1,721,141 research outputs found
Diarylurea: A Privileged Scaffold in Drug Discovery and Therapeutic Development
Full text linkdiarylure
Antiarrhythmic mexiletine: A review on synthetic routes to racemic and homochiral mexiletine and its enantioseparation
No full textMexiletine is an oral class IB antiarrhythmic agent. Although it was primarily studied for the treatment of ventricular arrhythmias, it has been demonstrated to be useful also for the treatment of chronic painful diabetic neuropathy, neuropathic pain, skeletal muscle channelopathies, and recently amyotrophic lateral sclerosis. This review presents a detailed report on the different synthetic routes to racemic and homochiral mexiletine developed in the last decades, as well as analytical studies regarding enantioseparation methods and enantiomeric excess determination. Finally, some analogues of mexiletine reported in the literature, most of which along with pharmacological studies, have been mentioned
1, 3‐Benzothiazoles as Antimicrobial Agents
No full textNovember 2015 1,3-Benzothiazoles as Antimicrobial Agents 1705Ivana Defrenza, Alessia Catalano,*Alessia Carocci,*Antonio Carrieri, Marilena Muraglia, Antonio Rosato,Filomena Corbo, and Carlo FranchiniDipartimento di Farmacia-Scienze del Farmaco, Università degli Studi di Bari ‘Aldo Moro’, via E. Orabona n. 4, 70125 Bari, Italy*E-mail: [email protected]; [email protected] November 5, 2013DOI 10.1002/jhet.2222Published online 24 October 2014 in Wiley Online Library (wileyonlinelibrary.com).Starting from 2-amino-1,3-mercaptobenzothiazoles recently reported (1a–h), a series of the corresponding2-mercapto-1,3-benzothiazole isosters (2a–h) were screened for their in vitro antibacterial and antifungalactivities. Results underline that the presence of the mercapto moiety at the 2-position of the heterocyclic nu-cleus is crucial for activity against bacteria. The biological screening against Candida spp. identified com-mercial 2f as the most promising compound as antifungal against Candida albicans and tropicalis.Molecular modeling studies supported these results. Then, to enlarge structure-activity relationship (SAR)studies on series 1, newly synthesized compounds (1k–p) were reported. All the compounds belonging to thisseries and bearing a bulky substituent at the 6-position of the aryl moiety showed high antifungal activity
Synthesis and biological evaluation of pyrrolidine derivatives as new ligands of AT1 receptors
No full textMexiletine metabolites: A review
No full textMexiletine belongs to class IB antiarrhythmic drugs and it is still considered a drug of choice for treating myotonias. However some patients do not respond to mexiletine or have significant side effects limiting its use; thus, alternatives to this drug should be envisaged. Mexiletine is extensive metabolized in humans via phase I and phase II reactions. Only a small fraction (about 10%) of the dose of mexiletine administered is recovered without modifications in urine. Although in the past decades Mex metabolites were reported to be devoid of biological activity, recent studies seem to deny this assertion. Actually, several hydroxylated metabolites showed pharmacological activity similar to that of Mex, thus contributing to its clinical profile. Purpose of this review is to summarize all the studies proposed till now about mexiletine metabolites, regarding structureactivity relationship studies as well as synthetic strategies. Biological and analytical studies will be also reported
Melatonergic drugs in development
Full text linkAlessia Carocci,1 Alessia Catalano,1 Maria Stefania Sinicropi2 1Department of Pharmacy–Drug Sciences, University of Bari Aldo Moro, Bari, 2Department of Pharmacy, Health and Nutritional Sciences, University of Calabria, Cosenza, Italy Abstract: Melatonin (N-acetyl-5-methoxytryptamine) is widely known as "the darkness hormone". It is a major chronobiological regulator involved in circadian phasing and sleep-wake cycle in humans. Numerous other functions, including cyto/neuroprotection, immune modulation, and energy metabolism have been ascribed to melatonin. A variety of studies have revealed a role for melatonin and its receptors in different pathophysiological conditions. However, the suitability of melatonin as a drug is limited because of its short half-life, poor oral bioavailability, and ubiquitous action. Due to the therapeutic potential of melatonin in a wide variety of clinical conditions, the development of new agents able to interact selectively with melatonin receptors has become an area of great interest during the last decade. Therefore, the field of melatonergic receptor agonists comprises a great number of structurally different chemical entities, which range from indolic to nonindolic compounds. Melatonergic agonists are suitable for sleep disturbances, neuropsychiatric disorders related to circadian dysphasing, and metabolic diseases associated with insulin resistance. The results of preclinical studies on animal models show that melatonin receptor agonists can be considered promising agents for the treatment of central nervous system-related pathologies. An overview of recent advances in the field of investigational melatonergic drugs will be presented in this review. Keywords: MT1/MT2 ligands, circadian rhythms, melatonin 
Organofluorinecontaining anti-infective agents
No full textFluorine atom is a suitable bioisostere in diverse organofluorine compounds acting as anti-infective agents
Going Beyond Counting First Authors in Author Co-citation Analysis
Full text linkThe present study examines one of the fundamental aspects of author co-citation analysis (ACA) - the way co-citation
counts are defined. Co-citation counting provides the data on which all subsequent statistical analyses and mappings
are based, and we compare ACA results based on two different types of co-citation counting - the traditional type that
only counts the first one among a cited work's authors on the one hand and a non-traditional type that takes into
account the first 5 authors of a cited work on the other hand. Results indicate that the picture produced through this non-traditional author co-citation counting contains more coherent author groups and is therefore considerably clearer. However, this picture represents fewer specialties in the research field being studied than that produced through the traditional first-author co-citation counting when the same number of top-ranked authors is selected and analyzed. Reasons for these effects are discussed
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