Recent patents on anti-infective drug discovery最新文献

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Current Approaches and Future Prospects of Nanomedicine in Tuberculosis Therapy. 纳米医学在结核病治疗中的应用现状与展望。
Recent patents on anti-infective drug discovery Pub Date : 2017-01-01 DOI: 10.2174/1574891X12666170425122416
Mohammad T Athar, Zabih Ullah
{"title":"Current Approaches and Future Prospects of Nanomedicine in Tuberculosis Therapy.","authors":"Mohammad T Athar,&nbsp;Zabih Ullah","doi":"10.2174/1574891X12666170425122416","DOIUrl":"https://doi.org/10.2174/1574891X12666170425122416","url":null,"abstract":"<p><strong>Background: </strong>Tuberculosis (TB), which is caused by the Mycobacterium tuberculosis, is a serious threat and one of the major health problems worldwide.</p><p><strong>Objective: </strong>In recent years, an estimated of 9.6 million TB cases occurred and 1.5 million death occurred due to TB worldwide.</p><p><strong>Conclusion: </strong>The present review is an attempt to introduce this disease focusing on the pathophysiology of the disease, the current approaches and the related patents for treatment and the future planning for combating this disease.</p>","PeriodicalId":20909,"journal":{"name":"Recent patents on anti-infective drug discovery","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2017-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"34942248","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}
引用次数: 2
Nanoemulsion-Based Transdermal Drug Delivery System for the Treatment of Tuberculosis. 基于纳米乳化剂的经皮给药系统治疗结核病。
Recent patents on anti-infective drug discovery Pub Date : 2017-01-01 DOI: 10.2174/1574891X12666170602075733
Mohammad Wais, Mohammad Aqil, Priyanka Goswami, Jaya Agnihotri, Sayyed Nadeem
{"title":"Nanoemulsion-Based Transdermal Drug Delivery System for the Treatment of Tuberculosis.","authors":"Mohammad Wais,&nbsp;Mohammad Aqil,&nbsp;Priyanka Goswami,&nbsp;Jaya Agnihotri,&nbsp;Sayyed Nadeem","doi":"10.2174/1574891X12666170602075733","DOIUrl":"https://doi.org/10.2174/1574891X12666170602075733","url":null,"abstract":"<p><strong>Background: </strong>The nanoemulsion based carriers are the most suitable delivery systems for poorly soluble drugs to improve the drugs solubility, permeation of drugs and ultimately increase bioavailability by transdermal therapeutic system. The nanoemulsion for poorly soluble drugs is admirable and offered several advantages over others drug delivery.</p><p><strong>Methods: </strong>For nanoemulsions formulation, they have to deliver the energetic element at the specific organ with nominal uneasiness. Because of the prevention of hepatic first pass uptake transdermal course excel usual crest and trough plasma shape that usually comfort the administration. The antitubercular drugs relate to the formulation of Poly DL-Lactide-Co-Glycolide nanoparticles having an active substance encapsulated within and that the encapsulated substances are stable with respect to each other.</p><p><strong>Conclusion: </strong>The present study aimed to explore the challenges and methods in order to increase the solubility of poorly aqueous soluble drug for improved bioavailability alongwith relative study of toxicity problems related to anti-tubercular drug.</p>","PeriodicalId":20909,"journal":{"name":"Recent patents on anti-infective drug discovery","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2017-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"35051867","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}
引用次数: 9
An Overwiev of ORF Virus Infection in Humans and Animals. 人类和动物感染口蹄疫病毒的全面调查。
Recent patents on anti-infective drug discovery Pub Date : 2017-01-01 DOI: 10.2174/1574891X12666170602080301
Hayati Demiraslan, Gokcen Dinc, Mehmet Doganay
{"title":"An Overwiev of ORF Virus Infection in Humans and Animals.","authors":"Hayati Demiraslan,&nbsp;Gokcen Dinc,&nbsp;Mehmet Doganay","doi":"10.2174/1574891X12666170602080301","DOIUrl":"https://doi.org/10.2174/1574891X12666170602080301","url":null,"abstract":"<p><strong>Background: </strong>Orf virus is a DNA virus that belongs to the Parapoxvirus genus. The virus is a causative agent of orf in humans or contagious ecthyma in animals which is mostly seen in sheep, goat and cattle.