- Thiazole analogues of the marine alkaloid nortopsentin as inhibitors of bacterial biofilm formation
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Anti-virulence strategy is currently considered a promising approach to overcome the global threat of the antibiotic resistance. Among different bacterial virulence factors, the biofilm formation is recognized as one of the most relevant. Considering the high and growing percentage of multi-drug resistant infections that are biofilm-mediated, new therapeutic agents capable of counteracting the formation of biofilms are urgently required. In this scenario, a new series of 18 thiazole derivatives was efficiently synthesized and evaluated for its ability to inhibit biofilm formation against the Gram-positive bacterial reference strains Staphylococcus aureus ATCC 25923 and S. aureus ATCC 6538 and the Gram-negative strain Pseudomonas aeruginosa ATCC 15442. Most of the new compounds showed a marked selectivity against the Gram-positive strains. Remarkably, five compounds exhibited BIC50 values against S. aureus ATCC 25923 ranging from 1.0 to 9.1 μM. The new compounds, affecting the biofilm formation without any interference on microbial growth, can be considered promising lead compounds for the development of a new class of anti-virulence agents.
- Carbone, Anna,Cascioferro, Stella,Parrino, Barbara,Carbone, Daniela,Pecoraro, Camilla,Schillaci, Domenico,Cusimano, Maria Grazia,Cirrincione, Girolamo,Diana, Patrizia
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Read Online
- Synthesis and characterization of nucleobase functionalized monothiophenes
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The synthesis of a series of nucleobase functionalized thiophene monomers has been accomplished through the reaction of 2-bromo-1-thiophen-3-yl-ethanone with the corresponding DNA base anion. The distinctive pKa values for the various amine groups in the nucleobases provided a pathway for the creation of specific anions through selective deprotonation of these groups. Using the appropriate anion it is possible to create an amine linkage between the thiophene and nucleobase that is, analogous to that found between the deoxyribose sugar and nucleobase, in the biologically occurring nucleoside.
- McTiernan, Christopher D.,Chahma, M'hamed
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Read Online
- Synthesis and characterization of two new benzothiadiazole- and fused bithiophene based low band-gap D-A copolymers: Application as donor bulk heterojunction polymer solar cells
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Two new narrow bandgap D-A conjugated copolymers P1 and P2 containing different fused thiophene donor unit and same benzothiadiazole acceptor unit were synthesized by Stille cross-coupling polymerization, and characterized by 1H NMR, elemental analysis and GPC, TGA, DSC. Cyclic voltammetry measurement showed that the HOMO energy level both copolymers is deep lying (-5.10 and -5.35 eV for P1 and P2, respectively) which show that copolymers has good stability in the air and assured a higher open circuit voltage when it photovoltaic application. These copolymer were used as donor along with PC71BM and the BHJ polymer solar cells based on P1:PC71BM and P2:PC71BM processed with chloroform (CF) solvent showed over all PCE of 4.54% and 4.36%, respectively. Additionally, the PCE was improved up to 5.62% and 5.24% for P1:PC71BM and P2:PC71BM active layer processed with DIO (4 v%)/CF solvent. The enhancement in the PCE has been attributed to improved nanoscale morphology and crystalline nature of active layer as well as charge transport in the device with the addition of DIO, due to the higher boiling point of DIO causing slow evaporation rate during the film formation.
- Keshtov,Sharma,Kuklin,Ostapov,Godovsky,Khokhlov,Chen
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Read Online
- Synthesis and antibacterial activity of new N-[2-(thiophen-3-yl)ethyl] piperazinyl quinolones
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As a part of continuing search for potential antibacterial agents in the quinolones field, we have synthesized novel quinolone agents bearing N-[2-(thiophen-3-yl)ethyl] piperazinyl moiety in the 7-position of the quinolone ring. In vitro antibacterial eva
- Letafat, Bahram,Emami, Saeed,Mohammadhosseini, Negar,Faramarzi, Mohammad Ali,Samadi, Nasrin,Shafiee, Abbas,Foroumadi, Alireza
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Read Online
- Vinylethylene Carbonates as α,β-Unsaturated Aldehyde Surrogates for Regioselective [3 + 3] Cycloaddition
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Herein, we report a novel stepwise addition-controlled ring size method, to access tetrahydropyrimidines through an operationally simple [3 + 3] cycloaddition of vinylethylene carbonates with triazinanes. Interestingly, we could also use this method for a [3 + 3] oxidative cycloaddition, which allows the facile synthesis of polysubstituted terphenyls under mild conditions. Mechanistic studies suggest that vinylethylene carbonates could generate α,β-unsaturated aldehydes as 3-carbon synthons for cycloaddition via a combination process of Pd-catalyzed decarboxylation and β-H elimination.
