Unsymmetrical urea derivatives are essential structural motifs in a wide array of biologically significant compounds. Despite the well-established methods for synthesizing symmetrical ureas, efficient strategies for the synthesis of unsymmetrical ure...
Tryprostatin A and B are prenylated, tryptophan-containing, diketopiperazine natural products, displaying cytotoxic activity through different mechanisms of action. The presence of the 6-methoxy substituent on the indole moiety of tryprostatin A was...
The reaction of papaverine with a series of Baran DiversinatesTM is reported. Although the yields were low, it was possible to synthesize a small biodiscovery library using this plant alkaloid as a scaffold for late-stage C–H functionalization....
Posttranslational modifications (PTMs) dramatically expand the functional diversity of the proteome. The precise addition and removal of PTMs appears to modulate protein structure and function and control key regulatory processes in living systems. D...
Voriconazole (VN) is an antifungal drug indicated for the treatment of several fungal infections. Due to its side effects, some works involving late-stage functionalization of VN have been reported in the literature. Here, we disclose a new VN deriva...
Biocatalysis is constantly providing novel options for the synthesis of active pharmaceutical ingredients (APIs). In addition to drug development and manufacturing, biocatalysis also plays a role in drug discovery and can support many active ingredie...
A radical approach to late-stage functionalization using photoredox and Diversinate™ chemistry on the Open Source Malaria (OSM) triazolopyrazine scaffold (Series 4) resulted in the synthesis of 12 new analogues, which were characterized by NMR, UV, a...
The targeting of facilitative sugar transporters (GLUTs) has been utilized in the development of tools for diagnostics and therapy. The interest in this area is promoted by the phenomenon of alterations in cellular metabolic processes that are linked...
Purpose: Facial paralysis results from congenital or acquired facial nerve damage, leading to significant cosmetic and functional deficits. Surgical resection of parotid and midface tumors can cause facial paralysis, necessitating effective treatment...
Globally, we are facing the tendency of aging, and demands for health enhancement among the older population have been steadily increasing. Among various exercise interventions, Pilates has been popularly utilized in rehabilitation; therefore, it is...
Silicon included in a restructured meat (RM) matrix (Si-RM) as a functional ingredient has been demonstrated to be a potential bioactive antidiabetic compound. However, the jejunal and hepatic molecular mechanisms by which Si-RM exerts its cholestero...
The incorporation of bromine, iodine or fluorine into the tricyclic core structure of thiaplakortone A (1), a potent antimalarial marine natural product, is reported. Although yields were low, it was possible to synthesise a small nine-membered libra...
Carbon-centered radicals represent highly useful reactive intermediates in organic synthesis. Their nucleophilic character is reflected by fast additions to electron deficient C=X double bonds as present in iminium ions or cationic heterocycles. Th...
Transition-metal-free direct arylation of C-H or N-H bonds is one of the key emerging methodologies that is currently attracting tremendous attention. Diaryliodonium salts serve as a stepping stone on the way to alternative environmentally friendly a...
This study aimed to assess associations between serum cartilage oligomeric matrix protein (sCOMP) and phenotypic characteristics in late-stage hip and knee Osteoarthritis (OA) as well as its correlation with further serum markers of possible comorbid...
Motor ability decline remains a major threat to the quality of life of the elderly. Although the later stages of aging co-exist with degenerative pathologies, the long process of aging is more complicated than a simple and gradual degeneration. To co...
31 May 2022
There is mounting evidence to suggest that individuals with chronic pain adjusted poorly to and were impacted negatively by social distancing measures during the lockdown. However, there is limited data on the factors that might protect against the n...
Brain-gut axis refers to the bidirectional functional connection between the brain and the gut, which sustains vital functions for vertebrates. This connection also underlies the gastrointestinal (GI) comorbidities associated with brain disorders. Us...
In patients with mild cognitive impairment (MCI), a lower level of cognitive function is associated with a higher likelihood of progression to dementia. In addition, gait disturbances and structural changes on brain MRI scans reflect cognitive levels...
Chronic kidney disease (CKD) is considered a major health problem, which poses a burden for health care systems worldwide. It has been estimated that 10% of the population worldwide have CKD; however, most of the cases are undiagnosed. If left untrea...
Background/Objectives: Post-infectious syndromes, including Post-COVID syndrome, Chronic Fatigue Syndrome, and late-stage Lyme disease, are associated with overlapping clinical features and autonomic dysfunction. Despite shared symptoms such as fatig...
Background/Objectives: Late presentations of advanced hepatocellular carcinoma (HCC) indicate a lack of detection of underlying cirrhosis and a need to identify clinical and socioeconomic risk factors contributing to early-stage HCC recognition. This...
The development of Multi-Target Directed Ligand is of clear interest for the treatment of multifactorial pathology such as Alzheimer’s disease (AD). In this context, acetylcholinesterase (AChE) inhibitors have been modulated in order to generate nove...
The self-similarity in space and time (hereafter self-similarity), either deterministic or statistical, is characterized by similarity exponents and a function of scaled variable, called the scaling function. In the present paper, we address mainly t...
There is a close correlation between type 2 diabetes mellitus (T2DM) and cognitive impairment leading to dementia. Lately, the incidence of T2DM-related dementia has increased with population aging. Factors such as oxidative stress and inflammatory r...
