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Recent patents on anti-infective drug discovery最新文献

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Preface 前言
Q3 Medicine Pub Date : 2019-10-21 DOI: 10.2174/1574891x1401191021170911
D. Kabelitz
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引用次数: 0
Meet Our Editorial Board Member 见见我们的编辑委员会成员
Q3 Medicine Pub Date : 2019-10-21 DOI: 10.2174/1574891x1401191021170733
A. Tsakris
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引用次数: 0
Patent Selection: 专利的选择:
Q3 Medicine Pub Date : 2019-10-21 DOI: 10.2174/187220831003161213115403
Bentham Science Publisher Bentham Science Publisher
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引用次数: 0
Nano-emulgel: Emerging as smarter topical lipidic emulsion based nanocarrier for skin Healthcare applications. 纳米乳液:作为皮肤保健应用中更智能的局部脂质乳液纳米载体。
Q3 Medicine Pub Date : 2019-05-01 DOI: 10.2174/1574891X14666190717111531
Kumar Anand, S. Ray, Mahfoozur Rahman, Adil Shaharyar, Rudranil Bhowmik, R. Bera, Sanmoy Karmakar
BACKGROUNDIn recent decades enormous effort of different drug discovery processes has led a number of drug molecules available to overcome different challenges of health care system. Unfortunately, more than half of these drugs are being listed in either BCS (biopharmaceutical classification system) class II/ IV or both and dropped from the development pipe line due to their limited clinical use. A Nanotechnological approach bears much hope and lipoidal fabrication of the same is found to be suitable systems for delivery of such drugs. Nanoemulsion based gel i.e. nanoemulgel out of different nanolipoidal formulations is found to be suitable for successful approach of drug delivery through topical route.METHODSNanoemulgel is basically an emulsion based topical gel formulation, where nano sized emulsion globules can be prepared with the help of high energy or low energy methods and further converted to nanoemulgel by adding a suitable gelling agent. Nanoemulgel fabrication enlists various kinds of polymeric materials, surfactants and fatty substances of natural, synthetic and semi synthetic nature resulting globule size range of 5 to 500 nm.RESULTSNanoemulgel can be applicable for various acute and chronic diseases through topical routes.CONCLUSIONNanoemulgel preparations of many recently approved drugs are being used successfully in different areas of health care and re-defining the significance of topical route of delivery as compared to other routes. However, along with various improvements in current state of delivery system, it also needs a serious concern related to safety and toxicological studies of the materials used for such formulation.
背景近几十年来,不同药物发现过程的巨大努力使许多药物分子能够克服医疗保健系统的不同挑战。不幸的是,这些药物中有一半以上被列入BCS(生物制药分类系统)II/IV类或两者兼有,由于其临床用途有限,因此从开发管道中删除。纳米技术方法有很大的希望,并且发现其脂质体制造是递送此类药物的合适系统。基于纳米乳液的凝胶,即来自不同纳米类脂制剂的纳米乳液凝胶,被发现适用于通过局部途径成功递送药物的方法。方法纳米乳液凝胶基本上是一种基于乳液的局部凝胶制剂,其中可以借助高能或低能方法制备纳米乳液球,并通过添加合适的胶凝剂进一步转化为纳米乳液凝胶。纳米乳胶凝胶的制造需要各种聚合物材料、表面活性剂和天然、合成和半合成性质的脂肪物质,产生的球大小范围为5至500nm。结果纳米乳胶凝胶可通过局部途径应用于各种急慢性疾病。结论许多最近批准的药物的纳米乳液制剂正在成功地用于不同的医疗保健领域,并重新定义了与其他途径相比,局部给药途径的重要性。然而,随着目前输送系统状态的各种改进,它也需要对用于此类制剂的材料的安全性和毒理学研究给予严重关注。
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引用次数: 30
Amarogentin as Topical Anticancer and Anti-Infective Potential: Scope of Lipid Based Vesicular in its Effective Delivery. 洋红素作为局部抗癌和抗感染的潜力:脂基囊泡在其有效递送中的范围。
Q3 Medicine Pub Date : 2019-01-01 DOI: 10.2174/1574891X13666180913154355
Kanika Patel, Vikas Kumar, Amita Verma, Mahfoozur Rahman, Dinesh K Patel

