Anti-infective agents in medicinal chemistry最新文献

{"title":"Recent Advances on Isoniazide Derivatives","authors":"J. Vinšová, A. Imramovský, J. Jampílek, J. Monreal, M. Doležal","doi":"10.2174/187152108783329780","DOIUrl":"https://doi.org/10.2174/187152108783329780","url":null,"abstract":"Tuberculosis remains the leading cause of mortality worldwide even in the 21st century. This review summarises all facts concerning a front-line antituberculotic drug isoniazide – metabolism, mechanism of activity and resistance. The antimycobacterial pharmacophore moiety of isoniazide has been introduced in a number of various types of molecules (about 510 derivatives have been found) to improve their activity against Mycobacteria species, as well as their multidrug-resistant strains. Several Schiff bases, hydrazones, hydrazides and metal complexes of isoniazide have shown very good activity. Various types of the most active isoniazide derivatives classified according to their structure are reported, their lipophilicity has been calculated and structure-activity relationships are discussed. The original new highly active isoniazide prodrug forms prepared at the Faculty of Pharmacy, Charles University, Czech Republic are presented in a separate chapter of the paper.","PeriodicalId":89320,"journal":{"name":"Anti-infective agents in medicinal chemistry","volume":"49 1","pages":"12-31"},"PeriodicalIF":0.0,"publicationDate":"2008-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.2174/187152108783329780","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"68020681","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Enhanced Killing of Intracellular Pathogenic Bacteria by Phenothiazines and the Role of K+ Efflux Pumps of the Bacterium and the Killing Macrophage","authors":"L. Amaral, M. Martins, M. Viveiros","doi":"10.2174/187152108783329807","DOIUrl":"https://doi.org/10.2174/187152108783329807","url":null,"abstract":"","PeriodicalId":89320,"journal":{"name":"Anti-infective agents in medicinal chemistry","volume":"7 1","pages":"63-72"},"PeriodicalIF":0.0,"publicationDate":"2008-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.2174/187152108783329807","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"68021888","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Antibacterial Agents Against Methicillin-Resistant Staphylococcus aureus (MRSA) and Vancomycin-Resistant Enterococci (VRE)","authors":"M. O. Mitchell","doi":"10.2174/187152107782023114","DOIUrl":"https://doi.org/10.2174/187152107782023114","url":null,"abstract":"","PeriodicalId":89320,"journal":{"name":"Anti-infective agents in medicinal chemistry","volume":"6 1","pages":"243-247"},"PeriodicalIF":0.0,"publicationDate":"2007-09-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.2174/187152107782023114","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"68021169","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Inhibition of Membrane Fusion as a Target for Antiviral Therapy","authors":"Richard K. Plemper, A. Hammond","doi":"10.2174/187152107782023088","DOIUrl":"https://doi.org/10.2174/187152107782023088","url":null,"abstract":"","PeriodicalId":89320,"journal":{"name":"Anti-infective agents in medicinal chemistry","volume":"6 1","pages":"248-262"},"PeriodicalIF":0.0,"publicationDate":"2007-09-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.2174/187152107782023088","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"68021109","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"New Developments in Therapeutic Agents for Legionnaires Disease","authors":"J. Roig, J. Arnau, A. Vallano, J. Rello","doi":"10.2174/187152107782023079","DOIUrl":"https://doi.org/10.2174/187152107782023079","url":null,"abstract":"","PeriodicalId":89320,"journal":{"name":"Anti-infective agents in medicinal chemistry","volume":"52 1","pages":"228-242"},"PeriodicalIF":0.0,"publicationDate":"2007-09-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.2174/187152107782023079","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"68021070","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Structure-Function Relationship of Thiazolides, a Novel Class of Anti- Parasitic Drugs, Investigated in Intracellular and Extracellular Protozoan Parasites and Larval-Stage Cestodes","authors":"A. Hemphill, N. Müller, Joachim Müller","doi":"10.2174/187152107782023105","DOIUrl":"https://doi.org/10.2174/187152107782023105","url":null,"abstract":"The thiazolide nitazoxanide (2-acetolyloxy-N-(5-nitro 2-thiazolyl) benzamide; NTZ) is a compound that has been synthesized based on the structures of niclosamide (antihelminthic) and metronidazole (anti-anaerobic). It is essen- tially composed of a nitrothiazole-ring and a salicylic acid moiety, which are linked together through an amide bond. NTZ exhibits a broad spectrum of activities against a wide range of intestinal and tissue-dwelling helminths, protozoa, and en- teric bacteria infecting animals and humans. The drug has been postulated to act via reduction of its nitro-group by ni- troreductases including pyruvate ferredoxin oxidoreductase (PFOR), which would then generate a toxic radical that could have anti-parasitic and anti-bacterial activities. However, experimental evidence for this mode of action is lacking. In- stead, the drug has been shown to inhibit the functional activity of PFOR in several extracellular anaerobic organisms, but the activity