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Bioorganic & Medicinal Chemistry Letters

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https://www.readbyqxmd.com/read/28214076/erratum-to-a-triple-exon-skipping-luciferase-reporter-assay-identifies-a-new-clk-inhibitor-pharmacophore-bioorg-med-chem-lett-27-2017-406-412
#1
Yihui Shi, Jaehyeon Park, Chandraiah Lagisetti, Wei Zhou, Lidia C Sambucetti, Thomas R Webb
No abstract text is available yet for this article.
February 14, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28202326/corrigendum-to-dimeric-sesquiterpene-and-thiophenes-from-the-roots-of-echinops-latifolius-bioorg-med-chem-lett-26-2016-5995-5998
#2
Qinghao Jin, Jin Woo Lee, Hari Jang, Ji Eun Choi, Hyung Sik Kim, Dongho Lee, Jin Tae Hong, Mi Kyeong Lee, Bang Yeon Hwang
No abstract text is available yet for this article.
February 12, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28216403/investigation-of-orexin-2-selective-receptor-antagonists-structural-modifications-resulting-in-dual-orexin-receptor-antagonists
#3
Jason W Skudlarek, Christina N DiMarco, Kerim Babaoglu, Anthony J Roecker, Joseph G Bruno, Mark A Pausch, Julie A O'Brien, Tamara D Cabalu, Joanne Stevens, Joseph Brunner, Pamela L Tannenbaum, W Peter Wuelfing, Susan L Garson, Steven V Fox, Alan T Savitz, Charles M Harrell, Anthony L Gotter, Christopher J Winrow, John J Renger, Scott D Kuduk, Paul J Coleman
In an ongoing effort to explore the use of orexin receptor antagonists for the treatment of insomnia, dual orexin receptor antagonists (DORAs) were structurally modified, resulting in compounds selective for the OX2R subtype and culminating in the discovery of 23, a highly potent, OX2R-selective molecule that exhibited a promising in vivo profile. Further structural modification led to an unexpected restoration of OX1R antagonism. Herein, these changes are discussed and a rationale for selectivity based on computational modeling is proposed...
February 9, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28209465/identification-of-highly-potent-and-selective-pi3k%C3%AE-inhibitors
#4
David Marcoux, Lan-Ying Qin, Zheming Ruan, Qing Shi, Qian Ruan, Carolyn Weigelt, Hongchen Qiu, Gary Schieven, John Hynes, Rajeev Bhide, Michael Poss, Joseph Tino
Selective PI3Kδ inhibitors have recently been hypothesized to be appropriate immunosuppressive agents for the treatment of immunological disorders such as rheumatoid arthritis. However, few reports have highlighted molecules that are highly selective for PI3Kδ over the other PI3K isoforms. In this letter, isoform and kinome selective PI3Kδ inhibitors are presented. The Structural Activity Relationship leading to such molecules is outlined.
February 7, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28216401/discovery-and-characterization-of-novel-indole-and-7-azaindole-derivatives-as-inhibitors-of-%C3%AE-amyloid-42-aggregation-for-the-treatment-of-alzheimer-s-disease
#5
Nampally Sreenivasachary, Heiko Kroth, Pascal Benderitter, Anne Hamel, Yvan Varisco, David T Hickman, Wolfgang Froestl, Andrea Pfeifer, Andreas Muhs
The aggregation of amyloid-β peptides into cytotoxic oligomeric and fibrillary aggregates is believed to be one of the major pathological events in Alzheimer disease. Here we report the design and synthesis of a novel series of indole and 7-azaindole derivatives containing, nitrile, piperidine and N-methyl-piperidine substituents at the 3-position to prevent the pathological self-assembly of amyloid-β. We have further demonstrated that substitution of the azaindole and indole derivatives at the 3 positions is required to obtain compounds with improved physicochemical properties to allow brain penetration...
February 4, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28216045/discovery-of-2-oxopiperazine-dengue-inhibitors-by-scaffold-morphing-of-a-phenotypic-high-throughput-screening-hit
#6
Cyrille S Kounde, Hui-Quan Yeo, Qing-Yin Wang, Kah Fei Wan, Hongping Dong, Ratna Karuna, Ina Dix, Trixie Wagner, Bin Zou, Oliver Simon, Ghislain M C Bonamy, Bryan K S Yeung, Fumiaki Yokokawa
A series of 2-oxopiperazine derivatives were designed from the pyrrolopiperazinone cell-based screening hit 4 as a dengue virus inhibitor. Systematic investigation of the structure-activity relationship (SAR) around the piperazinone ring led to the identification of compound (S)-29, which exhibited potent anti-dengue activity in the cell-based assay across all four dengue serotypes with EC50<0.1μM. Cross-resistant analysis confirmed that the virus NS4B protein remained the target of the new oxopiperazine analogs obtained via scaffold morphing from the HTS hit 4...
