Chemical Synthesis, Herbicidal Activity, Crop Safety, and Molecular Basis of -Fluoroalkoxy Substituted Sulfonylureas as Novel Acetohydroxyacid Synthase Inhibitors.

In the face of increasing resistance to the currently used commercial herbicides and the lack of success in identifying new herbicide targets, alternative herbicides need to be developed to control unwanted monocotyledon grasses in food crops. Here, a panel of 29 novel sulfonylurea-based compounds with fluoroalkoxy substitutions at the phenyl ring were designed and synthesized. Pot assays demonstrated that two of these compounds, and , have strong herbicidal activities against , , , and Steudel at a dosage of 15 g ha.

Structure-activity relationships of bensulfuron methyl and its derivatives as novel agents against drug-resistant Candida auris.

With the emergence of the human pathogen Candida auris as a threat to human health, there is a strong demand to identify effective medicines to prevent the harm caused by such drug-tolerant human fungi. Herein, a series of 33 new derivatives of bensulfuron methyl (BSM) were synthesized and characterized by H NMR, C NMR, and HRMS. Among the target compounds, 8a possessed the best K value of 1.

Treating radiation‑related nasopharyngeal necrosis with endostar in patient with nasopharyngeal carcinoma: A report of two cases and a literature review.

Radiation-related nasopharyngeal necrosis (RRNN) is a rare and often fatal complication in patients with nasopharyngeal carcinoma (NPC). Currently, no standard treatments are recommended for RRNN. The effects of traditional conservative treatments are suboptimal, and surgery for RRNN cannot be performed by inexperienced doctors.

Facile synthesis, crystal structure, quantum calculation, and biological evaluations of novel selenenyl sulfide compounds as potential agrochemicals.

Background: In order to design compounds with fresh molecular skeleton to break through the limitation of available agrochemicals, a series of 36 novel selenenyl sulfide compounds were chemically synthesized, and their biological activities were fully evaluated against tobacco mosaic virus (TMV), 14 plant pathogenic fungi, three insect species and plant acetohydroxyacid synthase (AHAS).

Results: All the target compounds were characterized by proton nuclear magnetic resonance ( H-NMR), carbon-13 ( C)-NMR, selenium-77 ( Se)-NMR, and high-resolution mass spectrometry (HRMS). The crystal structure of 10j indicated that the Se-S bond was successfully constructed.

Chemical preparation, degradation analysis, computational docking and biological activities of novel sulfonylureas with 2,5-disubstituted groups.

Based on the previous finding that a substitution at 5-position of the benzene ring is favorable to enhance the degradation rates of sulfonylurea herbicides, a total of 16 novel 2,5-disubsituted sulfonylurea compounds were chemically synthesized and fully characterized by means of H NMR, C NMR, HRMS and X-ray diffraction. By using HPLC analysis, the degradation behavior of M03, a compound belonging to this family, was studied and confirmed that chlorsulfuron itself is not a degraded product of the 2,5-disubstituted sulfonylureas. Inhibition constants against plant acetohydroxyacid synthase (AHAS) were determined for selected compounds, among which SU3 showed seven times stronger activity against the mutant W574L enzyme than chlorsulfuron.

Tailoring bacterial cellulose structure through CRISPR interference-mediated downregulation of galU in Komagataeibacter xylinus CGMCC 2955.

Diverse applications of bacterial cellulose (BC) have different requirements in terms of its structural characteristics. culturing Komagataeibacter xylinus CGMCC 2955, BC structure changes with alterations in oxygen tension. Here, the K.

Purification optimization for a recombinant single-chain variable fragment against type 1 insulin-like growth factor receptor (IGF-1R) by using design of experiment (DoE).

Design of experiment (DoE) is a statistics-based technique for experimental design that could overcome the shortcomings of traditional one-factor-at-a-time (OFAT) approach for protein purification optimization. In this study, a DoE approach was applied for optimizing purification of a recombinant single-chain variable fragment (scFv) against type 1 insulin-like growth factor receptor (IGF-1R) expressed in Escherichia coli. In first capture step using Capto L, a 2-level fractional factorial analysis and successively a central composite circumscribed (CCC) design were used to identify the optimal elution conditions.

Co-expression of Dsb proteins enables soluble expression of a single-chain variable fragment (scFv) against human type 1 insulin-like growth factor receptor (IGF-1R) in E. coli.

Type 1 insulin-like growth factor receptor (IGF-1R) is a promising therapeutic target for cancer treatment. A single-chain variable fragment (scFv) against human IGF-1R forms inclusion body when expressed in periplasmic space of E. coli routinely.

Pin1, endothelial nitric oxide synthase, and amyloid-β form a feedback signaling loop involved in the pathogenesis of Alzheimer's disease, hypertension, and cerebral amyloid angiopathy.

