Abstract:
:Combinations of different technologies are at the heart of the development and implementation of new, innovative processes and approaches for Industry 4.0 in the field of medicinal chemistry and drug discovery. Process intensification and advances in high-throughput synthetic techniques can dramatically improve reaction rates in processes for which slow kinetics represents a bottleneck. Easier access to target-based chemical library collections offers wider access to new leads for drug development. Green enabling technologies are a reliable ally for the design of environmentally friendly synthetic processes and more highly competitive pharmaceutical production. Mechanochemistry, microwaves, ultrasound and flow chemistry are mature techniques that can boast drug synthesis when properly integrated into the production chain. In this review, we selected examples from the literature of the last five years related to medicinal chemistry.
journal_name
Curr Pharm Desjournal_title
Current pharmaceutical designauthors
Tagliapietra S,Binello A,Bucciol F,Trukhan V,Colia M,Cravotto Gdoi
10.2174/1381612826999201116163951subject
Has Abstractpub_date
2020-01-01 00:00:00pages
5700-5712issue
44eissn
1381-6128issn
1873-4286pii
CPD-EPUB-111550journal_volume
26pub_type
杂志文章abstract::The oncoproteins MDM2 and MDMX negatively regulate the activity and stability of the p53 tumor suppressor, directly contributing to the development and progression of many tumors harboring wild type p53. Antagonizing MDM2 and MDMX to activate the p53 pathway has thus become an attractive new strategy for anticancer dr...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/138161211795222577
更新日期:2011-01-01 00:00:00
abstract::Gene delivery, a process of introducing foreign functional nucleic acids into target cells, has proven to be a very promising tool for inducing specific gene expression in host cells. Many different technologies have been developed for efficient gene delivery. Among them, electroporation has been adopted in gene deliv...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/1381612821666151027152121
更新日期:2015-01-01 00:00:00
abstract::The role of polyphenols in the cardiovascular diseases prevention is still a matter of scientific discussion. However, recent clinical studies indicate that intake of anthocyanins and in a lesser extent procyanidins can participate in prevention of hypertension and type 2 diabetes. Fruits of Aronia melanocarpa (chokeb...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/1381612822666151112152143
更新日期:2016-01-01 00:00:00
abstract::The skin remains an attractive area for drug delivery. The skin, however, often limits the ingress of drugs, because of its very low permeability. Much research, focusing on employing a variety of physical and chemical methods, aimed at reversibly altering skin permeability in favour of compounds, has been reported. O...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/1381612821666150428125812
更新日期:2015-01-01 00:00:00
abstract::DNA methylation is an important regulatory component which influences phenotypes by modulating gene expression. Changes in DNA methylation may lead to altered phenotypes and ability of an organism to respond to stress leading to subsequent manifestation of life style diseases, cancer, etc. The human X chromosome repre...
journal_title:Current pharmaceutical design
pub_type: 杂志文章
doi:10.2174/13816128113199990518
更新日期:2014-01-01 00:00:00
abstract::The American Academy of Pediatrics has proposed guidelines for treating term/near term infants with hyperbilirubinemia based primarily on maintaining the total serum bilirubin concentration (TSB) below a "critical" level of 25 mg/dL (426 micromol/L). We estimated the sensitivity and specificity of this critical TSB us...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/138161209789058228
更新日期:2009-01-01 00:00:00
abstract:BACKGROUND:The HERC family contains six members from HERC1 to HERC6 that are featured with the HECT domains that exerts ubiquitin ligase activity and the RCC1-like domains that are involved in cell cycle regulation. Although identified as early as 1990s, their biological functions are extensively studied in recent year...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/1381612824666180528081024
更新日期:2018-01-01 00:00:00
abstract:OBJECTIVE:High prevalence of Dental and periodontal problems during the gestation period may have a negative effect on oral health-related quality of life (OHRQoL) in pregnant women. This systematic review aimed to perform a quality assessment and provide a critical overview of the current research available on OHRQoL ...
