson’s disease (PD). However, bioavailability 3-HM very low due to rapid first-pass metabolism phenolic moiety. In present study, we sought improve metabolic stability overall pharmacokinetic profile 3-HM. Based on an iterative design process that suitably arranged heterocycle with NH group would serve as metabolically stable...