abstract：:Despite the growing global crisis caused by antimicrobial drug resistance among pathogenic bacteria, the number of new antibiotics, especially new chemical class of antibiotics under development is insufficient to tackle the problem. Our review focuses on an emerging class of antibacterial therapeutic agents that hold...

journal_title：Bioorganic & medicinal chemistry

authors： Xu WC,Silverman MH,Yu XY,Wright G,Brown N

更新日期：2019-08-01 00:00:00

abstract：:Bexarotene (1), a retinoid X receptor (RXR) agonist approved for the treatment of cutaneous T cell lymphoma (CTCL), was reported to migrate into baboon brain based on findings obtained by positron emission tomography (PET) with a 11C-labeled tracer. However, co-administration of non-radioactive 1 had no effect on the ...

journal_title：Bioorganic & medicinal chemistry

authors： Takamura Y,Shibahara O,Watanabe M,Fujihara M,Yamada S,Akehi M,Sasaki T,Hirano H,Kakuta H

更新日期：2019-07-15 00:00:00

abstract：:Betulinic acid (BA), a pentacyclic triterpenoid, exhibits broad spectrum antiproliferative activity, but generally with only modest potency. To improve BA's pharmacological properties, fluorine was introduced as a single atom at C-2, creating two diastereomers, or in a trifluoromethyl group at C-3. We evaluated the im...

journal_title：Bioorganic & medicinal chemistry

authors： Li J,Chang LC,Hsieh KY,Hsu PL,Capuzzi SJ,Zhang YC,Li KP,Morris-Natschke SL,Goto M,Lee KH

更新日期：2019-07-01 00:00:00

abstract：:Novel 4-oxobenzo[d]1,2,3-triazin derivatives bearing pyridinium moiety 6a-q were synthesized and screened against acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE). Most of the synthesized compounds showed good inhibitory activity against AChE. Among the synthesized compounds, the compound 6j exhibited the...

journal_title：Bioorganic & medicinal chemistry

authors： Hosseini F,Ramazani A,Mohammadi-Khanaposhtani M,Barazandeh Tehrani M,Nadri H,Larijani B,Mahdavi M

更新日期：2019-07-01 00:00:00

abstract：:7,8-Dihydroxy-3-methyl-isochromanone-4 (XJP), is a polyphenolic natural product with moderate antihypertensive activity. To obtain new agents with stronger potency and safer profile, we employed XJP and naftopidil as the lead compounds to design and synthesize a novel class of hybrids as antihypertensive agent candida...

journal_title：Bioorganic & medicinal chemistry

authors： Xie S,Li X,Yu H,Zhang P,Wang J,Wang C,Xu S,Wu Z,Liu J,Zhu Z,Xu J

更新日期：2019-07-01 00:00:00

abstract：:A synthetic flavone derivative 2-(benzo[d][1,3]dioxol-5-yl)-4H-chromen-4-one (BDC) was synthesized by the one pot reaction method and assessed for α-glucosidase inhibitory activity. The BDC demonstrated dose dependent inhibition of α-glucosidase activity. A maximum inhibition (99.3 ± 0.26%) of α-glucosidase was observ...

journal_title：Bioorganic & medicinal chemistry

authors： Meena SN,Kumar U,Naik MM,Ghadi SC,Tilve SG

更新日期：2019-06-15 00:00:00

abstract：:Our previous study has revealed 4-(4-(4-chlorophenyl)-1,4-diazepan-1-yl)-1-(4-fluorophenyl)butan-1-one·2HCl (SYA013) 1 as a sigma ligand with moderate selectivity for the sigma-2 receptor. Given the overexpression of sigma receptors in solid tumors and reports of sigma ligands with anticancer activities, we selected 1...

journal_title：Bioorganic & medicinal chemistry

authors： Asong G,Zhu XY,Bricker B,Andey T,Amissah F,Lamango N,Ablordeppey SY

更新日期：2019-06-15 00:00:00

abstract：:The biochemistry of all living organisms uses complex, enzyme-catalyzed metabolic reaction networks. Yet, at life's origins, enzymes had not yet evolved. Therefore, it has been postulated that non-enzymatic metabolic pathways predated their enzymatic counterparts. In this account article, we describe our recent work t...