- Xu, Yi,Chen, Lu,Yang, Yu-Wen,Zhang, Zhiqiang,Yang, Weibo
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supporting information
p. 6674 - 6678
(2019/09/03)
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- Diversity-Orientated Stereoselective Synthesis through Pd-Catalyzed Switchable Decarboxylative C?N/C?S Bond Formation in Allylic Surrogates
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Switchable catalytic transformation of reactants can be a powerful approach towards diversity-orientated synthesis from easily available molecular synthons. Herein, an endogenous ligand-controlled, Pd-catalyzed allylic substitution allowing for either selective C?N or C?S bond formation using vinylethylene carbonates (VECs) and N-sulfonylhydrazones as coupling partners has been developed. This versatile methodology provides a facile, divergent route for the highly chemo- and stereoselective synthesis of functional allylic sulfones or sulfonohydrazides. The newly developed protocol features wide substrate scope (nearly 80 examples), broad functional group tolerance, and potential for the late-stage functionalization of bioactive compounds. The isolation and crystallographic analysis of a catalytically competent π-allyl Pd complex suggests that the pathway leading to the allylic products proceeds through a different manifold as previously proposed for the functionalization of VECs with nucleophiles.
- Deng, Lei,Kleij, Arjan W.,Yang, Weibo
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supporting information
p. 19156 - 19161
(2018/11/30)
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- An efficient heterogeneous gold(I)-catalyzed hydration of haloalkynes leading to α-halomethyl ketones
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A highly efficient heterogeneous gold(I)-catalyzed hydration of haloalkynes has been developed that proceeds smoothly under mild and neutral conditions and provides a general and practical route for the synthesis of a variety of α-halomethyl ketones with high atom-economy, excellent yield, and recyclability of the gold(I) catalyst. The presented method delivers an attractive alternative to classical α-halogenation of ketones.
- Hu, Sifan,Liu, Dayi,Yan, Chenyu,Cai, Mingzhong
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supporting information
p. 2983 - 2991
(2018/12/04)
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- AuIII-Catalyzed Formation of α-Halomethyl Ketones from Terminal Alkynes
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A AuIII-catalyzed synthesis of α-halomethyl ketones from terminal alkynes was developed. This approach features excellent functional group compatibility and good yields for both aromatic and aliphatic terminal alkynes. The resulting α-halomethyl ketones were used to prepare heterocyclic indolizine structures. The plausible mechanism of the one-pot reaction is proposed.
- Xing, Yalan,Zhang, Ming,Ciccarelli, Sarah,Lee, John,Catano, Bryant
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supporting information
p. 781 - 785
(2017/02/15)
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- Water-controlled selective preparation of α-mono or α,α′-dihalo ketones: Via catalytic cascade reaction of unactivated alkynes with 1,3-dihalo-5,5-dimethylhydantoin
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The control of a reaction that can produce multiple products from the same starting material is a highly attractive and challenging concept in organic synthesis. An efficient protocol for the selective synthesis of α-mono or α,α′-dihalo ketones via a water-controlled three-component thiourea-catalyzed cascade reaction of unactivated alkynes, 1,3-dihalo-5,5-dimethylhydantoin and water has been developed. α-Monohaloketones were obtained in aqueous acetone at 45 °C; conversely, α,α′-dihalo ketones were formed with pure water as the sole solvent at room temperature.
- Wu, Chao,Xin, Xiu,Fu, Zhi-Min,Xie, Long-Yong,Liu, Kai-Jian,Wang, Zheng,Li, Wenyi,Yuan, Zhi-Hui,He, Wei-Min
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p. 1983 - 1989
(2017/06/09)
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- In(OTf)3/acid co-catalyzed hydration of 1-haloalkynes to α-halomethyl ketones
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A novel and efficient In(OTf)3and HOAc cooperatively catalyzed hydration of 1-haloalkynes is described. This method provides ready access to α-chloromethyl ketones, α-bromomethyl ketones and α-iodomethyl ketones in moderate to high yields from simple, inexpensive starting materials. A broad substrate scope is achieved, and the reaction is compatible with various functional groups, including alkoxy, trifluoromethyl, halide, hydroxyl, cyclohexyl, and heterocyclic groups.