Although the molecular mechanism has not yet been clarified until now, it is very interesting that Alzheimer's disease (AD), hypertension (HTN), and cerebral amyloid angiopathy (CAA) often occur synchronously and possess many similar pathological characteristics. Herein, we hypothesize that a feedback signaling loop, consisted of Pin1, endothelial nitric oxide synthase (eNOS), and amyloid-β (Aβ), may contribute to the interesting pathological phenomenon. First, Pin1 inhibits the production of Aβ, and enhances the activity of eNOS.

Focusing on the structure and the function of Pin1: new insights into the opposite effects of fever on cancers and Alzheimer's disease.

A new molecular mechanism is proposed to explain the opposite effects of fever on cancers and Alzheimer's disease (AD). The proposal is based on the experimental discovery that the fever stress interferes the structure and the activity of Pin1, which plays uniquely opposite roles in the pathogenesis of cancers and AD. Pin1 is the only known cis-trans isomerase that specifically isomerizes the pSer/pThr-Pro motifs in proteins, facilitating kinds of signaling pathways.

Crush stenting with drug-eluting stents: relevance of coronary bifurcation lesion location on angiographic and clinical outcomes.

Background: Data on the relevance of the location of coronary bifurcation lesions treated by crush stenting with outcomes were limited.

Hypothesis: We hypothesized that the location of the bifurcation lesion correlated with clinical outcome.

Method: A total of 212 patients with 230 true bifurcation lesions treated by crush stenting with drug-eluting stents (DES) were assessed prospectively.

Clinical outcome after management of unprotected left main in-stent restenosis after bare metal or drug-eluting stents.

Background: Implantation of either bare metal stent (BMS) or drug-eluting stent (DES) has been used in every day practice for patients with unprotected left main stenosis (UPLMS). There are still a lack of data regarding the subsequent results of UPLMS in-stent restenosis (ISR). The present study aimed at determining the clinical outcome of UPLMS ISR patients after implantation of either BMS or DES.

Mechanisms and clinical significance of quality of final kissing balloon inflation in patients with true bifurcation lesions treated by crush stenting technique.

Background: The mechanisms responsible for the occurrence of a kissing unsatisfied (KUS) result after classical crush stenting remain unclear. The present study aimed at analyzing the mechanisms and clinical significance of KUS.

Methods: Two hundred and thirteen patients with true bifurcation lesions treated with classical crush stenting and final kissing balloon inflation (FKBI) were assigned to upper, middle, and lower groups according to the position of the side branch re-wiring assessed by visual estimation, quantitative coronary analysis (QCA) and intravascular ultrasound (IVUS).

Different edge effects of paclitaxel- and sirolimus-eluting stents on proximal and distal edges in patients with unstable angina: serial intravascular ultrasound analysis.

Background: It is unclear whether edge segments have different responses to paclitaxel eluting stent (PES) and sirolimus eluting stent (SES) implantation in patients with unstable angina. This study aimed to compare the different vascular edge responses in patients with unstable angina and single de novo coronary lesion treated with SES and PES.

Methods: Two hundred and fifty-five patients with unstable angina and single de novo lesion were randomly assigned to PES and SES groups.

Effect of coronary bifurcation angle on clinical outcomes in Chinese patients treated with crush stenting: a subgroup analysis from DKCRUSH-1 bifurcation study.

Background: Bifurcation angles may have an impact on the clinical outcomes of crush stenting. We sought to compare high (> or = 60 degrees ) with low (< 60 degrees ) bifurcation angle in patients who underwent either classical or double kissing (DK) crush stenting for bifurcation lesions from the DKCRUSH-1 data base.

Methods: There were 212 patients with 220 lesions, some with low-angle (n = 138) and some with high-angle (n = 74).

[Comparison of DK crush with classical crush technique with drug-eluting stents for the treatment of coronary bifurcation lesions from DKCRUSH-1 study].

Objective: To determine independent factors correlated with clinical effects of DK crush and classical crush technique with drug-eluting stents on bifurcation lesions.

Methods: 311 patients with bifurcation lesions were randomized to classical (C, n = 156) or double kissing (DK) crush (n = 155) stent implantation group. The primary endpoints included major adverse cardiac events (MACE).

Crush stenting in treating coronary bifurcate lesions: paclitaxel eluting stents versus sirolimus eluting stents.

Background: Because no data regarding the comparison of crush stenting with paclitaxel (PES) or sirolimus eluting stents (SES) for coronary bifurcate lesions have been reported, we compared the clinical outcomes of these two types of stents.

Methods: Two hundred and thirty patients with 242 bifurcate lesions were enrolled in a prospective, nonrandomized trial. Primary endpoints included myocardial infarction, cardiac death and target vessel revascularization at 8 months.