journal_title:Current pharmaceutical design
pub_type: 杂志文章
doi:10.2174/1381612826666200523171639
更新日期:2020-01-01 00:00:00
abstract:BACKGROUND:Cardiovascular disease (CVD) despite the advances in medical management keeps on as the primary cause of morbidity and mortality for both genders in Western societies. Sex differences though modify the clinical picture as well as the effectiveness of treatment. METHODS AND RESULTS:In this literature review ...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/1381612822666160606202111
更新日期:2016-01-01 00:00:00
abstract::Immune complexes are major pathogenic factors contributing to tissue injury in a number of autoimmune diseases. Immune complexes consist of autoantibodies to self-antigens, which initiate an inflammatory response through binding to immunoglobulin Fc receptors (FcRs) or via complement components. The significance of Fc...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/1381612033454414
更新日期:2003-01-01 00:00:00
abstract::An important goal of biomedical research is to translate basic research findings into practical clinical implementation. Despite the advances in the technology used in drug discovery, the development of drugs for central nervous system diseases remains challenging. The failure rate for new drugs targeting important ce...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/1381612826666200224112534
更新日期:2020-01-01 00:00:00
abstract::DARPins (designed ankyrin repeat proteins), new kinds of binding proteins, have the potential to overcome the defects of monoclonal antibodies, and hence may become the alternatives to antibodies and generate a novel therapeutic approach. DARPins can be selected to bind any given target proteins with high affinity and...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/1381612811319120017
更新日期:2013-01-01 00:00:00
abstract::MicroRNAs (miRNAs) play a vital role in the onset and development of many diseases, including cancers. Emerging evidence shows that numerous miRNAs have the potential to be used as diagnostic biomarkers for cancers, and miRNA-based therapy may be a promising therapy for the treatment of malignant neoplasm. MicroRNA-14...
journal_title:Current pharmaceutical design
pub_type: 杂志文章
doi:10.2174/1381612826666201029095702
更新日期:2020-10-28 00:00:00
abstract::Recent progresses in the development of fluorescent technologies become a reliable device for drug discovery research. The fluorescence tools offer attractive options for an opportunity to visualize the effects of drug candidates in the cells. The fluorescent tools, such as fluorescent protein, are regularly used in a...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/138161209789207006
更新日期:2009-01-01 00:00:00
abstract::Cervical cancer is the second most common malignancy among women worldwide. While more than 90% of cervical cancers carry one or more high risk HPV types, the exact relationship between HPV oncoproteins and signaling pathways alterations in cervical cancer remains to be clarified. Vaccines and targeted therapies are t...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/138161213804805577
更新日期:2013-01-01 00:00:00
abstract::Alcohol dependence is a major disease burden of adults in modern society worldwide. There is no cure for alcohol dependence. In this study, we have examined the molecular targets of ethanol-induced toxicity in humans based on a systematic review of literature data and then discussed current and potential therapeutic t...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/138161210791034030
更新日期:2010-01-01 00:00:00
abstract::Vasopressin (AVP) secretion and release are regulated by a number of central nervous system sites that receive peripheral signals from the osmoreceptors and baroreceptors. Aim of this paper is to review anatomical pathways and neurotransmitters involved as well as drugs affecting AVP secretion. ...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/138161212802651607
更新日期:2012-01-01 00:00:00
abstract:PURPOSE:To summarize the main findings from research on food uses of Pine Bark Phenolic Extracts (PBPE), their origin, methods of extraction, composition, health effects, and incorporation into food products. METHODS:A narrative review of all the relevant papers known to the authors was conducted. RESULTS:PBPE are ma...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/1381612826666200212113903
更新日期:2020-01-01 00:00:00
abstract::Cancer and tumor have been major reasons for numerous deaths in this century across the world. Many strategies have been designed to treat, diagnose, or prevent cancer. The success of chemotherapy largely depends on drug targeting. The advent of nanotechnology has vastly improved drug delivery for targeting and diagno...