There is a need for the development of liposomes based nanomedicines formulation for better efficacy and safety of the available drugs in the market. Liposomes have various applications in the field of pharmaceutical and medical field for their drug target potential, diagnostic importance and imaging techniques. Natural plant based drugs and their derivatives have been used in the medicine, nutraceuticals, perfumery, cosmetic and beverages industry. More than half of the prescribed drugs in the worldwide are mainly derived from different natural sources. Development of plant derived product is an emerging field of food, pharmaceutical and health industries. Plants belonging to the Gentianaecae family are well known for their bitter taste and Swertia chirata is one of best plants among them. Various active phytochemical of Swertia chirata are bitter secoiridoids like gentiopicroside, amarogentin, swertiamarin, isovitexin and isogentisin. People use different species of Swertia in the form of decoction, infusion, paste and juice for the treatment of fever and enteric diseases. Swertia chirata possesses anticarcinogenic, antioxidative, hypoglycemic, antihepatotoxic, antimalarial, anti-inflammatory and antimicrobial activities. Amarogentin, a bitter secoiridoid glycoside present in Swertia chirata plant is an activator of human bitter taste receptor. Pharmacologically, amarogentin has antibacterial, antihepatitis, anticholinergic and chemopreventive activities, moreover, amarogentin has been proven for their anti-lieshmanial activity. Other studies also suggested that amarogentin acts on liver carcinogenesis, skin carcinogenesis and reduced tumour progression. In the present review, we have collected and compiled the data regarding biological sources, ethnomedicinal uses, phytochemistry, anticancer and anti-infective potential of amarogentin. For better understanding of various aspects of amarogentin, we have also discussed Swertia chirayita in a very concise manner. Further data related to various patents on amarogentin have also been discussed in this manuscript. However, we also admit that new advance biological research will also increase the medicinal and pharmacological value of amarogentin. Information regarding the chemistry of amarogentin, its biological sources, bioavailability as a pharmacological agent for the treatment and management of skin disorders and various forms of cancers will be beneficial to the scientists in the medicinal field.

为了提高市场上现有药物的疗效和安全性,有必要开发基于脂质体的纳米药物配方。脂质体以其潜在的药物靶点、诊断价值和成像技术在制药和医学领域有着广泛的应用。天然植物性药物及其衍生物已广泛应用于医药、保健品、香水、化妆品和饮料行业。全世界一半以上的处方药主要来自不同的天然来源。植物源性产品的开发是食品、医药和保健行业的一个新兴领域。龙胆科植物以其苦味而闻名,獐牙菜是其中最好的植物之一。獐牙獐牙獐牙菜的活性植物化学成分主要为苦环烯醚萜类化合物,如龙胆苦苷、獐牙獐牙菜苦苷、獐牙獐牙菜苦苷、异牡荆素和异龙胆皂苷等。人们将不同种类的獐牙菜以汤剂、冲剂、膏剂和果汁的形式用于治疗发烧和肠道疾病。獐牙菜具有抗癌、抗氧化、降血糖、抗肝毒、抗疟、抗炎、抗菌等作用。苦苦素是獐牙菜属植物中的一种苦味环烯醚萜苷,是人体苦味感受器的激活剂。药理学上,amarogentin具有抗菌、抗肝炎、抗胆碱能和化学预防活性,而且amarogentin还具有抗动物活性。其他研究也表明,amarogentin对肝癌、皮肤癌起作用,并减少肿瘤进展。本文对苦苣苔素的生物来源、民族医药用途、植物化学、抗癌和抗感染潜力等方面进行了综述。为了更好地了解苦苣苔素的各个方面,我们也以非常简洁的方式讨论了獐牙菜。进一步的数据有关的各种专利苋属植物素也讨论了在这篇手稿。然而,我们也承认,新的进展生物学研究也将增加amarogentin的药用和药理价值。关于amarogentin的化学成分、生物来源、生物利用度作为治疗和管理皮肤疾病和各种癌症的药理学制剂的信息将对医学领域的科学家有益。
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引用次数: 13
Topical Nano-emulgel for Skin Disorders: Formulation Approach and Characterization. 皮肤疾病局部纳米乳液:配方方法和表征。
Q3 Medicine Pub Date : 2019-01-01 DOI: 10.2174/1574891X14666181129115213
Javed Ahmad, Anuj Gautam, Shahadali Komath, Mehdiya Bano, Anuj Garg, Keerti Jain