- Zeng, Ming,Huang, Rui-Xue,Li, Wen-Yi,Liu, Xiao-Wen,He, Fu-Ling,Zhang, Yi-Yuan,Xiao, Fang
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p. 3818 - 3822
(2016/07/06)
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- Metal-free hydration of aromatic haloalkynes to α-halomethyl ketones
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A highly regioselective and efficient metal-free hydration of aromatic haloalkynes to α-halomethyl ketones using cheap tetrafluoroboric acid as catalyst is described. The protocol is conducted under convenient conditions and affords products in good to excellent yields, with broad substrate scope, including a variety of aromatic alkynyl chlorides, alkynyl bromides, and alkynyl iodides.
- Ye, Min,Wen, Yuelu,Li, Huifang,Fu, Yejuan,Wang, Qinghao
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supporting information
p. 4983 - 4986
(2016/10/21)
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- First Catalyzed Hydration of Haloalkynes by a Recyclable Catalytic System
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The hydration of haloalkynes to give α-halomethyl ketones was achieved based on a combination of a Cu(OAc)2 catalyst and a TFA (trifluoroacetic acid) promoter. This is the first synthesis of chloro/bromo/iodo methyl ketones through a hydration reaction catalyzed by a recyclable catalytic system. The catalytic system has a wide substrate scope and excellent chemoselectivity, and the procedure can also be scaled up.
- Zou, Huaxu,He, Weibao,Dong, Qizhi,Wang, Ruijia,Yi, Niannian,Jiang, Jun,Pen, Dongming,He, Weimin
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p. 116 - 121
(2016/01/26)
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- Highly Efficient Synthesis of α-Halomethylketones via Ce(SO4)2/Acid Co-Catalyzed Hydration of Alkynes
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A general atom-economical approach for the synthesis of α-halomethyl ketones is demonstrated through Ce(SO4)2/acid co-catalyzed hydration of a wide range of haloalkynes. The reactions are conducted under convenient conditions and provide products with excellent regioselectivity in good to excellent yields, with broad substrate scope. This protocol is an alternative to conventional α-halogenation of ketones.
- Zou, Huaxu,Jiang, Jun,Yi, Niannian,Fu, Wenqiang,Deng, Wei,Xiang, Jiannan
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supporting information
p. 1251 - 1254
(2016/12/27)
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- Proton pump inhibitors
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A proton pump inhibitor containing a compound represented by the formula (I) wherein X and Y are the same or different and each is a bond or a spacer having 1 to 20 carbon atoms in the main chain, R 1 is an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group, R 2 , R 3 and R 4 are the same or different and each is a hydrogen atom, an optionally substituted hydrocarbon group, an optionally substituted thienyl group, an optionally substituted benzo[b]thienyl group, an optionally substituted furyl group, an optionally substituted pyridyl group, an optionally substituted pyrazolyl group, an optionally substituted pyrimidinyl group, an acyl group, a halogen atom, a cyano group or a nitro group, R 5 and R 6 are the same or different and each is a hydrogen atom or an optionally substituted hydrocarbon group, which has a superior proton pump action and shows an antiulcer activity and the like after conversion to a proton pump inhibitor in the body, or a salt thereof. or a prodrug thereof is provided.
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Paragraph 0242
(2015/11/16)
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- Novel arylalkenylpropargylamines as neuroprotective, potent, and selective monoamine oxidase B inhibitors for the treatment of Parkinson's disease
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To develop novel neuroprotective agents, a library of novel arylalkenylpropargylamines was synthesized and tested for inhibitory activities against monoamine oxidases. From this, a number of highly potent and selective monoamine oxidase B inhibitors were identified. Selected compounds were also tested for neuroprotection in in vitro studies with PC-12 cells treated with 6-OHDA and rotenone, respectively. It was observed that some of the compounds tested yielded a marked increase in survival in PC-12 cells treated with the neurotoxins. This indicates that these propargylamines are able to confer protection against the effects of the toxins and may also be considered as novel disease-modifying anti-Parkinsonian agents, which are much needed for the therapy of Parkinson's disease.
