Synthesis of 1-[3-(4-benzotriazol-1/2-yl-3-fluoro-phenyl)-2-oxo-oxazolidin-5-ylmethyl]-3-substituted-thiourea derivatives as antituberculosis agents.

abstract：:Covalent drugs play corresponding bioactivities by forming covalent bonds with the target, which possess many significant pharmacological advantages including high potency, ligand efficiency, and long-lasting effects. However, development of covalent inhibitors is a challenge due to their presumed indiscriminate react...

journal_title：European journal of medicinal chemistry

authors： Liu J,Li L,Li X,Wang X,Zhao X,Qiao Y,Xu Y,Sun Y,Qian L,Liu Z,Ji A,Lou H

更新日期：2021-01-01 00:00:00

abstract：:The current epidemic of antibiotic resistant bacterial infections has fueled the demand for novel antibiotics exhibiting both antibacterial efficacy and anti-drug resistance. This need has not been fully satisfied by the conventional "one target-one molecule" approach. Consequently, there has been rising interest in t...

journal_title：European journal of medicinal chemistry

authors： Wetzel C,Lonneman M,Wu C

更新日期：2021-01-01 00:00:00

abstract：:Alzheimer's disease (AD) is the most common form of dementia characterized by presence of extracellular amyloid plaques and intracellular neurofibrillary tangles composed of tau protein. Currently there are close to 50 million people living with dementia and this figure is expected to increase to 75 million by 2030 pu...

journal_title：European journal of medicinal chemistry

authors： Wang L,Bharti,Kumar R,Pavlov PF,Winblad B

更新日期：2021-01-01 00:00:00

abstract：:Naturally occurring polyamines: putrescine, spermidine and spermine are crucial for Kinetoplastid growth and persistence. These aliphatic polycations are either biosynthesized or internalized into Kinetoplastid by active transport. Impairing the polyamine metabolism using polyamine derivatives is an interesting path i...

journal_title：European journal of medicinal chemistry

authors： Jagu E,Pomel S,Pethe S,Loiseau PM,Labruère R

更新日期：2017-10-20 00:00:00

abstract：:We previously reported the synthesis and the antimycobacterial activity of 4-(7,7-dimethyl-7H-furo[3,2-f]chromen-2-yl)pyridine. From this result, we sought to design simple synthetic accesses to related structures allowing the preparation of a diverse set of analogues. Two approaches were investigated. From 3-(2-bromo...

journal_title：European journal of medicinal chemistry

authors： Alvey L,Prado S,Saint-Joanis B,Michel S,Koch M,Cole ST,Tillequin F,Janin YL

更新日期：2009-06-01 00:00:00

abstract：:A number of 3-phenylquinolinylchalcone derivatives were synthesized and evaluated in vitro for their antiproliferative activities against three breast cancer cell lines (MCF-7, MDA-MB-231, and SKBR-3), and a non-cancer normal epithelial cell line (H184B5F5/M10). Among them, (E)-3-[3-(4-methoxyphenyl)quinolin-2-yl]-1-(...

journal_title：European journal of medicinal chemistry

authors： Tseng CH,Tzeng CC,Hsu CY,Cheng CM,Yang CN,Chen YL

更新日期：2015-06-05 00:00:00

abstract：:A striking dual inhibition of enzymes α-glucosidase and butyrylcholinesterase by small drug-like molecules, including 1,4-disubstituted-1,2,3-triazoles, chalcones, and benzothiazepines, was rationalized with the help of Molecular Field Topology Analysis, a 3D QSAR technique similar to CoMFA. A common pharmacophore sup...

journal_title：European journal of medicinal chemistry

authors： Jabeen F,Oliferenko PV,Oliferenko AA,Pillai GG,Ansari FL,Hall CD,Katritzky AR

更新日期：2014-06-10 00:00:00

abstract：:The two new mononuclear complexes were prepared by reacting symmetric Schiff base, containing pyrimidine rings and the metal chlorides of Pd(II) and Pt(II) in methanol. The mononuclear structure of the complexes was confirmed on the basis of elemental analyses, magnetic susceptibility, IR, UV-Vis, NMR, DTA/TGA and API...