Backgrounds: Acne vulgaris is a common chronic skin disease that affects around 9.4% (approx. 650 million people) of the global population. Growing research in the field of nanomedicine over the years has now been exploited in management of various human disorders. The nanomedicine concept has an immense opportunity for the effective management and control of acne disease by designing a novel, low-dose topical delivery system. Topical nanoemulsion-based gel preparations are said to have various benefits over the conventional formulations. The recent patents on topical anti-acne formulation (US 7241456B2; US 6897238B2; US 6284234B1) provided the concept to design thymol loaded nano-emulgel for topical application in acne.

Methods: The objective of the current investigation was to design a thymol loaded nanoemulgel preparation by exploiting low-energy emulsification method for topical application in acne. Furthermore, developed formulation was characterized for thermodynamic stability, mean droplet size, zeta potential, drug content and in-vitro drug diffusion study.

Results: The optimized thymol loaded nanoemulsion was found to be 13.60±0.117 nm with PdI 0.197±0.008. Nanoemulsions will provide an enormous surface area for better penetration of therapeutic agent into the pilosebaceous region, resulting better efficacy.

Conclusions: From the above studies, it concluded that aqueous-based gel vehicle of the developed formulation system exploited for topical delivery has moisturising properties which can improve local tolerability also.

背景:寻常痤疮是一种常见的慢性皮肤病,发病率约为9.4%。占全球人口的6.5亿。近年来,纳米医学领域的研究不断发展,现已被用于治疗各种人类疾病。纳米医学概念通过设计一种新颖的、低剂量的局部给药系统,为有效管理和控制痤疮疾病提供了巨大的机会。局部纳米乳化剂基凝胶制剂据说比常规制剂具有各种益处。最近获得的外用抗痘配方专利(US 7241456B2;我们6897238 b2;US 6284234B1)提供了设计百里香酚负载纳米乳液用于痤疮局部应用的概念。方法:采用低能乳化法制备百里香酚纳米乳液,用于痤疮外用。对制剂进行了热力学稳定性、平均滴度、zeta电位、药物含量和体外药物扩散研究。结果:优化后的百里香酚负载纳米乳粒径为13.60±0.117 nm, PdI为0.197±0.008。纳米乳液将提供巨大的表面积,使治疗剂更好地渗透到毛囊皮脂腺区域,从而获得更好的疗效。结论:从上述研究中得出结论,开发的用于局部给药的配方系统的水基凝胶载体具有保湿特性,也可以提高局部耐受性。
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引用次数: 38
Promising Role of Wolbachia as Anti-parasitic Drug Target and Eco-Friendly Biocontrol Agent. 沃尔巴克氏体作为抗寄生虫药物靶点和生态友好型生物防治剂的前景研究。
Q3 Medicine Pub Date : 2019-01-01 DOI: 10.2174/1574891X14666190211162403
Tooran Nayeri Chegeni, Mahdi Fakhar

Background: Wolbachia is the most common endosymbiotic bacteria in insectborne parasites and it is the most common reproductive parasite in the world. Wolbachia has been found worldwide in numerous arthropod and parasite species, including insects, terrestrial isopods, spiders, mites and filarial nematodes. There is a complicated relationship between Wolbachia and its hosts and in some cases, they create a mutual relationship instead of a parasitic relationship. Some species are not able to reproduce in the absence of infection with Wolbachia. Thus, the use of existing strains of Wolbachia bacteria offers a potential strategy for the control of the population of mosquitoes and other pests and diseases.

Methods: We searched ten databases and reviewed published papers regarding the role of Wolbachia as a promising drug target and emerging biological control agents of parasitic diseases between 1996 and 2017 (22 years) were considered eligible. Also, in the current study several patents (WO008652), (US7723062), and (US 0345249 A1) were reviewed.

