Discovery of quinazoline-benzothiazole derivatives as novel potent protease-activated receptor 4 antagonists with improved pharmacokinetics and low bleeding liability.

Protease-activated receptor 4 (PAR4) plays a critical role in the development of pathological thrombosis, and targeting PAR4 is considered a promising strategy for improving antiplatelet therapies. Here, we reported the design of a series of quinazoline-benzothiazole-based PAR4 antagonists using a scaffold-hopping strategy. Systematic structure-activity relationship exploration leads to the discovery of compounds 20f and 20g, which displayed optimal activity (h.

Eyecare-cloud: an innovative electronic medical record cloud platform for pediatric research and clinical care.

Background And Objectives: Clinical data are essential for developing cloud platforms for intelligent diagnosis and treatment decision of diseases. However, cloud platforms for data sharing and exchange with clinicians are poorly suited. We aim to establish Eyecare-cloud, a platform which provide a novel method for clinical data and medical image sharing, to provide a convenient tool for clinicians.

A fundus image dataset for intelligent retinopathy of prematurity system.

Image-based artificial intelligence (AI) systems stand as the major modality for evaluating ophthalmic conditions. However, most of the currently available AI systems are designed for experimental research using single-central datasets. Most of them fell short of application in real-world clinical settings.

Design, Synthesis and Biological Evaluation of 7-Substituted-1,3-diaminopyrrol[3,2-f]quinazolines as Potential Antibacterial Agents.

The evolution of drug-resistant bacteria poses a serious threat to public health; hence, it is imperative to develop new and efficient antibiotics. Irresistin-16 (IRS-16) is a dual-target antibacterial candidate that affects folate biosynthesis and membrane integrity and exhibits potent lethality against various bacteria. In this study, a series of 1,3-diamino-7H-pyrrol[3,2-f]quinazoline (DAPQ) derivatives based on IRS-16 was designed and synthesized to identify outstanding antibacterial candidates.

Predictors of female sexual problems in Shanxi, China: a population-based cross-sectional epidemiologic survey.

Background: Large studies on female sexual function have been conducted globally. Nonetheless, whether the state of female sexual function in China is significantly different from that in the rest of the world is largely unknown.

Aim: In this study, we aimed to investigate the associated risk factors for sexual problems in women in Shanxi, China, by conducting a population-based cross-sectional epidemiological survey.

Role of the microbiome and its metabolites in ankylosing spondylitis.

Ankylosing spondylitis (AS), a chronic condition that commonly influences the spine and sacroiliac joints, usually progresses to stiffness and progressive functional limitation. Its fundamental etiology and pathogenesis are likely multifactorial and remain elusive. As environmental factors, gut microbiota performs critical functions in the pathogenesis of AS through various mechanisms, including interacting with genes, enhancing intestinal permeability, activating the gut mucosa immune system, and affecting the intestinal microbiota metabolites.

Synthesis and evaluation of novel and potent protease activated receptor 4 (PAR4) antagonists based on a quinazolin-4(3H)-one scaffold.

Protease activated receptor 4 (PAR4) is an important target in antiplatelet therapy to reduce the risk of heart attack and thrombotic complications in stroke. PAR4 antagonists can prevent harmful and stable thrombus growth, while retaining initial thrombus formation, by acting on the late diffusion stage of platelet aggregation, and may provide a safer alternative to other antiplatelet agents. To date, only two PAR4 antagonists, BMS-986120 and BMS-986141 have entered clinical trials for thrombosis.

Protease activated receptor 4 (PAR4) antagonists: Research progress on small molecules in the field of antiplatelet agents.

Protease activated receptor 4 (PAR4) is a key target in antiplatelet medication to reduce the risk of heart attack and thrombotic complications in stroke. PAR4 antagonists can prevent harmful and stable thrombus growth while retaining initial thrombus formation by acting on the late diffusion stage of platelet activation, which may provide a safer alternative than other antiplatelet agents. Currently, research on PAR4 antagonists is of increasing interest in the field of antiplatelet agents.

Structure evaluation and highly enhanced luminescence of Dy3+ -doped ZnO nanocrystals by Li+ doping via combustion method.

In this paper, Dy3+ -doped ZnO nanocrystals have been synthesized via a simple combustion method. The as-prepared cuboid-like ZnO nanocrystals appear to be single hexagonal crystalline phase with an average diameter of 20 nm. The characteristic luminescence of doped Dy3+ ions has been evaluated, and the highly enhanced photoluminescence of Dy3+ ions can be obtained by Li+ doping.

Polymeric bis(N,N-dimethylacetamide)tetrakis(thiocyanato)cadmium(II)mercury(II).

The title complex, [[CdHg(SCN)(4)(C(4)H(9)NO)(2)](2)](n), contains two crystallographically independent Cd(II) centres and two Hg(II) centres. Each Cd(II) atom is bound to four N atoms belonging to SCN groups and to two O atoms from N,N-dimethylacetamide (DMA) ligands in an octahedral geometry. Each Hg(II) centre is tetrahedrally coordinated by four SCN S atoms.

catena-Poly[[bis(thiocyanato-kappa N)cadmium(II)]-di-mu-thiourea-kappa(4)S:S].

The Cd(II) ion in the title complex, [Cd(SCN)(2)[SC(NH(2))(2)](2)](infinity), is situated at a centre of symmetry, and is bound to two N atoms belonging to thiocyanate groups and to four S atoms of bridging thiourea ligands. The structure consists of infinite chains of slightly distorted edge-shared Cd-centred octahedra. The bridging S atoms of two thiourea ligands comprise the common edge.

Poly[[[tri(urea-kappaO)manganese(II)]-mu-thiocyanato-kappa2N:S-mercury(II)]-tri-mu-tetrathiocyanato].

The title complex, [MnHg(SCN)4(CH4N2O)3]n, consists of slightly distorted octahedral MnN3O3 and tetrahedral HgS4 units. The Mn(II) atom is coordinated by the O atoms of three urea molecules and by the N atoms of three SCN- ions; Hg(II) is coordinated by four S atoms from SCN- ions. Each pair of Mn(II) and Hg(II) atoms is connected by an -SCN- bridge, forming infinite two-dimensional -Mn-NCS-Hg- networks.