journal_title：Bioorganic & medicinal chemistry

authors： Muchowska KB,Chevallot-Beroux E,Moran J

更新日期：2019-06-15 00:00:00

abstract：:Autophagy ensures cellular homeostasis by the degradation of long-lived proteins, damaged organelles and pathogens. This catabolic process provides essential cellular building blocks upon nutrient deprivation. Cellular metabolism, especially mitochondrial respiration, has a significant influence on autophagic flux, an...

journal_title：Bioorganic & medicinal chemistry

authors： Kaiser N,Corkery D,Wu Y,Laraia L,Waldmann H

更新日期：2019-06-15 00:00:00

abstract：:In this paper, we report the synthesis of a new series of α-aminophosphonates derivatives based in an efficient three-component reaction. All compounds prepared showed significant anti-inflammatory activity, being the compounds 1a, 1c, 1d, 1f, 2b and 2c the most promising ones, in terms of maximal efficacy (over 95%),...

journal_title：Bioorganic & medicinal chemistry

authors： Romero-Estudillo I,Viveros-Ceballos JL,Cazares-Carreño O,González-Morales A,de Jesús BF,López-Castillo M,Razo-Hernández RS,Castañeda-Corral G,Ordóñez M

更新日期：2019-06-15 00:00:00

abstract：:A small library of spirooxindole-pyrrolidine hybrids have been synthesized for the first time in an ionic liquid, [bmim]Br in good to excellent yields employing a new class of non-stabilized azomethine ylides derived from isatin and tyrosine, a combination that has been rarely employed for the in situ generation of az...

journal_title：Bioorganic & medicinal chemistry

authors： Kumar RS,Almansour AI,Arumugam N,Mohammad F,Kotresha D,Menéndez JC

更新日期：2019-06-15 00:00:00

abstract：:Antagonizing transcriptional activity of farnesoid X receptor (FXR) in the intestine has been reported as an effective means for the treatment of nonalcoholic fatty liver disease, type 2 diabetes and obesity. We describe herein that the building blocks necessary to maintain the antagonism of our chemotype were investi...

journal_title：Bioorganic & medicinal chemistry

authors： Teno N,Yamashita Y,Masuda A,Iguchi Y,Oda K,Fujimori K,Hiramoto T,Nishimaki-Mogami T,Une M,Gohda K

更新日期：2019-06-01 00:00:00

abstract：:We have developed a platform for activatable fluorescent substrates of glucose transporters (GLUTs). We firstly conjugated fluorescein to glucosamine via an amide or methylene linker at the C-2 position of d-glucosamine, but the resulting compounds, FLG1 and FLG2, showed no uptake into MIN6 cells. So, we changed the f...

journal_title：Bioorganic & medicinal chemistry

authors： Takasugi T,Hanaoka K,Sasaki A,Ikeno T,Komatsu T,Ueno T,Yamada K,Urano Y

更新日期：2019-05-15 00:00:00

abstract：:Sigma-1 receptor imaging probes for determining the expression levels are desirable for diagnoses of various diseases and companion diagnoses of therapeutic agents targeting the sigma-1 receptor. In this study, we aimed to develop probes with higher affinity for the sigma-1 receptor. For this purpose, we synthesized a...

journal_title：Bioorganic & medicinal chemistry

authors： Ogawa K,Masuda R,Mishiro K,Wang M,Kozaka T,Shiba K,Kinuya S,Odani A

更新日期：2019-05-15 00:00:00

abstract：:Antibiotic resistance remains a major global public health threat that requires sustained discovery of novel antibacterial agents with unexploited scaffolds. Structure-activity relationship of the first-generation aryl isonitrile compounds we synthesized led to an initial lead molecule that informed the synthesis of a...

journal_title：Bioorganic & medicinal chemistry

authors： Kyei-Baffour K,Mohammad H,Seleem MN,Dai M

更新日期：2019-05-01 00:00:00

abstract：:Synthetic derivatives of cyclic adenosine monophosphate, such as halogenated or other more hydrophobic analogs, are widely used compounds, to investigate diverse signal transduction pathways of eukaryotic cells. This inspired us to develop cyclic nucleotides, which exhibit chemical structures composed of brominated 7-...