Results: Endosymbiotic Wolbachia bacteria, which are inherited from mothers, is transmitted to mosquitoes and interferes with pathogen transmission. They can change the reproduction of their host. Wolbachia is transmitted through the cytoplasm of eggs and have evolved different mechanisms for manipulating the reproduction of its hosts, including the induction of reproductive incompatibility, parthenogenesis, and feminization. The extensive effects of Wolbachia on reproduction and host fitness have made Wolbachia the issue of growing attention as a potential biocontrol agent.

Conclusion: Wolbachia has opened a new window to design a costly, potent and ecofriendly drug target for effective treatment and elimination of vector-borne parasitic diseases.

背景:沃尔巴克氏体是虫媒寄生虫中最常见的内共生细菌,是世界上最常见的生殖寄生虫。沃尔巴克氏体在世界各地的许多节肢动物和寄生虫物种中被发现,包括昆虫、陆生等足动物、蜘蛛、螨虫和丝状线虫。沃尔巴克氏体和它的宿主之间有一种复杂的关系,在某些情况下,它们创造了一种相互关系,而不是寄生关系。有些物种在没有沃尔巴克氏体感染的情况下无法繁殖。因此,利用现有的沃尔巴克氏菌菌株为控制蚊子种群和其他病虫害提供了一种潜在的策略。方法:检索10个数据库,回顾1996年至2017年(22年)关于沃尔巴克氏体作为一种有前景的药物靶点和新兴寄生虫病生物防治剂作用的已发表论文。此外,本研究还审查了几项专利(WO008652)、(US7723062)和(US 0345249 A1)。结果:从母体遗传的内共生沃尔巴克氏菌可通过蚊虫传播,干扰病原体传播。它们可以改变宿主的繁殖。沃尔巴克氏体通过卵子的细胞质传播,并进化出不同的机制来操纵宿主的繁殖,包括诱导生殖不相容、孤雌生殖和雌性化。沃尔巴克氏体对生殖和宿主适应性的广泛影响使得沃尔巴克氏体作为一种潜在的生物防治剂日益受到关注。结论:沃尔巴克氏体为设计一种昂贵、有效、环保的药物靶点,有效治疗和消除媒介传播的寄生虫病打开了一扇新的窗口。
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引用次数: 2
Lyme Neuroborreliosis - The Mystifying Pitfall: "Neuropathology and Current Therapeutics". 莱姆病神经螺旋体-神秘的陷阱:“神经病理学和当前的治疗”。
Q3 Medicine Pub Date : 2019-01-01 DOI: 10.2174/1574891X14666190327114641
Vishal Chavda, Snehal Patel

Lyme's Disease (LD) is a severe, rapidly growing, broad spectrum chronic infection caused by the bacterium 'Borrelia (B.) burgdorferi', which can be easily transmitted through the bite of certain species of ticks. The prevalence of LD is swiftly mounting in the present scenario in many countries from species to species. Although Lyme's infection is now detectable via serologic examination of early and late Lyme neuroborreliosis (LNB), the management of persistent symptoms is still fraught with quora of doubt and debate. LD is a multisystem spirochete which results after the dissemination of B. burgdorferi from a dermal inoculation site after a tick bite. Lyme's infection can easily get transmitted to the central nervous system and develop various neurological symptoms due to inflammation and an autoimmune response from body may lead to life-threatening "Lyme Borreliosis". The neurological symptoms are well mixed in presentation, late and confusing to get differentiated easily from other diseases. The use of antibiotics in post Lyme infection with neurological complications is still a topic of debate. Babesiosisstates, and human ehrlichiosis' the two other diseases, are associated with the same ticks that spread the LD. However, the prevalence of diagnosed human cases is usually much lower than that of actual cases of LD due to misdiagnosis, late diagnosis or undiagnosis at y such lateral neuroinfection stage after the tick bite. The current review focuses on the molecular neuropathology and current advancements in LD. There are very few patents or discoveries made on borrelia infection, drawing attention towards more focused and targeted research for the cure.