February 4, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28202327/synthesis-and-evaluation-of-anticonvulsant-properties-of-new-n-mannich-bases-derived-from-pyrrolidine-2-5-dione-and-its-3-methyl-3-isopropyl-and-3-benzhydryl-analogs
#7
Sabina Rybka, Jolanta Obniska, Anna Rapacz, Barbara Filipek, Paweł Żmudzki
The aim of this paper was to describe the synthesis of a library of 28 new 1,3-substituted pyrrolidine-2,5-dione as potential anticonvulsant agents. The anticonvulsant activity was evaluated using three acute models of seizures in mice (MES-maximal electroshock, scPTZ-subcutaneous pentylenetetrazole, and 6Hz-psychomotor seizure tests). The neurotoxicity was determined by rotarod test. The most promising compound was found to be N-[{morpholin-1-yl}-methyl]-3-benzhydryl-pyrrolidine-2,5-dione (15), as it was active in the MES (ED50=41...
February 4, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28202325/synthesis-and-biological-evaluation-of-heterocyclic-analogues-of-pregnenolone-as-novel-anti-osteoporotic-agents
#8
Saransh Wales Maurya, Kapil Dev, Krishna Bhan Singh, Reena Rai, Ibadur Rahman Siddiqui, Divya Singh, Rakesh Maurya
The structural modifications of pregnenolone have been described via the introduction of heterocyclic moieties at C-17 position by limiting the acyl group. Novel heterocyclic analogues of pregnenolone have been synthesized by using Friedlander and Claisen-Schmidt reactions, and the synthesized compounds were evaluated for their osteogenic activity. Among the synthesized derivatives, four compounds showed significantly increased ALP activity. Among all four active compounds, the novel compound 3a has shown significant bone matrix mineralization and mRNA expressions of osteogenic marker genes, BMP2, RUNX-2 and OCN at 1pM concentration...
February 4, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28169160/corrigendum-to-discovery-of-benzofuran-propanoic-acid-gpr120-agonists-from-uhts-hit-to-mechanism-based-pharmacodynamic-effects-bioorg-med-chem-lett-26-2016-5724-5728
#9
Matthew Lombardo, Kate Bender, Clare London, Michael A Plotkin, Melissa Kirkland, Joel Mane, Michele Pachanski, Wayne Geissler, John Cummings, Bahanu Habulihaz, Taro E Akiyama, Jerry Di Salvo, Maria Madeira, Joanna Pols, Mary Ann Powles, Michael F Finley, Eric Johnson, Thomas Roussel, Victor N Uebele, Alejandro Crespo, Dennis Leung, Candice Alleyne, Dorina Trusca, Ying Lei, Andrew D Howard, Feroze Ujjainwalla, James R Tata, Christopher J Sinz
No abstract text is available yet for this article.
February 4, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28209374/design-synthesis-and-evaluation-of-novel-pyrazolo-pyrimido-4-5-d-pyrimidine-derivatives-as-potent-antibacterial-and-biofilm-inhibitors
#10
Lingala Suresh, P Sagar Vijay Kumar, Y Poornachandra, C Ganesh Kumar, G V P Chandramouli
An efficient four-component reaction of 6-amino-1,3-dimethyluracil, N,N-dimethylformamide dimethylacetal, 1-phenyl-3-(4-substituted-phenyl)-4-formyl-1H-pyrazoles and aromatic amines was conducted in the presence of [Bmim]FeCl4 ionic liquid as a promoting medium. This strategy provided a convenient route without any additional catalyst or metal salt under mild conditions. All the synthesized pyrazolo-pyrimido[4,5-d]pyrimidines derivatives were evaluated for their antibacterial, minimum bactericidal concentration (MBC), biofilm inhibition, intracellular ROS accumulation and protein leakage activities...