journal_title：European journal of medicinal chemistry

authors： Sönmez M,Celebi M,Yardim Y,Sentürk Z

更新日期：2010-09-01 00:00:00

abstract：:A practicable method of introducing a side chain to the C-4' position of 5-O-desosamine in the 14-membered ketolides was developed. And using this method, a series of novel modified 5-O-mycaminose ketolides were synthesized. These ketolides containing 5-O-4'-carbamate mycaminose were evaluated for their in vitro antib...

journal_title：European journal of medicinal chemistry

authors： Xu Y,Chen X,Zhu D,Liu Y,Zhao Z,Jin L,Liu C,Lei P

更新日期：2013-11-01 00:00:00

abstract：:Phenolic acids are ubiquitous antioxidants accounting for approximately one third of the phenolic compounds in our diet. Their importance was supported by epidemiological studies that suggest an inverse relationship between dietary intake of phenolic antioxidants and the occurrence of diseases, such as cancer and neur...

journal_title：European journal of medicinal chemistry

authors： Teixeira J,Silva T,Benfeito S,Gaspar A,Garrido EM,Garrido J,Borges F

更新日期：2013-04-01 00:00:00

abstract：:Eukaryotic translation initiation factor 4E (eIF4E) is considered as the corner stone in the cap-dependent translation initiation machinery. Its role is to recruit mRNA to the ribosome through recognition of the 5'-terminal mRNA cap structure (m7GpppN, where G is guanosine, N is any nucleotide). eIF4E is implicated in...

journal_title：European journal of medicinal chemistry

authors： Soukarieh F,Nowicki MW,Bastide A,Pöyry T,Jones C,Dudek K,Patwardhan G,Meullenet F,Oldham NJ,Walkinshaw MD,Willis AE,Fischer PM

更新日期：2016-11-29 00:00:00

abstract：:A series of novel (5-oxazolyl)phenyl amine derivatives were synthesized and their antiviral activities against the hepatitis C virus (HCV) and the coxsackie virus B3 (CVB3) and B6 (CVB6) were evaluated in vitro. Bioassays showed that the synthesized compounds 17a1, 17a4, 17a6, 17b1, 17d1, 17e2 and 17g3 exhibited poten...

journal_title：European journal of medicinal chemistry

authors： Zhong ZJ,Zhang DJ,Peng ZG,Li YH,Shan GZ,Zuo LM,Wu LT,Li SY,Gao RM,Li ZR

更新日期：2013-11-01 00:00:00

abstract：:Herein we report the design, synthesis, bioinformatic and biological studies of benzimidazole and benzothiophene derivatives as new cannabinoid receptor ligands. To test the hypothesis that the lack of a hydrogen bond interaction between benzimidazole and benzothiophene derivatives with Lys192 reduces their affinity f...

journal_title：European journal of medicinal chemistry

authors： Romero-Parra J,Mella-Raipán J,Palmieri V,Allarà M,Torres MJ,Pessoa-Mahana H,Iturriaga-Vásquez P,Escobar R,Faúndez M,Di Marzo V,Pessoa-Mahana CD

更新日期：2016-11-29 00:00:00

abstract：:The target phosphoramidates 5a-e were prepared in one step from 3-hydroxypropyl derivatives 3a-e of nonsteroidal anti-inflammatory drugs (fenoprofen, ketoprofen, ibuprofen, indomethacin, diclofenac). The products 3a-e and 5a-e were evaluated for their cytostatic and antiviral activity against malignant tumour cell lin...

journal_title：European journal of medicinal chemistry

authors： Wittine K,Benci K,Rajić Z,Zorc B,Kralj M,Marjanović M,Pavelić K,De Clercq E,Andrei G,Snoeck R,Balzarini J,Mintas M

更新日期：2009-01-01 00:00:00

abstract：:Three new copper(II) complexes of 5-pyridin-2-yl-[1,3]dioxolo[4,5-g]isoquinoline (PYP), i.e. [Cu₂(PYP)₂Cl₄] (1), [Cu₄(PYP)₄(ClO₄)₂(H₂O)₂](ClO₄)₂·2H₂O (2), and [Cu₂(PYP)2Cl4]n (3), were synthesized and fully characterized. In comparison to free PYP, complexes 1-3 exhibited enhanced cytotoxicity against tested human tum...