</p><p><strong>Discussion: </strong>Orf is an emerging zoonosis with an increasing number of worldwide outbreaks that have been reported. It is a contagious disease that tends to spread very fast among livestock. The morbidity rate is very high, particularly among young unvaccinated animals. The fatality rate is low but can be seen due to secondary infections. The disease has a significant effect on livestock health and may lead to economical losses. Humans may become infected if they have a direct contact with animal lesions. The disease is seen as a cutaneous lesion with a mild clinical outcome. Human to human transmission exists but is very rare. Nosocomial transmission was reported with one outbreak in a burn unit. The diagnosis is mostly based on the history of animal contact and clinical findings. Molecular tests are used to confirm clinical diagnose. There is no specific treatment but a live vaccine is available for animals. Surveillance implementations and infection control measurements are very important for the prevention of infection. Currently, there are limited studies on orf or contagious ecthyma. It has been observed that there are few studies that have resulted in patents.</p><p><strong>Conclusion: </strong>The aim of this paper was to review the current relevant patents, epidemiological features, clinical presentations, the diagnosis and treatment of orf.</p>","PeriodicalId":20909,"journal":{"name":"Recent patents on anti-infective drug discovery","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2017-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"35051868","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}
引用次数: 14
Editorial: Nanomedicines for the Treatment of Tuberculosis: Role of Nanocarriers and Functional Excipients. 社论:治疗肺结核的纳米药物:纳米载体和功能赋形剂的作用。
Recent patents on anti-infective drug discovery Pub Date : 2017-01-01 DOI: 10.2174/1574891X1202180503101725
Abdus Samad, Iram Nazish, Sarwar Beg
{"title":"Editorial: Nanomedicines for the Treatment of Tuberculosis: Role of Nanocarriers and Functional Excipients.","authors":"Abdus Samad,&nbsp;Iram Nazish,&nbsp;Sarwar Beg","doi":"10.2174/1574891X1202180503101725","DOIUrl":"https://doi.org/10.2174/1574891X1202180503101725","url":null,"abstract":"","PeriodicalId":20909,"journal":{"name":"Recent patents on anti-infective drug discovery","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2017-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.2174/1574891X1202180503101725","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"36085065","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}
引用次数: 0
Recent Complications and Issues in Tuberculosis Treatment. 结核病治疗的近期并发症和问题。
Recent patents on anti-infective drug discovery Pub Date : 2017-01-01 DOI: 10.2174/1574891X12666171006104430
Mohammad Taleuzzaman, Vinay Kumar
{"title":"Recent Complications and Issues in Tuberculosis Treatment.","authors":"Mohammad Taleuzzaman,&nbsp;Vinay Kumar","doi":"10.2174/1574891X12666171006104430","DOIUrl":"https://doi.org/10.2174/1574891X12666171006104430","url":null,"abstract":"<p><strong>Background: </strong>Tuberculosis is one of the major communicable diseases which can be prevented and cured. The prevalence of tuberculosis infection is more despite this disease causes major morbidity and mortality. To establish connection between tuberculosis (TB) related stigma and hindrance in search of a treatment after the inception of symptoms associated with tuberculosis.</p><p><strong>Methods: </strong>Physicians conducted the interviews using a structured questionnaire. Information from the medical reports available at health care centers (especial results of sputum microscopy, radiological and other investigations) was also distracted. Patients is said to be infected with TB having a minimum two initial +ve sputum smears or one +ve sputum smear and chest radiographic abnormalities along with active pulmonary TB as determined by clinician; one sputum +ve culture specimen +ve for Mycobacterium tuberculosis. High resolution computed tomography (HRCT), a new susceptible technique shows erratically disseminated military nodules. The organs associated and extents of lesions of miliary TB in the pulmonary tuberculosis are examined by ultrasonography, computed tomography (CT) and magnetic resonance imaging (MRI). Histopathological examination of tissue biopsy is a conservative and fast technique for the separation of mycobacterium tuberculosis and assessment of choroid tubercles in fundus.</p><p><strong>Conclusion: </strong>Even though numerous prognostic markers have been described which envisage mortality, yet untreated miliary TB has a serious outcome within one year. A high index of clinical research, early diagnosis and timely institution of anti-tuberculosis treatment can be life-saving. Response to first-line anti-tuberculosis drugs is good. Anti-tuberculosis drugs are patent.</p>","PeriodicalId":20909,"journal":{"name":"Recent patents on anti-infective drug discovery","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2017-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"35427045","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}
引用次数: 4
Macrophage Targeted Cellular Carriers for Effective Delivery of Anti-Tubercular Drugs. 巨噬细胞靶向细胞载体有效递送抗结核药物。
Recent patents on anti-infective drug discovery Pub Date : 2017-01-01 DOI: 10.2174/1574891X13666171207151313
Jaya Agnihotri, Sobhna Singh, Mohammad Wais, Abhishek Pathak