February 3, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28196701/filamenting-temperature-sensitive-mutant-z-inhibitors-from-glycyrrhiza-glabra-and-their-inhibitory-mode-of-action
#11
Takashi Matsui, Subehan Lallo, Khoirun Nisa, Hiroyuki Morita
FtsZ is an essential protein for bacterial cell division, and an attractive and underexploited novel antibacterial target protein. Screening of Indonesian plants revealed the inhibitory activity of the methanol extract of Glycyrrhiza glabra on the Bacillus subtilis FtsZ (BsFtsZ) GTPase, and further bioassay-guided fractionation of the active methanol extract led to the isolation of seven known polyketides (1-7). Among them, gancaonin I (1), glycyrin (3), and isolicoflavanol (5) exhibited anti-BsFtsZ GTPase activities, at levels comparable to that of the synthetic FtsZ inhibitor, Zantrin Z3...
February 3, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28189421/synthesis-molecular-docking-and-%C3%AE-glucosidase-inhibition-of-2-5-6-diphenyl-1-2-4-triazin-3-yl-thio-n-arylacetamides
#12
Guangcheng Wang, Xin Li, Jing Wang, Zhenzhen Xie, Luyao Li, Ming Chen, Shan Chen, Yaping Peng
A novel series of 2-((5,6-diphenyl-1,2,4-triazin-3-yl)thio)-N-arylacetamides 5a-5q have been synthesized and evaluated for their α-glucosidase inhibitory activity. All newly synthesized compounds exhibited potent α-glucosidase inhibitory activity in the range of IC50=12.46±0.13-72.68±0.20μM, when compared to the standard drug acarbose (IC50=817.38±6.27μM). Among the series, compound 5j (12.46±0.13μM) with strong electron-withdrawing nitro group on the arylacetamide moiety was identified as the most potent inhibitor of α-glucosidase...
February 2, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28216405/design-synthesis-and-biological-evaluation-of-nonsecosteroidal-vitamin-d3-receptor-ligands-as-anti-tumor-agents
#13
Bin Wang, Meixi Hao, Can Zhang
1α,25-dihydroxyvitamin D3 (1,25-(OH)2D3, also known as calcitriol), the active form of vitamin D3, is being increasingly recognized for cancer therapy. Our previous work showed that phenyl-pyrrolyl pentane analogs, which mimicked anti-proliferative activities against several cancer cell lines of the natural secosteroidal ligand 1,25-(OH)2D3. Here, in order to optimize the structural features and discover more potent derivative, a series of nonsecosteroidal vitamin D3 receptor (VDR) ligands bearing acetylene bond linker was designed, synthesized and evaluated...
February 1, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28216402/synthesis-of-novel-spiro-pyrazolo-4-3-d-pyrimidinones-and-spiro-benzo-4-5-thieno-2-3-d-pyrimidine-2-3-indoline-2-4-3h-diones-and-their-evaluation-for-anticancer-activity
#14
Ismail, Bhaskar Kuthati, Gangadhar Thalari, Venkatesham Bommarapu, Chaitanya Mulakayala, Suresh Kumar Chitta, Naveen Mulakayala
An efficient and novel method for the preparation of spiro[pyrazolo[4,3-d]pyrimidin]-7'(1'H)-ones by the condensation of 4-amino-1-methyl-3-propylpyrazole-5-carboxamide with ketones under mild conditions using catalytic InCl3 was reported. This method has been extended for the synthesis of novel spiro[benzo[4,5]thieno[2,3-d]pyrimidine-2,3'-indoline]-2',4(3H)-dione which are having potential applications in medicinal chemistry. All the synthesized compounds were evaluated for their anti-proliferative properties in vitro against cancer cell lines and several compounds were found to be active...
February 1, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28216044/radiolabeling-and-initial-biological-evaluation-of-18-f-kbm-1-for-imaging-rar-%C3%AE-receptors-in-neuroblastoma
#15
Kiran Kumar Solingapuram Sai, Bhaskar C Das, Anirudh Sattiraju, Frankis G Almaguel, Suzanne Craft, Akiva Mintz
Retinoic acid receptor alpha (RAR-α) plays a significant role in a number of diseases, including neuroblastoma. Children diagnosed with high-risk neuroblastoma are treated13-cis-retinoic acid, which reduces risk of cancer recurrence. Neuroblastoma cell death is mediated via RAR-α, and expression of RAR-α is upregulated after treatment. A molecular imaging probe that binds RAR-α will help clinicians to diagnose and stratify risk for patients with neuroblastoma, who could benefit from retinoid-based therapy...