journal_title:Current pharmaceutical design
pub_type: 杂志文章
doi:10.2174/1381612826666200720235752
更新日期:2020-01-01 00:00:00
abstract::Alzheimer disease (AD) is characterized by excessive deposition of amyloid beta-peptides (Abeta peptides) in the form of senile plaques as well as neurofibrillary tangles (NFTs) in the brain. In the amyloidogenic pathway, the amyloid-beta precursor protein (APP) is cleaved by beta-secretase first, followed by gamma-se...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/138161206778792994
更新日期:2006-01-01 00:00:00
abstract::Synaptic transmission through descending motor pathways to lumbar motoneurons and then to leg muscles is essential for walking in humans and rats. Spinal cord injury (SCI), even when incomplete, results in diminished transmission to motoneurons and very limited recovery of motor function. Neurotrophins have emerged as...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/13816128113199990378
更新日期:2013-01-01 00:00:00
abstract::In recent years, new strategies in cancer therapy have been developed targeting key signaling molecules in the receptor tyrosine kinase signal transduction pathway. In contrast, most therapeutical concepts to manipulate G protein-coupled receptors (GPCR)-mediated disorders are still limited to the use of receptor-spec...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/1381612043384367
更新日期:2004-01-01 00:00:00
abstract::During the last years, mass spectrometry has revolutionised protein biochemistry and has advanced to a superior tool for the identification and detailed analysis of peptides and proteins. The high throughput allowed by some mass spectrometry platforms has enabled the important step from analysis of individual proteins...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/1381612054546932
更新日期:2005-01-01 00:00:00
abstract::In the mid seventies a drug design programme using the Amanita muscaria constituent muscimol (7) as a lead structure, led to the design of guvacine (23) and (R)-nipecotic acid (24) as specific GABA uptake inhibitors and the isomeric compounds isoguvacine (10) and isonipecotic acid (11) as specific GABAA receptor agoni...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/1381612003399608
更新日期:2000-08-01 00:00:00
abstract::Estrogens are known as important modulators of development, growth and maintenance of primary sexual physiology. The medical field has also grown increasingly appreciative of the effects of estrogens on non-traditional target tissues such as bone, cardiovascular tissue and the CNS. Postmenopausal women have been the b...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/1381612023393404
更新日期:2002-01-01 00:00:00
abstract::Regulation of cellular redox balances is important for the homeostasis of human health. Thus, many important human diseases, such as inflammation, diabetes, glaucoma, cancers, ischemia and neurodegenerative diseases, have been investigated in the field of reactive oxygen species (ROS) and oxidative stress. To overcome...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/138161211797052600
更新日期:2011-01-01 00:00:00
abstract::The prevalence of hypertension (HTN) worldwide is high and is constantly rising. HTN is considered to be a silent killer since often there are no obvious symptoms but long-term, HTN significantly increases the risk of coronary heart disease and cerebrovascular diseases. Those with diagnosed HTN or at high risk of its ...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/1381612823666170215144649
更新日期:2017-01-01 00:00:00
abstract::Hyperferritinemia is observed in one-third of patients with non-alcoholic fatty liver disease (NAFLD) and Metabolic Syndrome (MetS). The condition characterized by increased body iron stores associated with components of MetS has been defined as Dysmetabolic Iron Overload Syndrome (DIOS). DIOS represents the most freq...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/1381612826666200131103018
更新日期:2020-01-01 00:00:00
abstract::Heat shock proteins (HSPs) are involved in a number of cellular processes, including cell cycle, growth, and survival, apoptosis, stress responses, angiogenesis, and oncogenesis. Among the characterized HSPs, the molecular chaperone HSP90 has emerged as an exciting molecular target for cancer therapy since its discove...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:
更新日期:2013-01-01 00:00:00
abstract::Since their proposal in 1976, sigma (σ) receptors have been increasingly implicated in the pathophysiology of virtually all major central nervous system (CNS) disorders, including anxiety, depression, schizophrenia, and drug addiction. Due to their involvement in motor function and higher cognitive function,σ recepto...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/138161212799436539
更新日期:2012-01-01 00:00:00