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Journal of Antibiotics

L Ravithej Singh, Srinivasa Rao Avula, Sneha Raj, Akanksha Srivastava, Gopala Reddy Palnati, C K M Tripathi, Mukesh Pasupuleti, Koneni V Sashidhara
Molecular hybridization approach is an emerging tool in drug discovery for designing new pharmacophores with biological activity. A novel, new series of coumarin-benzimidazole hybrids were designed, synthesized and evaluated for their broad spectrum antimicrobial activity. Among all the synthesized molecules, compound (E)-3-(2-1H-benzo[d]imidazol-1-yl)-1-((4-chlorobenzyl)oxy)imino)ethyl)-2H-chromen-2-one showed the most promising broad spectrum antibacterial activity against Pseudomonas aeruginosa, Staphylococcus aureus, Bacillus subtilis and Proteus vulgaris...
June 21, 2017: Journal of Antibiotics
Kosuke Minagawa, Daisuke Urabe, Masayuki Inoue
C19-diterpene alkaloids are a class of alkaloids with pharmacologically important activities having an intricately fused hexacyclic ABCDEF-ring system. Here we report expeditious assembly of the ACE-ring substructure 4a by applying a three-component coupling strategy. A radical-polar crossover reaction between an AE-ring radical precursor, a C-ring radical acceptor and an aldehyde was realized by the actions of Et3B and O2, resulting in the installation of three new stereocenters and extension of the carbon chain corresponding to the B-ring...
June 14, 2017: Journal of Antibiotics
Fabrizio Angius, Enrica Piras, Sabrina Uda, Clelia Madeddu, Roberto Serpe, Rachele Bigi, Wuguo Chen, Dirk P Dittmer, Raffaello Pompei, Angela Ingianni
Kaposi sarcoma herpesvirus (KSHV), also known as human herpesvirus 8, is the causative agent of Kaposi sarcoma; this malignant angiosarcoma is usually treated with conventional antitumor agents that can control disease evolution, but do not clear the latent KSHV episome that binds to cellular DNA. Some commercial antibacterial sulfonamides were tested for the ability to suppress latent KSHV. Quantitative PCR (qPCR) and cytofluorometry assays were used for detecting both viral DNA and the latency factor LANA (latency-associated nuclear antigen) in BC3 cells, respectively...
June 14, 2017: Journal of Antibiotics
Sandra Halecker, Frank Surup, Halvor Solheim, Marc Stadler
No abstract text is available yet for this article.
June 7, 2017: Journal of Antibiotics
Pia Uusitalo, Ulrik Hägglund, Elin Rhöös, Henrik Scherman Norberg, Mikael Elofsson, Charlotta Sundin
Pseudomonas aeruginosa is an opportunistic pathogen that can be very hard to treat because of high resistance to different antibiotics and alternative treatment regimens are greatly needed. An alternative or a complement to traditional antibiotic is to inhibit virulence of the bacteria. The salicylidene acylhydrazide, INP0341, belongs to a class of compounds that has previously been shown to inhibit virulence in a number of Gram-negative bacteria. In this study, the virulence blocking effect of INP0341 on P...
June 7, 2017: Journal of Antibiotics
Fumiaki Tabuchi, Yasuhiko Matsumoto, Masaki Ishii, Keita Tatsuno, Mitsuhiro Okazaki, Tomoaki Sato, Kyoji Moriya, Kazuhisa Sekimizu
Vancomycin is a widely used clinical drug to treat for infection by methicillin-resistant Staphylococcus aureus. Some patients show a weak response to vancomycin treatment. We previously reported that β-lactams increase the susceptibility to vancomycin by vancomycin-highly resistant S. aureus (VRSA) strains obtained following repeated in vitro mutagenesis and vancomycin selection. Here we found that the susceptibility of the VRSA strains to vancomycin was remarkably increased by combined treatment with D-cycloserine...