February 1, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28214077/new-homoisoflavonoid-analogues-protect-cells-by-regulating-autophagy
#16
Li-She Gan, Lin-Wei Zeng, Xiang-Rong Li, Chang-Xin Zhou, Jie Li
As a special group of naturally occurring flavonoids, homoisoflavonoids have been discovered as active components of several traditional Chinese medicines for nourishing heart and mind. In this study, twenty homoisoflavonoid analogues, including different substitution groups on rings A and B, as well as heteroaromatic B ring, were synthesized and evaluated for their cardioprotective and neuroprotective activities. In a H2O2-induced H9c2 cardiomyocytes injury assay, nine homoisoflavonoid analogues showed promising activities in the same level as the positive control, diazoxide...
February 1, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28190633/novel-5-arylthio-5h-chromenopyridines-as-a-new-class-of-anti-fibrotic-agents
#17
Renukadevi Patil, Anandita Ghosh, Phoebus Sun Cao, Roger D Sommer, Kyle A Grice, Gulam Waris, Shivaputra Patil
Liver fibrosis is a critical wound healing response to chronic liver injury such as hepatitis C virus (HCV) infection. If persistent, liver fibrosis can lead to cirrhosis and hepatocellular carcinoma (HCC). The development of new therapies for preventing liver fibrosis and its progression to cancer associated with HCV infection remains a critical challenge. Identification of novel anti-fibrotic compounds will provide opportunities for innovative therapeutic intervention of HCV-mediated liver fibrosis. We designed and synthesized a focused set of 5-arylthio-5H-chromenopyridines as a new class of anti-fibrotic agents...
February 1, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28189422/synthesis-and-antimicrobial-evaluation-of-cationic-low-molecular-weight-amphipathic-1-2-3-triazoles
#18
Thomas A Bakka, Morten B Strøm, Jeanette H Andersen, Odd R Gautun
A library of 28 small cationic 1,4-substituted 1,2,3-triazoles was prepared for studies of antimicrobial activity. The structures addressed the pharmacophore model of small antimicrobial peptides and an amphipathic motif found in marine antimicrobials. Eight compounds showed promising antimicrobial activity, of which the most potent compound 10b displayed minimum inhibitory concentrations of 4-8μg/mL against Streptococcus agalacticae, Staphylococcus aureus, Pseudomonas aeruginosa, Escherichia coli, and Enterococcus faecalis...
February 1, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28185720/discovery-of-phenyl-acetamides-as-potent-and-selective-gpr119-agonists
#19
Cheng Zhu, Liping Wang, Yuping Zhu, Zack Zhiqiang Guo, Ping Liu, Zhiyong Hu, Jason W Szewczyk, Ling Kang, Gary Chicchi, Anka Ehrhardt, Andrea Woods, Toru Seo, Morgan Woods, Margaret van Heek, Karen H Dingley, Jianmei Pang, Gino M Salituro, Joyce Powell, Jenna L Terebetski, Viktor Hornak, Louis-Charles Campeau, Robert K Orr, Feroze Ujjainwalla, Michael Miller, Andrew Stamford, Harold B Wood, Timothy Kowalski, Ravi P Nargund, Scott D Edmondson
The paper describes the SAR/SPR studies that led to the discovery of phenoxy cyclopropyl phenyl acetamide derivatives as potent and selective GPR119 agonists. Based on a cis cyclopropane scaffold discovered previously, phenyl acetamides such as compound 17 were found to have excellent GPR119 potency and improved physicochemical properties. Pharmacokinetic data of compound 17 in rat, dog and rhesus will be described. Compound 17 was suitable for QD dosing based on its predicted human half-life, and its projected human dose was much lower than that of the recently reported structurally-related benzyloxy compound 2...
February 1, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28214075/asymmetric-total-synthesis-of-tetrahydroprotoberberine-derivatives-and-evaluation-of-their-binding-affinities-at-dopamine-receptors
#20
David Y W Lee, Jing Liu, Shuzhen Zhang, Peng Huang, Lee-Yuan Liu-Chen
Cocaine addiction remains a serious challenge for clinical and medical research because there is no effective pharmacological treatment. l-THP, a natural product isolated from Corydalis yanhusuo W.T. Wang, is one of the most frequently used traditional herbs to treat drug addiction in China. Our laboratory first reported that its demethylated metabolites l-ICP, l-CD, and l-CP had high affinity at dopamine D1, D2, and D5 receptors. Here we report the chemical synthesis of these metabolites and other derivatives and their binding affinities at dopamine receptors...
January 31, 2017: Bioorganic & Medicinal Chemistry Letters
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