journal_title：Bioorganic & medicinal chemistry

authors： Lelle M,Otte M,Thon S,Bertinetti D,Herberg FW,Benndorf K

更新日期：2019-04-15 00:00:00

abstract：:G-quadruplexes (G4s) are non-B DNA structures present in guanine-rich regions of gene regulatory areas, promoters and CpG islands, but their occurrence and functions remain incompletely understood. Thus, methodology to identify G4 sequences is needed. Here, we describe the synthesis of a novel cyclic hepta-oxazole com...

journal_title：Bioorganic & medicinal chemistry

authors： Iida K,Tsushima Y,Ma Y,Sedghi Masoud S,Sakuma M,Yokoyama T,Yoshida W,Ikebukuro K,Nagasawa K

更新日期：2019-04-15 00:00:00

abstract：:We efficiently synthesized 2'-O,4'-C-aminomethylene-bridged nucleic acid (2',4'-BNANC) monomers bearing the four nucleobases, guanine, adenine, thymine, and 5-methylcytosine and incorporated these monomers into oligonucleotides. Initially, we carried out the transglycosylation reaction on several 2'-O-substituted 5-me...

journal_title：Bioorganic & medicinal chemistry

authors： Fujisaka A,Hari Y,Takuma H,Rahman SMA,Yoshikawa H,Pang J,Imanishi T,Obika S

更新日期：2019-04-15 00:00:00

abstract：:Hypoxia is a common characteristic of many types of solid tumors and is associated with tumor propagation, malignant progression, and resistance to anti-cancer therapy. HIF-1 pathway is one of the survival pathways activated in tumor in response to hypoxia. In hypoxic condition, hypoxia-inducible factor-1α (HIF-1α) is...

journal_title：Bioorganic & medicinal chemistry

authors： Li J,Xi W,Li X,Sun H,Li Y

更新日期：2019-04-01 00:00:00

abstract：:Filamenting temperature-sensitive mutant Z (FtsZ) is recognized as a promising target for new antibiotics development because of its high conservatism and pivotal role in the bacteria cell division. The aromatic heterocyclic scaffold of indole is known showing merit medical functions in antiviral and antimicrobial. In...

journal_title：Bioorganic & medicinal chemistry

authors： Cai S,Yuan W,Li Y,Huang X,Guo Q,Tang Z,Fang Z,Lin H,Wong WL,Wong KY,Lu YJ,Sun N

更新日期：2019-04-01 00:00:00

abstract：:Selective proteinase inhibitors have demonstrated utility in the investigation of cartilage degeneration mechanisms and may have clinical use in the management of osteoarthritis. The cysteine protease cathepsin K (CatK) is an attractive target for arthritis therapy. Here we report the synthesis of two cathepsin K inhi...

journal_title：Bioorganic & medicinal chemistry

authors： Yuan XY,Ren Z,Wu Y,Bougault C,Brizuela L,Magne D,Buchet R,Mebarek S

更新日期：2019-03-15 00:00:00

abstract：:Leucyl-tRNA synthetase (LRS) plays an important role in amino acid-dependent mTORC1 signaling, which is known to be associated with cellular metabolism and proliferation. Therefore, LRS-targeting small molecules that can suppress mTORC1 activation may provide an alternative strategy to current anticancer therapy. In t...

journal_title：Bioorganic & medicinal chemistry

authors： Yoon S,Kim SE,Kim JH,Yoon I,Tran PT,Ann J,Kim C,Byun WS,Lee S,Kim S,Lee J,Lee J

更新日期：2019-03-15 00:00:00

abstract：:The dysfunction and mutual compensatory activation of RAF-MEK-ERK and PI3K-PDK1-AKT pathways have been demonstrated as the hallmarks in several primary and recurrent cancers. The strategy of concurrent blocking of these two pathways shows clinical merits on effective cancer therapy, such as combinatory treatments and ...

journal_title：Bioorganic & medicinal chemistry

authors： Yu Z,Chen Z,Su Q,Ye S,Yuan H,Kuai M,Lv M,Tu Z,Yang X,Liu R,Hu G,Li Q

更新日期：2019-03-15 00:00:00

abstract：:Molecules designed for cell-specific imaging were studied, taking advantage of an enzyme-inhibitor interaction. 1-Deoxynojirimycin (DNJ) can be actively captured by cells which express the surface membrane protein α-glucosidase. New probes composed of DNJ for recognition linked to a fluorophore signal portion were pre...