June 7, 2017: Journal of Antibiotics
Yoshinari Wakiyama, Ko Kumura, Eijiro Umemura, Kazutaka Ueda, Takashi Watanabe, Keiko Yamada, Takafumi Okutomi, Keiichi Ajito
To modify lincomycin (LCM) at the C-6 and the C-7 positions, we firstly prepared various substituted proline intermediates (7, 11-15 and 17). These proline intermediates were coupled with methyl 1-thio-α-lincosamide and tetrakis-O-trimethylsilylation followed by selective deprotection of the TMS group at the 7-position gave a wide variety of key intermediates (23-27, 47 and 50). Then, we synthesized a variety of novel LCM analogs modified at the 7-position in application of the Mitsunobu reaction, an SN2 reaction, and a Pd-catalyzed cross-coupling reaction...
May 31, 2017: Journal of Antibiotics
Konami Takahashi, Kazunari Sakai, Yuriko Nagano, Sakiko Orui Sakaguchi, Andre O Lima, Vivian H Pellizari, Masato Iwatsuki, Kiyotaka Takishita, Kenichi Nonaka, Katsunori Fujikura, Satoshi Ōmura
No abstract text is available yet for this article.
May 31, 2017: Journal of Antibiotics
Xin Qi, Xinwei Wang, Hao Ren, Feng Zhang, Xiumin Zhang, Ning He, Wenqiang Guo, Ruxian Chen, Yunying Xie, Qiyang He
No abstract text is available yet for this article.
May 31, 2017: Journal of Antibiotics
Akihiro Sugawara, Hitomi Maruyama, Sho Shibusawa, Hidehito Matsui, Tomoyasu Hirose, Ayumi Tsutsui, Robrecht Froyman, Carolin Ludwig, Johannes Koebberling, Hideaki Hanaki, Gerd Kleefeld, Satoshi Ōmura, Toshiaki Sunazuka
Tylosin is a 16-membered macrolide broad-spectrum antibiotic that has an important role in veterinary medicine, active against Gram-positive and a restricted range of Gram-negative bacteria. We synthesized 15 types of tylosin-related derivatives by chemical modification and evaluated them against mastitis pathogens. Among them, 20-deoxy-20-{N-methyl-N-[1-(3-quinolyl)-1H-1,2,3-triazol-4-yl]methylamino}-5-O-mycaminosyltylonolide 2f and 20-deoxy-20-{N-benzyl-N-[1-(3-quinolyl)-1H-1,2,3-triazol-4-yl]methylamino}-5-O-mycaminosyltylonolide 2k were found to not only expand their antibacterial impact to include Gram-negative bacteria, such as Escherichia coli and Klebsiella pneumoniae, but also to retain or increase antibacterial activity against Gram-positive bacteria, such as Staphylococcus aureus and Streptococcus uberis in comparison with the parent tylosin...
May 31, 2017: Journal of Antibiotics
Christopher J Lacriola, Shaun P Falk, Bernard Weisblum
No abstract text is available yet for this article.
May 31, 2017: Journal of Antibiotics
Jinjin Zhang, Ke Ma, Hongyu Chen, Kai Wang, Weiping Xiong, Li Bao, Hongwei Liu
No abstract text is available yet for this article.
May 24, 2017: Journal of Antibiotics
Maria Falzone, Emmanuel Crespo, Klarissa Jones, Gulaba Khan, Victoria L Korn, Amreen Patel, Mira Patel, Krishnaben Patel, Carrie Perkins, Sana Siddiqui, Drew Stenger, Eileen Yu, Michael Gelber, Robert Scheffler, Vasyl Nayda, Ariela Ravin, Ronica Komal, Jeffrey D Rudolf, Ben Shen, Vincent Gullo, Arnold L Demain
Streptomyces platensis MA7327 is a bacterium producing interesting antibiotics, which act by the novel mechanism of inhibiting fatty acid biosynthesis. The antibiotics produced by this actinomycete are platensimycin and platencin plus some minor related antibiotics. Platensimycin and platencin have activity against antibiotic-resistant bacteria such as methicillin-resistant Staphylococcus aureus and vancomycin-resistant Enterococcus; they also lack toxicity in animal models. Platensimycin also has activity against diabetes in a mouse model...
May 3, 2017: Journal of Antibiotics
Wei Hong, Jingyang Li, Zhe Chang, Xiaoli Tan, Hao Yang, Yifan Ouyang, Yanhui Yang, Sargit Kaur, Ian C Paterson, Yun Fong Ngeow, Hao Wang
The emergence of drug resistance in bacterial pathogens is a growing clinical problem that poses difficult challenges in patient management. To exacerbate this problem, there is currently a serious lack of antibacterial agents that are designed to target extremely drug-resistant bacterial strains. Here we describe the design, synthesis and antibacterial testing of a series of 40 novel indole core derivatives, which are predicated by molecular modeling to be potential glycosyltransferase inhibitors. Twenty of these derivatives were found to show in vitro inhibition of Gram-positive bacteria, including methicillin-resistant Staphylococcus aureus...