莱姆病(LD)是一种严重的、迅速发展的广谱慢性感染,由伯氏疏螺旋体(B.)伯氏疏螺旋体引起,它很容易通过某些种类的蜱虫叮咬传播。在目前的情况下,在许多国家,从一个物种到另一个物种,致病菌的发病率正在迅速上升。虽然莱姆病感染现在可以通过早期和晚期莱姆病神经螺旋体病(LNB)的血清学检查检测到,但持续症状的管理仍然充满了疑问和争论。LD是一种多系统螺旋体,由蜱叮咬后皮肤接种部位传播伯氏疏螺旋体引起。莱姆病感染很容易传播到中枢神经系统,并因炎症和身体自身免疫反应而出现各种神经系统症状,可能导致危及生命的“莱姆病”。神经系统症状表现混杂,较晚,易混淆,易与其他疾病鉴别。莱姆病后感染伴神经系统并发症的抗生素使用仍是一个有争议的话题。巴贝斯虫病和人类埃利希体病这两种疾病与传播LD的同一种蜱有关。然而,由于在蜱叮咬后的这种侧神经感染阶段误诊、诊断晚或未诊断,诊断出的人类LD病例的患病率通常远低于实际病例。目前的综述主要集中在分子神经病理学和LD的最新进展。关于伯氏疏螺旋体感染的专利或发现很少,引起人们对更集中和有针对性的治疗研究的关注。
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引用次数: 0
Perspective in Topical Infective and Non-infective Skin Diseases Therapy with Emergence of Nanomedicine. 纳米医学在局部感染性和非感染性皮肤病治疗中的应用前景。
Q3 Medicine Pub Date : 2019-01-01 DOI: 10.2174/1574891x1401191021171205
Mahfoozur Rahman, S. Beg
The current crisis of skin infections caused by a wide range of bacteria, fungi and virus has resulted in an exponential increase in morbidity [1, 2]. Despite the recent advancements in dermatological treatments, the treatment of topical infections has always been a difficult proposition because of the lack of efficacy of existing formulations, longer period of treatment and yet incomplete recovery. Implication of various microbes like Staphylococcus aureus, Methicillin-Resistant Staphylococcus aureus (MRSA), Pseudomonas aeruginosa, Gram-positive, Gram-negative bacteria and fungi is causing complex problems [3]. Moreover, the severity of the problem also depends on the structure of skin layers and the target site. Although, the defensive properties of skin like acidic pH and significant antibacterial activity exhibited by its constituent components like Lauric acid and palmitoleic acid encompass the anti-infective mechanism against topical infections [4], however, in certain conditions like burns, wounds and diabetes mellitus, skin loses its defense mechanism with the entry of pathogens followed by the development of infection. Further, its barrier nature presents an arduous impediment for most drugs to be delivered into and through it owing to the prevailing patho-physiological conditions [5]. Besides, the drug’s intrinsic physico-chemical characteristics viz. pKa, molecular size, stability, binding affinity, solubility and partition coefficient remain unfavorable for drug delivery across the skin barrier [6-8]. Human beings are the natural hosts for many bacterial pathogens that colonize the skin as normal flora. Staphylococcus aureus and Streptococcus pyogenes account for a wide variety of bacterial infections. A wide variety of bacterial infections affect the normal physiology of skin including cellulitis, folliculitis, impetigo, carbuncle and furuncle. The predisposing factors to infection