- Huleatt, Paul B.,Khoo, Mui Ling,Chua, Yi Yuan,Tan, Tiong Wei,Liew, Rou Shen,Balogh, Balázs,Deme, Ruth,G?l?ncsér, Flóra,Magyar, Kalman,Sheela, David P.,Ho, Han Kiat,Sperlágh, Beáta,Mátyus, Péter,Chai, Christina L. L.
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supporting information
p. 1400 - 1419
(2015/03/04)
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- Synthesis and structure-activity relationship of aminoarylthiazole derivatives as correctors of the chloride transport defect in cystic fibrosis
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Abstract The cystic fibrosis transmembrane conductance regulator (CFTR) is a chloride channel present in the membrane of epithelial cells. Mutations affecting the CFTR gene cause cystic fibrosis (CF), a multi-organ severe disease. The most common CF mutation, F508del, impairs the processing and activity (gating) of CFTR protein. Other mutations, like G551D, only cause a gating defect. Processing and gating defects can be targeted by small molecules called generically correctors and potentiators, respectively. Aminoarylthiazoles (AATs) represent an interesting class of compounds that includes molecules with dual activity, as correctors and potentiators. With the aim to improve the activity profile of AATs, we have now designed and synthesized a library of novel compounds in order to establish an initial SAR that may provide indications about the chemical groups that are beneficial or detrimental for rescue activity. The new compounds were tested as correctors and potentiators in CFBE41o-expressing F508del-CFTR using a functional assay. A dual active compound, AAT-4a, characterized by improved efficacy and marked synergy when combined with the corrector VX-809 has been identified. Moreover, by computational methods, a possible binding site for AATs in nucleotide binding domain NBD1 has been detected. These results will direct the synthesis of new analogues with possibly improved activity.
- Pesce, Emanuela,Bellotti, Marta,Liessi, Nara,Guariento, Sara,Damonte, Gianluca,Cichero, Elena,Galatini, Andrea,Salis, Annalisa,Gianotti, Ambra,Pedemonte, Nicoletta,Zegarra-Moran, Olga,Fossa, Paola,Galietta, Luis J.V.,Millo, Enrico
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supporting information
p. 14 - 35
(2015/06/08)
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- 2- and 3-substituted imidazo[1,2-a]pyrazines as inhibitors of bacterial type IV secretion
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A novel series of 8-amino imidazo[1,2-a]pyrazine derivatives has been developed as inhibitors of the VirB11 ATPase HP0525, a key component of the bacterial type IV secretion system. A flexible synthetic route to both 2- and 3-aryl substituted regioisomers has been developed. The resulting series of imidazo[1,2-a]pyrazines has been used to probe the structure-activity relationships of these inhibitors, which show potential as antibacterial agents.
- Sayer, James R.,Walldn, Karin,Pesnot, Thomas,Campbell, Frederick,Gane, Paul J.,Simone, Michela,Koss, Hans,Buelens, Floris,Boyle, Timothy P.,Selwood, David L.,Waksman, Gabriel,Tabor, Alethea B.
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p. 6459 - 6470
(2015/01/09)
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- Gold-catalyzed hydration of haloalkynes to α-halomethyl ketones
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A general atom-economical approach for the synthesis of α-halomethyl ketones is demonstrated through hydration of a wide range of haloalkynes. Other outstanding features include excellent yields from both alkyl- and aryl-substituted haloalkynes and wide functional group tolerance. This protocol is an alternative to conventional α-halogenation of ketones.
- Xie, Longyong,Wu, Yundong,Yi, Weiguo,Zhu, Lei,Xiang, Jiannan,He, Weimin
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p. 9190 - 9195
(2013/10/08)
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- SUBSTITUTED 8 - AMINO - IMIDAZO [1, 2-A] PYRAZ1NES AS ANTIBACTERIAL AGENTS
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The present invention relates to substituted imidazo[1,2-a]pyrazines of Formula (I) and their use as antibacterial agents.