{"title":"Macrophage Targeted Cellular Carriers for Effective Delivery of Anti-Tubercular Drugs.","authors":"Jaya Agnihotri,&nbsp;Sobhna Singh,&nbsp;Mohammad Wais,&nbsp;Abhishek Pathak","doi":"10.2174/1574891X13666171207151313","DOIUrl":"https://doi.org/10.2174/1574891X13666171207151313","url":null,"abstract":"<p><strong>Background: </strong>Newly developed vaccine VPM1002 confers paradigm swing in the prophylactic treatment of tuberculosis (TB). Multi-drug resistant and latent TB in adults as well as in underprivileged patients is instigating menace over world population if the host is immune-compromised.</p><p><strong>Methods: </strong>One third of the world's population is infected with TB. Recently it is estimated around 9.6 million people around the world became sick with TB disease. There were 1.5 million TB-related deaths worldwide. Therefore with the advent in biotechnology and Nano engineering, newly adapted survival molecular mechanism of Mycobacterium tuberculosis, new targets receptors on alveolar macrophages must be explored out for eradication of TB from the globe. Macrophage acts as a reservoir of phagocytic receptors to execute diverse physiological functions as well as to perform defense mechanism.</p><p><strong>Results: </strong>Advances in novel carriers open new era for the treatment of tuberculosis which remains a very substantial global health encumbrance. Different binding receptors especially mannose, folate and scavenger receptors are attractive platform for internalization of therapeutics in alveolar macrophage. Nano-carriers and nano-devices designed after the acquaintance of receptor composition and functioning affords site specific targeting of biodegradable and biocompatible drug delivery systems for the treatment of tuberculosis offering complete cure and patient compliance.</p><p><strong>Conclusion: </strong>This chapter encompasses recent studies on nanocarriers and new treatment strategies for tuberculosis. In spite of the budding benefits of nano carriers, many limitations still remain to be overcome such as poor oral stability, instability in circulation, inadequate tissue distribution as well as toxicity to normal cells.</p>","PeriodicalId":20909,"journal":{"name":"Recent patents on anti-infective drug discovery","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2017-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"35323678","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}
引用次数: 0
Antibiotic Effects of Loperamide: Homology of Human Targets of Loperamide with Targets in Acanthamoeba spp. 洛哌丁胺的抗生素作用:洛哌丁胺人靶点与棘阿米巴原虫靶点的同源性。
Recent patents on anti-infective drug discovery Pub Date : 2017-01-01 DOI: 10.2174/1574891X12666170425170544
Abdul M Baig, Zohaib Rana, Mohsin Mannan, Sumayya Tariq, H R Ahmad
{"title":"Antibiotic Effects of Loperamide: Homology of Human Targets of Loperamide with Targets in Acanthamoeba spp.","authors":"Abdul M Baig,&nbsp;Zohaib Rana,&nbsp;Mohsin Mannan,&nbsp;Sumayya Tariq,&nbsp;H R Ahmad","doi":"10.2174/1574891X12666170425170544","DOIUrl":"https://doi.org/10.2174/1574891X12666170425170544","url":null,"abstract":"<p><strong>Background: </strong>Loperamide is an anti-diarrheal drug prescribed for non-infectious diarrhea. The drug is an opioid receptor agonist, blocker of voltage-dependent calcium channel (Cav) and calmodulin (CaM) inhibitor on human cells. Loperamide has been reported to exert anti-amoebic effects against pathogenic strains of Acanthamoeba castellanii.</p><p><strong>Objectives: </strong>The precise mode of antibiotic action, cellular target homology with human counterparts and the pattern of cell death induced by loperamide in Acanthamoeba castellanii remain to be established. Additionally, we attempt to establish the presence a primitive Cav in Acanthamoeba castellanii.</p><p><strong>Methods: </strong>Bioinformatics, 3D structural modelling, ligand binding predictions and apoptotic/ amoebicidal assays were used in this study to answer the above queries. Amino acid sequences and structural models were compared between human and A. castellanii proteins that are involved in the regulation of calcium (Ca+2) homeostasis.</p><p><strong>Results: </strong>Our results show that A. castellanii expresses similar, to near identical types of primitive calcium channels Cav Ac and CaM that are well known targets of loperamide in humans. The growth assays showed anti-amoebic effects of loperamide at different doses, both alone and in combinations with other Ca+2- CaM inhibitors. The synergistic actions of loperamide with haloperidol showed to be more amoebicidal than when either of them used alone. Imaging with Annexin V, Acridine orange and Propidium iodide showed apoptosis in A. castellanii at a dose of 100 µg/ml and necrosis at higher doses of 250 µg/ml.</p><p><strong>Conclusion: </strong>Though, Acanthamoeba does not express a homolog of the human mu-opioid receptor, but does shows evidence of the homologs for other known human targets of loperamide that are involved in Ca+2 uptake and Ca+2 signal transduction pathways. This suggests optimization of similar drug interactions with these targets may be useful in developing new approaches to control the growth of this parasite and possibly the diseases caused by it.</p>","PeriodicalId":20909,"journal":{"name":"Recent patents on anti-infective drug discovery","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2017-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"34996353","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}