journal_title：European journal of medicinal chemistry

authors： Huang KB,Chen ZF,Liu YC,Wang M,Wei JH,Xie XL,Zhang JL,Hu K,Liang H

更新日期：2013-01-01 00:00:00

abstract：:Several regioisomeric tetrazolyl indole derivatives with structurally modified alkyl substituents at the tetracyclic indole nitrogen containing N-ethyl amino tetrazole moiety have been synthesized and screened for their ER binding affinity, agonist (estrogenic), antagonist (antiestrogenic) and anti-implantation activi...

journal_title：European journal of medicinal chemistry

authors： Singh US,Shankar R,Yadav GP,Kharkwal G,Dwivedi A,Keshri G,Singh MM,Moulik PR,Hajela K

更新日期：2008-10-01 00:00:00

abstract：:A series of 19 analogues of the antiproliferative naphthopyran LY290181 were prepared for structure-activity relationship studies. We found the best activities for test compounds bearing small substituents at the meta position of the phenyl ring. The mode of action of LY290181 and eight new analogues was studied in de...

journal_title：European journal of medicinal chemistry

authors： Schmitt F,Gold M,Rothemund M,Andronache I,Biersack B,Schobert R,Mueller T

更新日期：2019-02-01 00:00:00

abstract：:A new series of pyrazolo[3,4-d]pyridazin-7-one derivatives were synthesised and evaluated for their in vitro antileishmanial activity against Leishmania amazonensis promastigote and axenic amastigote forms. The results showed that the pyrazolo[3,4-d]-pyridazin-7-one-N-acylhydrazone-(bi)thiophene hybrids 5b, 6b and 6d ...

journal_title：European journal of medicinal chemistry

authors： Jacomini AP,Silva MJV,Silva RGM,Gonçalves DS,Volpato H,Basso EA,Paula FR,Nakamura CV,Sarragiotto MH,Rosa FA

更新日期：2016-11-29 00:00:00

abstract：:We report the design and synthesis of a series of dipeptide-type inhibitors with novel P3 scaffolds that display potent inhibitory activity against SARS-CoV 3CLpro. A docking study involving binding between the dipeptidic lead compound 4 and 3CLpro suggested the modification of a structurally flexible P3 N-(3-methoxyp...

journal_title：European journal of medicinal chemistry

authors： Thanigaimalai P,Konno S,Yamamoto T,Koiwai Y,Taguchi A,Takayama K,Yakushiji F,Akaji K,Chen SE,Naser-Tavakolian A,Schön A,Freire E,Hayashi Y

更新日期：2013-10-01 00:00:00

abstract：:Using a dengue replicon cell line-based screening, we identified 3-(dimethylamino)propyl(3-((4-(4-fluorophenyl)-1-oxophthalazin-2(1H)-yl)methyl)phenyl)carbamate (10a) as a potent DENV-2 inhibitor, with an IC50 value of 0.64 μM. A series of novel phthalazinone derivatives based on hit 10a were synthesized and evaluated...

journal_title：European journal of medicinal chemistry

authors： Lu D,Liu J,Zhang Y,Liu F,Zeng L,Peng R,Yang L,Ying H,Tang W,Chen W,Zuo J,Tong X,Liu T,Hu Y

更新日期：2018-02-10 00:00:00

abstract：:In the last years the continuous efforts in the development of novel and effective inhibitors of human monoamine oxidases (hMAOs) promoted the discovery of new agents able to effectively and selectively bound one of the two isoforms (hMAO-A and hMAO-B). However, the parent chalcone scaffold still covers an important r...

journal_title：European journal of medicinal chemistry

authors： Guglielmi P,Mathew B,Secci D,Carradori S

更新日期：2020-11-01 00:00:00

abstract：:We identified a new series of azole antifungal agents bearing a pyrrolotriazinone scaffold. These compounds exhibited a broad in vitro antifungal activity against pathogenic Candida spp. (fluconazole-susceptible and fluconazole-resistant) and were 10- to 100-fold more active than voriconazole against two Candida albic...

journal_title：European journal of medicinal chemistry

authors： Montoir D,Guillon R,Gazzola S,Ourliac-Garnier I,Soklou KE,Tonnerre A,Picot C,Planchat A,Pagniez F,Le Pape P,Logé C