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(2013/02/27)
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- Design and synthesis of 2-heterocyclyl-3-arylthio-1H-indoles as potent tubulin polymerization and cell growth inhibitors with improved metabolic stability
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New arylthioindoles (ATIs) were obtained by replacing the 2-alkoxycarbonyl group with a bioisosteric 5-membered heterocycle nucleus. The new ATIs 5, 8, and 10 inhibited tubulin polymerization, reduced cell growth of a panel of human transformed cell lines
- La Regina, Giuseppe,Bai, Ruoli,Rensen, Willeke,Coluccia, Antonio,Piscitelli, Francesco,Gatti, Valerio,Bolognesi, Alessio,Lavecchia, Antonio,Granata, Ilaria,Porta, Amalia,Maresca, Bruno,Soriani, Alessandra,Iannitto, Maria Luisa,Mariani, Marisa,Santoni, Angela,Brancale, Andrea,Ferlini, Cristiano,Dondio, Giulio,Varasi, Mario,Mercurio, Ciro,Hamel, Ernest,Lavia, Patrizia,Novellino, Ettore,Silvestri, Romano
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experimental part
p. 8394 - 8406
(2012/02/14)
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- INDOLIC DERIVATIVES AND USE THEREOF IN MEDICAL FIELD
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The present invention concerns indolic derivatives and use thereof in medical field. Particularly, the invention concerns 3-[(3',4',5'- trimethoxyphenyl)thio]-1 H-indole derivatives and bioisosteric derivatives thereof and their use for the treatment of tumours.
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Page/Page column 22-23
(2011/10/13)
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- Pyrrolidino-tetrahydroisoquinolines bearing pendant heterocycles as potent dual H3 antagonist and serotonin transporter inhibitors
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A series of novel and potent 6-heteroaryl-pyrrolidino-tetrahydroisoquinolines with dual histamine H3 antagonist/serotonin transporter inhibitor activity is described. In vitro and in vivo data are discussed.
- Keith, John M.,Gomez, Leslie A.,Barbier, Ann J.,Wilson, Sandy J.,Boggs, Jamin D.,Lord, Brian,Mazur, Curt,Aluisio, Leah,Lovenberg, Timothy W.,Carruthers, Nicholas I.
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p. 4374 - 4377
(2008/02/11)
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- PROTON PUMP INHIBITORS
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A proton pump inhibitor containing a compound represented by the formula (I) wherein X and Y are the same or different and each is a bond or a spacer having 1 to 20 carbon atoms in the main chain, R1 is an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group, R2, R3 and R4 are the same or different and each is a hydrogen atom, an optionally substituted hydrocarbon group, an optionally substituted thienyl group, an optionally substituted benzo[b]thienyl group, an optionally substituted furyl group, an optionally substituted pyridyl group, an optionally substituted pyrazolyl group, an optionally substituted pyrimidinyl group, an acyl group, a halogen atom, a cyano group or a nitro group, R5 and R6 are the same or different and each is a hydrogen atom or an optionally substituted hydrocarbon group, which has a superior proton pump action and shows an antiulcer activity and the like after conversion to a proton pump inhibitor in the body, or a salt thereof. or a prodrug thereof is provided.
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- PROTON PUMP INHIBITORS
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Proton pump inhibitors which have excellent proton pumping activity and which can be converted in vivo into proton pump inhibitors to exhibit antiulcer effect and so on, containing compounds represented by the general formula (I) or salts thereof or prodrugs of the same: (I) wherein X and Y are each independently a free valency or a spacer whose main chain has 1 to 20 carbon atoms; R1 is an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group; R2, R3 and R4 are each independently hydrogen, an optionally substituted hydrocarbon group, optionally substituted thienyl, optionally substituted benzo[b]thienyl, optionally substituted furyl, optionally substituted pyridyl, optionally substituted pyrazolyl, optionally substituted pyrimidinyl, acyl, halogeno, cyano, or nitro; and R5 and R6 are each independently hydrogen or an optionally substituted hydrocarbon group.
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(2010/10/20)
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- TMS·OTf-Catalyzed α-bromination of carbonyl compounds by N-bromosuccinimide
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Various carbonyl compounds undergo α-bromination reaction under a mild and practical condition utilizing N-bromosuccinimide (NBS), catalyzed by trimethylsilyl trifluoromethanesulfonate (TMS·OTf). This method is also effective for the side-chain bromination of heteroaromatic carbonyl compounds without the ring brominations.
- Guha, Samar Kumar,Wu, Bo,Kim, Beom Soo,Baik, Woonphil,Koo, Sangho
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p. 291 - 293
(2007/10/03)
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- HEXAHYDRO-PYRROLO-ISOQUINOLINE COMPOUNDS
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Certain hexahydro-pyrrolo-isoquinoline compounds are histamine H3 receptor and serotonin transporter modulators useful in the treatment of histamine H3 receptor- and serotonin-mediated diseases.