journal_title：Bioorganic & medicinal chemistry

authors： Hatano A,Kanno Y,Kondo Y,Sunaga Y,Umezawa H,Fukui K

更新日期：2019-03-01 00:00:00

abstract：:Acute myeloid leukemia (AML) is characterized by fast progression and low survival rates, in which Fms-like tyrosine kinase 3 (FLT3) receptor mutations have been identified as a driver mutation in cancer progression in a subgroup of AML patients. Clinical trials have shown emergence of drug resistant mutants, emphasiz...

journal_title：Bioorganic & medicinal chemistry

authors： Grimm SH,Gagestein B,Keijzer JF,Liu N,Wijdeven RH,Lenselink EB,Tuin AW,van den Nieuwendijk AMCH,van Westen GJP,van Boeckel CAA,Overkleeft HS,Neefjes J,van der Stelt M

更新日期：2019-03-01 00:00:00

abstract：:New compounds able to counteract staphylococcal biofilm formation are needed. In this study we investigate the mechanism of action of pyrrolomycins, whose potential as antimicrobial agents has been demonstrated. We performed a new efficient and easy method to use microwave organic synthesis suitable for obtaining pyrr...

journal_title：Bioorganic & medicinal chemistry

authors： Raimondi MV,Listro R,Cusimano MG,La Franca M,Faddetta T,Gallo G,Schillaci D,Collina S,Leonchiks A,Barone G

更新日期：2019-03-01 00:00:00

abstract：:A novel series of acetamide-substituted derivatives and two prodrugs of doravirine were designed and synthesized as potent HIV-1 NNRTIs by employing the structure-based drug design strategy. In MT-4 cell-based assays using the MTT method, it was found that most of the new compounds exhibited moderate to excellent inhi...

journal_title：Bioorganic & medicinal chemistry

authors： Wang Z,Yu Z,Kang D,Zhang J,Tian Y,Daelemans D,De Clercq E,Pannecouque C,Zhan P,Liu X

更新日期：2019-02-01 00:00:00

abstract：:A series of novel metronidazole aryloxy, carboxy and azole derivatives has been synthesized and their cytotoxic activities on three cancer cell lines were evaluated by MTT assay. Compounds 4m, 4l and 4d showed the most potent cytotoxic activity (IC50s less than 100 µg/mL). Apoptosis was also detected for these compoun...

journal_title：Bioorganic & medicinal chemistry

authors： Faghih-Mirzaei E,Sabouri S,Zeidabadinejad L,AbdolahRamazani S,Abaszadeh M,Khodadadi A,Shamsadinipour M,Jafari M,Pirhadi S

更新日期：2019-01-15 00:00:00

abstract：:Competitive antagonists (CAs) of ionotropic GABA receptors (GABARs) reportedly exhibit insecticidal activity and have potential for development as novel insecticides for overcoming emerging resistance to traditional GABAR-targeting insecticides. Our previous studies demonstrated that 4,5-disubstituted 3-isoxazolols or...

journal_title：Bioorganic & medicinal chemistry

authors： Liu G,Li H,Shi J,Wang W,Furuta K,Liu D,Zhao C,Ozoe F,Ju X,Ozoe Y

更新日期：2019-01-15 00:00:00

abstract：:A series of ferrocene appended chalcone allied triazole coupled organosilatranes (FCTSa 7-FCTSa 12) were synthesised with the aim of amalgamating the pharmacological action of the constituting moieties into a single molecular scaffold. All the synthesised silatranes were well characterized by various spectroscopic tec...

journal_title：Bioorganic & medicinal chemistry

authors： Singh G,Arora A,Kalra P,Maurya IK,Ruizc CE,Estebanc MA,Sinha S,Goyal K,Sehgal R

更新日期：2019-01-01 00:00:00

abstract：:Heroin is a highly abused opioid that has reached epidemic status within the United States. Yet, existing therapies to treat addiction are inadequate and frequently result into rates of high recidivism. Vaccination against heroin offers a promising alternative therapeutic option but requires further development to enh...

journal_title：Bioorganic & medicinal chemistry

authors： Hwang CS,Ellis B,Zhou B,Janda KD

更新日期：2019-01-01 00:00:00

abstract：:Design and synthesis of LuxS enzyme inhibitors otherwise known as S-ribosylhomocysteine analogues, to target quorum sensing in bacteria, has been considerably developed within the last decade. This review presents which molecules have been synthesized to target LuxS enzyme in other words inhibitors of S-ribosylhomocys...