引用次数: 7
Nanostructured Therapeutic Carriers for Tuberculosis Treatment: Approaches & Challenges. 纳米结构结核治疗载体:方法与挑战。
Recent patents on anti-infective drug discovery Pub Date : 2017-01-01 DOI: 10.2174/1574891X12666171006105409
Zabih Ullah, Mohammad T Athar, Abdus Samad
{"title":"Nanostructured Therapeutic Carriers for Tuberculosis Treatment: Approaches & Challenges.","authors":"Zabih Ullah,&nbsp;Mohammad T Athar,&nbsp;Abdus Samad","doi":"10.2174/1574891X12666171006105409","DOIUrl":"https://doi.org/10.2174/1574891X12666171006105409","url":null,"abstract":"<p><strong>Background: </strong>The diseases tuberculosis, triggered by intracellular pathogens, is a major problem for the global medical professionals. Treatments for these diseases through conventional dosage form consist of long-term therapy with multiple drugs, leading to several side effects and contribute to low patient compliance and drug resistance. The pathogens are found to be situated in the intracellular compartments of the cells, which ultimately results in additional blockades to effective treatment. Therefore, improved and more efficient therapies for such intracellular diseases are required.</p><p><strong>Methods: </strong>This review discusses the potential of nanomedicine and related patents to improve intracellular disease chemotherapy. To complete the objective, we searched bibliographic databases of indexed literature using a focused and structured criteria. The quality and characteristics of selected papers were assessed using standard parameters with qualitative analysis having a conceptual framework.</p><p><strong>Results: </strong>Nanoparticle-based drug delivery systems are suitable for the treatment of illnesses, such as tuberculosis. Due to the unique size-dependent properties, nanocarriers such as nanoparticles, liposomes, niosomes and microspheres offer the opportunity to develop new therapeutic and diagnostic tools. The ability to integrate drugs into nanosystems displays a new standard in pharmacotherapy that could be used for cell-targeted drug therapy. Experimental data showed the possibility of intermittent chemotherapy with main antituberculosis drugs by employing nanocarriers. Besides the advantage of the controlled release of medications in organs, the other benefits of the nanocarriers include the possibility of various routes of therapy, reduction in drug dosage and adverse effects, reduced possibility of drug interactions, and drug-resistant targeting. Published literature including patented studies suggests that nanomedicine mediated drug delivery may improve tuberculosis chemotherapy by offering benefits such as targeting to the specific organs, sustained and controlled drug release, tuberculosis diagnosis, drug delivery to the pathogen's intracellular location, and tuberculosis vaccine development.</p><p><strong>Conclusion: </strong>The properties of nanomedicine may prove beneficial in developing improved, efficacious or alternative therapies for tuberculosis diseases.</p>","PeriodicalId":20909,"journal":{"name":"Recent patents on anti-infective drug discovery","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2017-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"35427044","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}
引用次数: 0
New Drugs and Vaccines for Tuberculosis. 新的结核病药物和疫苗。
Recent patents on anti-infective drug discovery Pub Date : 2017-01-01 DOI: 10.2174/1574891X12666171006105921
Praveen K Gaur, Shikha Mishra