against intracellular pathogens appears to be based on (an)other mechanism(s) of action. Since the first synthe- sis of the drug, a number of derivatives of NTZ have been produced, which are collectively named thiazolides. These are modified versions of NTZ, which include the replacement of the nitro-thiazole with other functional groups, and the dif- ferential positioning of methyl- and methoxy-groups on the salicylate ring. Investigations on the activities of these thiazol- ides were carried out by studying morphological and ultrastructural changes upon drug treatments, by defining physio- logical alterations, and by applying biochemical and genetic approaches to identify respective targets and the molecular basis of resistance formation. Collectively, these studies strongly suggest that NTZ and other thiazolides exhibit multiple mechanisms of action, targeting differential metabolic pathways, and each acting specifically against intracellular and ex- tracellular pathogens, respectively. This could explain the broad range of activities (anti-parasitic, anti-bacterial and anti- viral) of the thiazolide class.","PeriodicalId":89320,"journal":{"name":"Anti-infective agents in medicinal chemistry","volume":"6 1","pages":"273-282"},"PeriodicalIF":0.0,"publicationDate":"2007-09-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"68021156","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Antiidiotype-Derived Killer Peptides As New Potential Tools to Combat HIV-1 and AIDS-Related Opportunistic Pathogens","authors":"W. Magliani, S. Conti, D. L. Maffei, L. Ravanetti, L. Polonelli","doi":"10.2174/187152107782023060","DOIUrl":"https://doi.org/10.2174/187152107782023060","url":null,"abstract":"","PeriodicalId":89320,"journal":{"name":"Anti-infective agents in medicinal chemistry","volume":"6 1","pages":"263-272"},"PeriodicalIF":0.0,"publicationDate":"2007-09-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.2174/187152107782023060","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"68021061","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Two Different Functions of Doxycycline Which is Both An Antimicrobial Agent and An Immune Modulator","authors":"M. Fujita, Y. Nakanishi","doi":"10.2174/187152107782023097","DOIUrl":"https://doi.org/10.2174/187152107782023097","url":null,"abstract":"","PeriodicalId":89320,"journal":{"name":"Anti-infective agents in medicinal chemistry","volume":"6 1","pages":"222-227"},"PeriodicalIF":0.0,"publicationDate":"2007-09-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.2174/187152107782023097","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"68021122","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Novel Antiinflammatory and Antiinfective Agents","authors":"P. Garidel, J. Andrä, J. Howe, T. Gutsmann, K. Brandenburg","doi":"10.2174/187152107781023647","DOIUrl":"https://doi.org/10.2174/187152107781023647","url":null,"abstract":"","PeriodicalId":89320,"journal":{"name":"Anti-infective agents in medicinal chemistry","volume":"6 1","pages":"185-200"},"PeriodicalIF":0.0,"publicationDate":"2007-06-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"68020930","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Dendrimers and Dendritic Polymers as Anti-infective Agents: New Antimicrobial Strategies for Therapeutic Drugs","authors":"J. Rojo, R. Delgado","doi":"10.2174/187152107781023674","DOIUrl":"https://doi.org/10.2174/187152107781023674","url":null,"abstract":"Nearly 3 decades ago, a dendritic structure was stepwise synthesized for the first time as a new type of mole- cules with promising applications. During years a huge effort has been devoted to implement the synthetic skills concern- ing the synthesis of these molecules and especially, new methods for purification and characterization of these compounds that are in the nanoscale range. The chemical manipulation of the surface and inner core of dendrimers were strategically used to allow a tailor-made control of physical-chemical properties and to discover new applications in material science and biomedicine. Although several examples have been reported in the literature describing applications of functionalized dendrimers and acclaiming a key role of these molecules, very scarce examples are actually close to the market. This review summarizes the state of the art of dendrimers and dendritic polymers as anti-infective agents, with a special focus on the strategies to block receptors used by pathogens for attachment, cell entry and dissemination. These nanome- tre size molecules are very attractive compounds as new drugs easily to be manipulated to improve their activity and scope. This is already a very active area of research, where we are involved, with interesting potential as demonstrated by the Phase I clinical trial of a functionalized dendrimer with real possibilities to reach the market soon. The success of this compound should provoke an enormous stimulus to scientists working in this area as well as in the industrial companies for investment in this topic.","PeriodicalId":89320,"journal":{"name":"Anti-infective agents in medicinal chemistry","volume":"6 1","pages":"151-174"},"PeriodicalIF":0.0,"publicationDate":"2007-06-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.2174/187152107781023674","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"68021040","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}