journal_title：Bioorganic & medicinal chemistry

authors： Mina G,Chbib C

更新日期：2019-01-01 00:00:00

abstract：:BMS-986120 is a PAR4 antagonist that is being investigated as an antiplatelet agent in phase I clinical trial. An improved synthesis of BMS-986120 has been developed. Based on the novel synthetic approach to BMS-986120, a series of deuterated derivatives of BMS-986120 have been synthesized and biologically evaluated t...

journal_title：Bioorganic & medicinal chemistry

authors： Chen P,Ren S,Song H,Chen C,Chen F,Xu Q,Kong Y,Sun H

更新日期：2019-01-01 00:00:00

abstract：:The scorpion toxin AmmTx3 is a specific blocker of Kv4 channels. It was shown to have interesting potential for neurological disorders. In this study, we report the first chemical synthesis of AmmTx3 by using the native chemical ligation strategy and validate its biological activity. We determined its 3D structure by ...

journal_title：Bioorganic & medicinal chemistry

authors： Zoukimian C,Meudal H,De Waard S,Ouares KA,Nicolas S,Canepari M,Béroud R,Landon C,De Waard M,Boturyn D

更新日期：2019-01-01 00:00:00

abstract：:Dimeric cynnamoyl analogues (DCAs) with depigmenting activity have been developed. In this study, a role of diamide linkage chain length of DCAs as a tyrosinase inhibitor was investigated on tyrosinase inhibitory activity, antioxidative activity, hydrophobicity and anti-melanogenesis as well as structural characterist...

journal_title：Bioorganic & medicinal chemistry

authors： Ha JH,Park SN

更新日期：2018-12-15 00:00:00

abstract：:The function of acid ceramidase (ACDase), whose congenital deficiency leads to Farber disease, has been recognized to be vital to tumor cell biology, and inhibition of its activity may be beneficial in cancer therapy. Therefore, manipulation of the activity of this enzyme may have significant effect, especially on can...

journal_title：Bioorganic & medicinal chemistry

authors： Bai A,Bielawska A,Rahmaniyan M,Kraveka JM,Bielawski J,Hannun YA

更新日期：2018-12-15 00:00:00

abstract：:Synthetic derivatives of 1,4-benzoxazin-3-ones have been shown to possess promising antimicrobial activity, whereas their natural counterparts were found lacking in this respect. In this work, quantitative structure-activity relationships (QSAR) of natural and synthetic 1,4-benzoxazin-3-ones as antimicrobials were est...

journal_title：Bioorganic & medicinal chemistry

authors： de Bruijn WJC,Hageman JA,Araya-Cloutier C,Gruppen H,Vincken JP

更新日期：2018-12-15 00:00:00

abstract：:AKR1C3 is a promising therapeutic target for castration-resistant prostate cancer. Herein, an evaluation of in-house library discovered substituted pyranopyrazole as a novel scaffold for AKR1C3 inhibitors. Preliminary SAR exploration identified its derivative 19d as the most promising compound with an IC50 of 0.160 μM...

journal_title：Bioorganic & medicinal chemistry

authors： Zheng X,Jiang Z,Li X,Zhang C,Li Z,Wu Y,Wang X,Zhang C,Luo HB,Xu J,Wu D

更新日期：2018-12-01 00:00:00

abstract：:The multi-step ligand action to a target protein is an important aspect when understanding mechanisms of ligand binding and discovering new drugs. However, structurally capturing such complex mechanisms is challenging. This is particularly true for interactions between large membrane proteins and small molecules. One ...

journal_title：Bioorganic & medicinal chemistry

authors： Niitsu A,Egawa A,Ikeda K,Tachibana K,Fujiwara T

更新日期：2018-11-15 00:00:00

abstract：:N-acetyl-β-d-hexosaminidase (Hex) is potential target for pesticide design. Here, a series of thiazolylhydrazone derivatives were designed, synthesized and evaluated as competitive inhibitors of OfHex1, a Hex from the agricultural pest Ostrinia furnacalis. The derivative 3k, with a (benzyloxy)methyl group at the N3 at...

journal_title：Bioorganic & medicinal chemistry

authors： Yang H,Liu T,Qi H,Huang Z,Hao Z,Ying J,Yang Q,Qian X

更新日期：2018-11-01 00:00:00