{"title":"New Drugs and Vaccines for Tuberculosis.","authors":"Praveen K Gaur,&nbsp;Shikha Mishra","doi":"10.2174/1574891X12666171006105921","DOIUrl":"https://doi.org/10.2174/1574891X12666171006105921","url":null,"abstract":"<p><strong>Background: </strong>Tuberculosis (TB) is an infectious disease that resulted in estimated 9.6 million new cases in 2014 and 1.5 million deaths. The available drug regimen for TB is time consuming which more often leads to the patient non compliance which then results in occurrence of drug resistant TB (Multi-drug and extremely drug resistant TB) in several portions of the world.</p><p><strong>Methods: </strong>The dangerous combinations of TB and HIV is taking its toll on human health. The foremost factor is non- profit associated with the development of anti TB drugs. There is almost 10 different drugs in various levels of trials whereas the vaccine development is focusing more on adult vaccine rather than a child vaccine.</p><p><strong>Results: </strong>More than 15 vaccine candidate are in various stages of pipelines. Present compilation gives an account for various drug candidates and vaccine products in various stages of drug development. Also included is a recent collection of patents for assay methods, potential drug candidates/classes and vaccination products.</p><p><strong>Conclusion: </strong>The need is for improvement in the activity and chemical and biological description of under development compounds. Lastly the set up for clinical and appropriate uses for running a reliable clinical trial is a necessary prerequisite.</p>","PeriodicalId":20909,"journal":{"name":"Recent patents on anti-infective drug discovery","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2017-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"35427047","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}
引用次数: 6
Targets and Patented Drugs for Chemotherapy of Chagas Disease in the Last 15 Years-Period. 近15年来恰加斯病化疗的靶点和专利药物
Recent patents on anti-infective drug discovery Pub Date : 2016-07-31 DOI: 10.2174/1574891X11666161024165304
V. Duschak
{"title":"Targets and Patented Drugs for Chemotherapy of Chagas Disease in the Last 15 Years-Period.","authors":"V. Duschak","doi":"10.2174/1574891X11666161024165304","DOIUrl":"https://doi.org/10.2174/1574891X11666161024165304","url":null,"abstract":"BACKGROUND\u0000The American trypanosomiasis, Chagas disease, is a parasitic infection typically spread by triatomine vectors affecting millions of people all over Latin America. Existing chemotherapy is centered on the nitroaromatic compounds benznidazole and nifurtimox that provide unsatisfactory results and substantial side effects. So, the finding and exploration of novel ways to challenge this neglected disease is a main priority.\u0000\u0000\u0000METHODS\u0000The biologic and biochemical progress in the scientific knowledge of Trypanosoma cruzi in the period comprising last 15-years has increased the identification of multiple targets for Chagas´ disease chemotherapy. In the middle of the best encouraging targets for trypanocidal drugs, ergosterol biosynthesis pathway and cruzipain, a key cysteine protease (CP) of T. cruzi, have been pointed out. Unfortunately, recent clinical trials investigating the administration of pozoconazole and ravuconazole to chronic indeterminate Chagas disease patients revealed their inferiority compared to the standard drug Benznidazole.\u0000\u0000\u0000RESULTS\u0000In view of the information gained in the preceding years, a reasonable approach for the fast development of novel anti-T. cruzi chemotherapy would be focused on K777, the cysteine proteinase inhibitor (CPI) near to enter to clinical trials, and founded on the clinical evaluation of combination of known drugs with existing trypanocidal agents to obtain more efficiency and less secondary effects. Top series of xanthine have been recently identified as clinical candidate for Chagas disease. In addition, trypanothione biosynthesis, thiol-dependant redox and polyamine metabolism, the glycolytic, glyconeogenic, pentose phosphate, lipidic and polyisoprenoid biosynthetic pathways, and the enzymes from biosynthetic glycoconjugates pathways have been studied. Several specific enzymes from these particular biosynthetic pathways such as hypoxanthine-guaninephosphoribosyl- transferase and farnesyl-pyrophosphate synthase, among others, have also been broadly studied in T. cruzi. Novel synthesized anti-T. cruzi compounds with or without specific single or multi-target assigned are also described in detail.\u0000\u0000\u0000CONCLUSION\u0000In summary, loans on anti-Chagas disease agents focused to specific parasite targets as their metabolic pathways or specific enzymes will be summarized. Targets will also be specifically discussed. Patent literature collected and published from 2000 to 2015, alleging inhibitors for specific T. cruzi targets or trypanocidal activity was achieved over the search database from Delphion Research intellectual property network including international patents and the European patent office, Espacenet.","PeriodicalId":20909,"journal":{"name":"Recent patents on anti-infective drug discovery","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2016-07-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.2174/1574891X11666161024165304","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"67992799","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}
引用次数: 27
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