Background and Objectives: The aim of this study was to investigate the changes in the SIRT family, the effects of sirtuins on kidney graft function, and their potential as biomarkers in patients who develop rejection after kidney transplantation. Ma...
16 December 2020
Knowledge-sharing strategies are used across the industry as open innovation and distributed collaboration are becoming more popular to achieve technological competencies, faster time-to-market, competitiveness and growth. Sharing of knowledge can pr...
A simple and rapid method for efficient synthesis of sulfonyl chlorides/bromides from sulfonyl hydrazide with NXS (X = Cl or Br) and late-stage conversion to several other functional groups was described. A variety of nucleophiles could be engaged in...
Wnt signaling has been shown to play multiple roles in regenerative processes, one of the most widely studied of which is the regeneration of the intestinal luminal epithelia. Most studies in this area have focused on self-renewal of the luminal stem...
Amyloid-β (Aβ) deposition and Aβ-induced neurodegeneration appear in the retina and retinorecipient areas in the early stages of Alzheimer’s disease (AD). Although these Aβ-related changes in the retina cause damage to the v...
A healthy lymphatic system is required to return excess interstitial fluid back to the venous circulation. However, up to 49% of breast cancer survivors eventually develop breast cancer-related lymphedema due to lymphatic injuries from lymph node dis...
The construction of well-defined polyurethane dendrimers is challenging due to the high reactivity of externally added or in situ formed isocyanates leading to the formation of side products. With a primary focus of dendrimer research being the inter...
Regioselective benzanilide bromination that generates either regioisomer from the same starting material is desirable. Herein, we develop switchable site-selective C(sp2)-H bromination by promoter regulation. This protocol leads to regiodivergent bro...
Malignant ureteral obstruction (MUO) caused by a primarily urological tumor or secondary to a late-stage malignancy can be difficult for the urologist to manage. Due to a lack of clinical data on the management of MUO, every case is particular and sh...
Organization of extracellular matrix (ECM) components, including collagens, proteoglycans, and elastin, is essential for maintaining the structure and function of heart valves throughout life. Mutations in ECM genes cause connective tissue disorders,...
Cancer cachexia is one of the leading causes of mortality for late-stage cancer patients. One of its key characteristics is abnormal metabolism and loss of metabolic flexibility, i.e., loss of ability to switch between use of fats and carbohydrates a...
Recently, crop breeders have widely adopted a new biotechnology-based process, termed Seed Production Technology (SPT), to produce hybrid varieties. The SPT does not produce nuclear male-sterile lines, and instead utilizes transgenic SPT maintainer l...
Natural products, with their array of structural complexity, diversity, and biological activity, have inspired generations of chemists and driven the advancement of techniques in their total syntheses. The field of natural product synthesis continuou...
A catalyst-free, additive-free, and eco-friendly method for synthesizing 1,2,4-triazolo[1,5-a]pyridines under microwave conditions has been established. This tandem reaction involves the use of enaminonitriles and benzohydrazides, a transamidation me...
Late-stage modification of drug molecules is a fast method to introduce diversity into the already biologically active scaffold. A notable number of analogs of mefloquine, chloroquine, and hydroxychloroquine have been synthesized, starting from the r...
Since its discovery, the Julia–Kocienski olefination reaction has over past 30 years become one of the key C-C connective methods that is used in late-stage natural product synthesis. The reaction proceeds under mild reaction conditions, with a...
Nitriles are valuable compounds because they have widespread applications in organic chemistry. This report details the nickel-catalyzed reductive cyanation of aryl halides and epoxides with cyanogen bromide for the synthesis of nitriles. This robust...
Cordycepin, extracted from the medicinal mushroom Cordyceps militaris, was shown to induce cancer cell apoptosis. Yet its anticancer function was limitedly evaluated, and the mechanism was not entirely elucidated. In this study, we demonstrated the e...
Liver disease is a leading cause of mortality worldwide, resulting in 1.3 million deaths annually. The vast majority of liver disease is caused by metabolic disease (i.e., NASH) and alcohol-induced hepatitis, and to a lesser extent by acute and chron...
Maxillary deficiency, a common transversal dentofacial deformity, affects aesthetics and function. Timely intervention during adolescence is crucial, as the growth potential of the maxilla provides an opportunity to optimize treatment outcomes. This...
31 March 2006
Apoptosis arises from the active initiation and propagation of a series of highly orchestrated specific biochemical events leading to the demise of the cell. It is a normal physiological process, which occurs during embryonic development as well as i...
An efficient palladium-catalyzed carbonylation of aryl fluorosulfates with aryl formates for the facile synthesis of esters was developed. The cross-coupling reactions proceeded effectively in the presence of a palladium catalyst, phosphine ligand, a...
Owing to the pioneering works performed on the metal-catalyzed sp2 C–H arylation of indole and pyrrole by Sanford and Gaunt, N– and C-arylation involving diaryliodonium salts offers an attractive complementary strategy for the late-stage...
Wnt signaling plays a major role in bone metabolism. Advances in our understanding of secreted regulators of Wnt have yielded several therapeutic targets to stimulate osteoanabolism—the most promising of which is the Wnt inhibitor sclerostin. S...
Colonic mucosa exhibits numerous functional alterations associated to type 2 diabetes mellitus (T2DM). Oxidative stress, a factor involved in T2DM pathogenesis and its complications, may contribute to some of the colonic alterations. Silicon (Si) is...
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