1,721,096 research outputs found
Synthesis and evaluation of indole based molecules for treatment of oxidative stress related diseases
No full textThe chemical versatility of the indole nucleus still inspires the pharmaceutical research to develop innovative suitable indole based drugs. The present work is an overview of the use and application of indole molecule based derivatives, as possible treatment in the main Oxidative Stress related diseases, such as cardiovascular, neurological, and cancer. The indole nucleus is a particular class of reducers, very efficient when bearing aliphatic substitutions in position 3, like that found in tryptophan (Trp). The principal chemical modifications carried out on the indole nucleus, were focused to obtain orally active drugs for a simpler delivery to the patients
Acute rejection and graft survival in renal transplanted patients with viral diseases. Response.
No full text
Ligandi TRPV1
No full textLa presente invenzione concerne composti aventi alta affinità, capaci di legare il recettore canale permeabile ai cationi transient receptor potential, sottofamiglia Vanilloide, tipo 1 o TRPV1. Essendo questo recettore coinvolto in processi dolorosi e in risposte infiammatorie neurogene ed essendo sovra-regolato durante condizioni di dolore cronico, i composti dell’invenzione trovano particolare applicazione in tutte le condizioni mediche coinvolgenti detti recettori, in particolare come agenti per la terapia del dolore e/o antiinfiammatoria e/o della terapia della cefalea a grappolo e/o antiossidante e/o per la terapia antitumorale. Inoltre, la struttura chimica di questi composti fornisce l’opportunità di sviluppare nuovi radiofarmaci per la Positron Emission Tomography (PET) imaging. Questi radiofarmaci sono di notevole importanza per la mappatura dei recettori TRPV1 in condizioni (pato)fisiologiche
Gene expression of Transforming growth factor beta receptors I and II in non-small-cell lung tumors.
No full textTRPV1-FAAH-COX: The Couples Game in Pain Treatment
Full text linkPain is a complex sensation involving the perception and transduction of diverse environmental pain stimuli with cognitive and emotional processing by the central nervous system. It can manifest as acute or chronic pain. Pain is controlled by a series of enzymes and receptors, implicated in a variety of interconnected mechanisms and pathways. In fact, several studies have shown the cannabinoid receptor1 and the transient receptor potential vanilloid channel1 to be new players in modulating the sophisticated pain transduction system at the central level. At the peripheral level, the perception of pain involves cyclooxygenases and fatty acid amide hydrolase, as recent studies demonstrate. This Minireview describes the physiological aspects of the receptors and enzymes mentioned above and focuses on the consideration of dual mechanisms as a new therapeutic approach in the treatment of pain
Triazolopyrimidinium salts: discovery of a new class of agents for cancer therapy
No full textAim: The [1,2,4]triazolo[1,5-a]pyrimidine core is highly privileged in medicinal chemistry due to its versatile pharmacological activity profile. Recently, the search for novel anticancer agents has focused on [1,2,4]triazolo[1,5-a]pyrimidine derivatives. Results: Our hit functionalization has led to the discovery of new [1,2,4]triazolo[1,5-a]pyrimidinium salts with potential anticancer activity. Among a small library of molecules, compound 9 significantly inhibits cancer cell growth in a panel of in vitro models. Molecular docking studies and preliminary binding assay have displayed that 9 could directly bind the Src homology 2 (SH2) domain of STAT3 protein. Conclusion: Compound 9 is a novel promising lead compound that motivates additional evaluation of [1,2,4]triazolo[1,5-a]pyrimidinium salts as novel potential chemotherapeutics
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