更新日期：2020-03-01 00:00:00

abstract：:Based on our previous results on the ascertained potent growth inhibition effect against a panel of 60 human tumors cell lines at National Cancer Institute of Bethesda (NCI), we have synthesized a novel series of thirty-one 2-[N-methyl(R-phenyl)-aminomethyl]-3-phenyl-7-trifluoromethylquinoxalines (1-31). The lead comp...

journal_title：European journal of medicinal chemistry

authors： Piras S,Carta A,Briguglio I,Corona P,Paglietti G,Luciani R,Costi MP,Ferrari S

更新日期：2014-03-21 00:00:00

abstract：:Glycogen synthase kinase 3β (GSK-3β) is widely recognised as a relevant player in the pathogenesis of several highly prevalent disorders such as Alzheimer's disease, mood disorders, diabetes and cancer. Therefore, this enzyme constitutes a highly attractive therapeutic target for the development of selective inhibitor...

journal_title：European journal of medicinal chemistry

authors： Bidon-Chanal A,Fuertes A,Alonso D,Pérez DI,Martínez A,Luque FJ,Medina M

更新日期：2013-02-01 00:00:00

abstract：:Understanding subtle aspects of hydrogen bonding is a challenging but crucial task to improve our ability to design ligands with high affinity for protein hosts. To gain a deeper understanding of these aspects, we investigated a series of thrombin inhibitors in which the basicity of the ligand's group that accepts an ...

journal_title：European journal of medicinal chemistry

authors： Nasief NN,Said AM,Hangauer D

更新日期：2017-01-05 00:00:00

abstract：:Novel 2-substituted isobutyric acid derivatives were synthesized and their hypolipidemic activity was evaluated in high cholesterol diet fed rat model. The amide 5a was found to decrease the levels of serum total cholesterol, LDL cholesterol and triglycerides in hyperlipidemic rats to a greater degree than the referen...

journal_title：European journal of medicinal chemistry

authors： Idrees GA,Abuo-Rahma Gel-D,Aly OM,Radwan MF

更新日期：2009-06-01 00:00:00

abstract：:Cytarabine is a chemotherapeutic agent predominately used for the treatment of acute myeloid leukemia and lymphoblastic leukemia. Cytarabine is a polar nucleoside, has a short plasma half-life, and its use is associated with severe side effects. Fatty acyl derivatives of cytarabine were synthesized with the expectatio...

journal_title：European journal of medicinal chemistry

authors： Chhikara BS,Mandal D,Parang K

更新日期：2010-10-01 00:00:00

abstract：:Survival of the human malaria parasite Plasmodium falciparum is dependent on pantothenate (vitamin B5), a precursor of the fundamental enzyme cofactor coenzyme A. CJ-15,801, an enamide analogue of pantothenate isolated from the fungus Seimatosporium sp. CL28611, was previously shown to inhibit P. falciparum proliferat...

journal_title：European journal of medicinal chemistry

authors： Spry C,Sewell AL,Hering Y,Villa MVJ,Weber J,Hobson SJ,Harnor SJ,Gul S,Marquez R,Saliba KJ

更新日期：2018-01-01 00:00:00

abstract：:Very recently, we demonstrated that N(6)-isopentenyladenosine, a cytokinin nucleoside, exerts a potent and selective antiviral effect on the replication of human enterovirus 71. The present study is devoted to the structure optimization of another natural compound: N(6)-benzyladenosine. We mainly focused on the explor...

journal_title：European journal of medicinal chemistry

authors： Drenichev MS,Oslovsky VE,Sun L,Tijsma A,Kurochkin NN,Tararov VI,Chizhov AO,Neyts J,Pannecouque C,Leyssen P,Mikhailov SN

更新日期：2016-03-23 00:00:00

abstract：:A series of anthracenone-based oxime ethers and -esters were synthesized in order to evaluate their antiproliferative activity. Several investigated compounds displayed strong antiproliferative activity against K562 leukemia cells and proved to be strong inhibitors of tubulin polymerization. In this context, anthracen...

journal_title：European journal of medicinal chemistry

authors： Surkau G,Böhm KJ,Müller K,Prinz H

更新日期：2010-08-01 00:00:00