1,721,074 research outputs found
Direct- and spacer-coupled codrug strategies for the treatment of Alzheimer’s disease
No full textOver the last years, the ‘multi-target-directed ligand’ strategy has been
exploited by many researchers to develop novel attractive tools in the search
for new agents for Alzheimer’s disease (AD). Small molecules that concurrently
target and modulate AD multiple pathological factors can be synthesized using
such strategy. This paper will mainly focus on direct- and spacer-coupled codrug
approaches that we recently rationally used to design multifunctional molecules
able to contrast oxidative stress, neuroinflammation, glutamate toxicity, and
metal dyshomeostasis, as a function of the structural elements introduced in the
chemical framework.
Although the potential use of these strategies needs further exhaustive
studies, it may offer a promising therapeutic alternative for increasing neuronal
protection and preventing AD progression
Microbial Infections and Wound Healing: Medicinal-Chemistry and Technological Based Approaches
Full text linkMicrobial infections represent a significant global health challenge that impacts all populations [...
Sintesi di trans-2-ammino-5(o 6)-cloro-6(o 5)-idrossi-1-fenil-2,3-diidro-1H-indani quali precursori di derivati a potenziale affinità per i recettori della dopamina
No full textRole of Dietary Supplements in the Management of Parkinson’s Disease
Full text linkThe use of food supplements or functional food has significantly increased in the past decades, especially to compensate both the modern lifestyle and the food shortages of the industrialized countries. Despite food supplements are habitually intended to correct nutritional deficiencies or to support specific physiological functions, they are often combined with common drug therapies to improve the patient’s health and/or mitigate the symptoms of many chronic diseases such as cardiovascular diseases, cystic fibrosis, cancer, liver and gastrointestinal diseases. In recent years, increased attentions are given to the patient’s diet, and the use of food supplements and functional food rich in vitamins and antioxidants plays a very important role in the treatment and prevention of neurodegenerative diseases such as Parkinson’s disease (PD). Natural compounds, phytochemicals, vitamins, and minerals can prevent, delay, or alleviate the clinical symptoms of PD in contrast to some of the main physiopathological mechanisms involved in the development of the disease, like oxidative stress, free radical formation, and neuroinflammation. The purpose of this review is to collect scientific evidences which support the use of specific biomolecules and biogenic elements commonly found in food supplements or functional food to improve the clinical framework of patients with PD
In vivo anti-apoptotic effect of compound 4 in rats infused with Aβ (1-40), as a model of Alzheimer’s disease
No full text
Structure-Activity relationships of biphalin analogs and their biological evaluation on opioid receptors
No full textBiphalin (Tyr-D-Ala-Gly-Phe-NH-NH<-Phe<-Gly<-D-Ala<-Tyr) is an opioid octapeptide with a dimeric structure based on two identical pharmacophore portions, derived from enkephalins, joined "tail to tail"by a hydrazide bridge. This particular structure enhances the antinociceptive activity of the native enkephalins with an unknown mechanism, probably based on a cooperative binding and improved enzymatic stability. Biphalin has excellent binding affinity for μ and δ receptors and it is a highly potent analgesic, as potent as or more potent than ethorphine. A definitive explanation of the extraordinary in vivo potency shown by this compound, which has pronounced efficacy in pain modulation, is still not available; it has been suggested, however, that the high agonist activity may be related to its binding mode at both μ and δ opioid receptors. Biphalin has significantly higher potency than other analgesics with novel biological profiles; in particular, most recent data show that biphalin is unlikely to produce dependency in chronic use. In the past 20 years, there have been many attempts to modify its structure to obtain products unaffected by the action of enkephalinases, to enhance its antinociceptive activity and to modify the BBB penetration. In addition, structure-activity relationship studies (SAR) were performed in order to understand the elements responsible for biphalin's high activity. The aim of the studies reported in this review was to clarify: i) the role of the hydrazide bridge, ii) the role of residues in position 4, 4' and 3, 3', iii) the consequences of molecular simplifications (truncation, delection), iv) the consequences of cyclization through a disulfide bridge, v) conjugation with PEG and fluorescet residues, and vi) radiolabeling on Tyr1
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