include minor trauma, pre-existing skin disease, poor hygiene, and rarely, impaired host immunity. Cellulitis is a superficial bacterial infection of the lower dermis and upper subcutaneous tissue frequently affecting the legs. The major causative organism of cellulitis is Group A beta-hemolytic Staphylococcus aureus along with other microbes like Pseudomonas aeruginosa, Escherichia coli and Klebsiella species [9]. Impetigo is a superficial cutaneous infection resulting from the direct invasion of healthy tissues, or occurs secondarily to an underlying skin disease especially around nose, mouth and wounds. It occurs in patients already exposed to eczema and diabetes caused mainly by Staphylococcus aureus and Staphylococcus pyogens [10]. Folliculitis is a cutaneous infection of the hair follicles such as the scalp, neck, beard area, axillae, buttocks and limbs characterized by follicular-based pustules. Carbuncles show inflamed skin and pus drainage from hair follicles [10]. The treatment strategies for bacterial skin infections include dicloxacillin, clavu
当前各种细菌、真菌和病毒引起的皮肤感染危机导致发病率呈指数增长[1,2]。尽管最近在皮肤病学治疗方面取得了进展,但由于现有配方缺乏疗效,治疗时间较长且尚未完全恢复,局部感染的治疗一直是一个困难的命题。金黄色葡萄球菌、耐甲氧西林金黄色葡萄球菌(MRSA)、铜绿假单胞菌、革兰氏阳性、革兰氏阴性细菌和真菌等多种微生物的影响正在引起复杂的问题。此外,问题的严重程度还取决于皮肤层的结构和目标部位。虽然皮肤的防御特性,如酸性pH值和其组成成分如月桂酸和棕榈油酸所表现出的显著抗菌活性,包含了抗局部感染的抗感染机制,但在某些情况下,如烧伤、伤口和糖尿病,随着病原体的进入和感染的发展,皮肤失去了防御机制。此外,由于其普遍的病理生理条件,它的屏障性质对大多数药物进入和通过它提出了艰巨的障碍。此外,药物固有的物理化学特性,如pKa、分子大小、稳定性、结合亲和力、溶解度和分配系数,仍然不利于药物通过皮肤屏障传递[6-8]。人类是许多细菌病原体的天然宿主,它们以正常菌群的形式定植在皮肤上。金黄色葡萄球菌和化脓性链球菌是多种细菌感染的病因。各种各样的细菌感染会影响皮肤的正常生理机能,包括蜂窝织炎、毛囊炎、脓疱疮、痈和疖。感染的易感因素包括轻微创伤、先前存在的皮肤病、不卫生,以及很少的宿主免疫力受损。蜂窝织炎是一种浅表细菌感染下真皮和上层皮下组织经常影响腿。蜂窝织炎的主要致病菌是A群溶血性金黄色葡萄球菌,其他微生物如铜绿假单胞菌、大肠杆菌和克雷伯氏菌[9]。脓疱疮是一种浅表皮肤感染,由直接侵入健康组织引起,或继发于潜在的皮肤疾病,特别是在鼻子、嘴和伤口周围。它发生在已经暴露于主要由金黄色葡萄球菌和化脓性葡萄球菌引起的湿疹和糖尿病的患者中。毛囊炎是一种皮肤感染的毛囊,如头皮、颈部、胡须区域、腋窝、臀部和四肢,其特征是基于毛囊的脓疱。红肿表明皮肤发炎和脓液从毛囊流出。细菌性皮肤感染的治疗策略包括双氯西林、克拉维酸、阿莫西林、红霉素、克林霉素和万古霉素。真菌和酵母菌局部感染包括皮肤癣、花斑糠疹和念珠菌病。皮肤癣指由红毛癣引起的感染,对角质化组织如皮肤、头发和指甲有很高的亲和力。另一种常见的皮肤真菌感染是由念珠菌引起的,即白色念珠菌。这些包括念珠菌外阴阴道炎,三门间(皮肤褶感染),餐巾皮炎,慢性甲沟炎(甲褶感染)和甲真菌病(甲板感染)[10]。花斑癣是一种由酵母菌引起的机会性感染。足癣影响脚底的鳞状斑块。头癣的特征是皮肤呈鳞状、红斑并伴有脱发。真菌局部感染的治疗策略包括特比萘芬、克霉唑、益康唑、氟康唑、酮康唑和伊曲康唑[10]。单纯疱疹(HSV)、带状疱疹、传染性软疣、传染性红斑、婴儿玫瑰疹、单纯疱疹和水痘是一些病毒性局部感染。HSV感染是痛苦的,其特征是成组的囊泡伴皮炎。HSV I型与口腔面部疾病有关,HSV II型与生殖器感染有关。传染性软疣通过直接接触传播,由良性痘病毒引起。带状疱疹(带状疱疹)是一种急性、疼痛性皮炎,存在免疫抑制。病毒感染的常见治疗策略包括阿昔洛韦、伐昔洛韦和咪喹莫特。
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引用次数: 0
Meet Our Editorial Board Member 会见我们的编辑委员会成员
Q3 Medicine Pub Date : 2018-12-10 DOI: 10.2174/1574891x1302181106123044
M. Bukrinsky
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引用次数: 0
期刊
Recent patents on anti-infective drug discovery
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