May 3, 2017: Journal of Antibiotics
Ke-Yao He, Cheng Zhang, Yi-Ru Duan, Guo-Lei Huang, Chun-Yan Yang, Xing-Rui Lu, Cai-Juan Zheng, Guang-Ying Chen
Two new chlorinated metabolites 4-chloro-1-hydroxy-3-methoxy-6-methyl-8-methoxycarbonyl-xanthen-9-one (1) and 2'-acetoxy-7-chlorocitreorosein (2), together with three known compounds (3-5), were obtained from the EtOAc extract of the endophytic fungus Penicillium citrinum HL-5126 isolated from the mangrove Bruguiera sexangula var. rhynchopetala collected in the South China Sea. Their structures were elucidated by the detailed analysis of comprehensive spectroscopic data. All compounds were evaluated for their antibacterial and topoisomerase I inhibitory activities...
May 3, 2017: Journal of Antibiotics
Hiroyasu Onaka
Streptomyces have the potential to produce more than 30 secondary metabolites; however, the expression of most metabolite biosynthetic gene clusters is cryptic or silent. Indeed, the expression of these genes is conditional and dependent on culture conditions. To activate such gene clusters, many methods have been developed. In this review, I describe two activation approaches developed in my laboratory: use of the activation mediator goadsporin and combined-culture. Goadsporin is a chemical substance isolated from Streptomyces sp...
April 26, 2017: Journal of Antibiotics
Hossein Naeimi, Asieh Didar, Zahra Rashid, Zohreh Zahraie
In this study, the one-pot four-component reaction of aromatic aldehyde, 2-thiobarbituric acid, ammonium acetate in the presence of a catalytic amount of [H-NMP](+)[HSO4](-) under ultrasonic irradiation in water is reported. In the present procedure, the pyrido[2,3-d:6,5-d']dipyrimidine derivatives were purely produced as valuable products. The process proved to be simple, environmentally friendly, efficient and high to excellent yielding. Moreover, some of the synthetic compounds were investigated and revealed important antimicrobial activity of prepared products...
April 26, 2017: Journal of Antibiotics
Olga F Smetanina, Anton N Yurchenko, Elena V Ivanets, Anatoly I Kalinovsky, Yuliya V Khudyakova, Sergey A Dyshlovoy, Gunhild von Amsberg, Ekaterina A Yurchenko, Shamil Sh Afiyatullov
No abstract text is available yet for this article.
April 26, 2017: Journal of Antibiotics
Lyudmila N Lysenkova, Oleg Y Saveljev, Natalya E Grammatikova, Vladimir B Tsvetkov, Olga B Bekker, Valery N Danilenko, Lyubov G Dezhenkova, Eugene E Bykov, Olga A Omelchuk, Alexander M Korolev, Andrey E Shchekotikhin
Although, the structure of oligomycin A (1) was confirmed by spectroscopic and chemical evaluations, some crystallographic data cast doubt on the originally adopted structure of the side 2-hydroxypropyl moiety of this antibiotic. It was suggested that the side chain of the oligomycin is enol-related (2-hydroxy-1-propenyl). To clarify this matter we synthesized and evaluated 33-dehydrooligomycin A (2) prepared by the Kornblum oxidation of 33-O-mesyloligomycin A (3) by dimethyl sulfoxide. NMR data for 33-dehydrooligomycin (2) and results of quantum chemical calculations have shown that this derivative exists in the keto rather than in the enol tautomer 2a...
April 19, 2017: Journal of Antibiotics
Mei Zhang, Cheng Long Yang, Yong Sheng Xiao, Bo Zhang, Xin Zhao Deng, L I Yang, Jing Shi, Y I Shuang Wang, Wei Li, Rui Hua Jiao, Ren Xiang Tan, Hui Ming Ge
No abstract text is available yet for this article.
April 19, 2017: Journal of Antibiotics
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