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(2010/11/25)
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- Pyrrole derivatives and medicinal composition
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The invention relates to a pharmaceutical composition comprising a pyrrole derivative of the following formula [1] or a pharmaceutically acceptable salt thereof, or a solvate of either of them, as an active ingredient. STR1 (wherein R1 represents hydrogen or alkoxycar91 bonylamino, R2 represents alkyl, aryl which may be substituted, aromatic heterocyclyl which may be substituted, unsubstituted amino, monoalkylamino, dialkylamino, or cyclic amino which may be substituted; R3 represents cyano or carbamoyl; R4 represents hydrogen or alkyl; E represents alkylene; q is equal to 0 or 1, A represents methyl, aryl which may be substituted, or aromatic heterocyclyl which may be substituted). The pharmaceutical composition of the invention is effective for the treatment of pollakiuria or urinary incontinence.
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- METHODS FOR PREPARING ANTIPROLIFERATIVE 5-SUBSTITUTED PYRIMIDONE COMPOUNDS
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Intermediates for preparing derivatives of 5-thia- and5-selenopyrimidinone which are useful as inhibitors of the enzymes glydnamide ribonucleotide formyl transferase (GARFT) and amino imidazole carboxamide ribonucleotide formyl transferase (AICARFT). The present invention is also directed to methods of preparing these intermediates
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- Antiproliferative substituted 5-thiapyrimidinone and 5-selenopyrimidinone compounds
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The present invention is directed to derivatives of 5-thia- and 5-selenopyrimidinone, which are useful as inhibitors of the enzymes glycinamide ribonucleotide formyl transferase (GARFT) and amino imidazole carboxamide ribonucleotide formyl transferase AICARFT), pharmaceutical compositions containing these derivatives, and methods of using these derivatives. The present invention is also directed to intermediates useful for preparing these derivatives and methods of preparing these intermediates.
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- Synthesis and evaluation of a novel series of pyrrolizine derivatives as dual cyclooxygenase-1 and 5-lipoxygenase inhibitors
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The aim of our study was to investigate structure activity relationship following the replacement of the 6-phenyl substituent at the 6,7-diaryl-2,3-dihydropyrrolizine template by various heteroaromatic residues. In this context we developed a new, efficient, and highly sensitive test method for the screening of dual cyclooxygenase-1 (COX-1) and 5-lipoxygenase (5-LOX) inhibitors. We used human platelets as a source of COX-1 and human PMNLs as a source of 5-LOX. Both cell types were isolated from the same volume of blood. PGE2 and LTB4 respectively were determined by highly selective and sensitive ELISA kits, using monoclonal antibodies. For a single determination at most 0.5 mL whole blood is needed.
- Laufer, Stefan,Striegel, Hans-Guenter,Neher, Karola,Zechmeister, Pia,Donat, Cornelia,Stolingwa, Katrin,Baur, Sibylle,Tries, Susanne,Kammermeier, Thomas,Dannhardt, Gerd,Kiefer, Werner
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p. 307 - 312
(2007/10/03)
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- The chemistry of pseudomonic acid part 14. Synthesis and in vivo biological activity of heterocyclyl substituted oxazole derivatives
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Semisynthetic analogues of pseudomonic acid A have been prepared containing a heterocyclyl substituted oxazole. Derivatives in which the heterocycle was thiophene, furan, pyridine, or isoxazole showed good antibacterial potency and were further evaluated in vivo. Both pharmacokinetic parameters and oral activity against an experimental intraperitoneal sepsis were superior to results obtained from previously described pseudomonic acid A derivatives.
- Broom,Elder,Hannan,Pons,O'Hanlon,Walker,Wilson,Woodall
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p. 1336 - 1344
(2007/10/02)
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- Oxygen Isosteric Derivatives of 3-(3-Hydroxyphenyl)-N-n-propylpiperidine
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Some substituted 3-phenylmorpholines (10a-e,j,k) and 3-thienylmorpholines (10f,g), isosteres of 3-(3-hydroxyphenyl)-N-n-propylpiperidine (3-PPP), were prepared and submitted to binding assays on D-2 dopaminergic and 5-HT1 and 5-HT2 serotonergic receptors, in comparison with 3-PPP and its analogue 3a,b.The results show the loss of D-2 affinity for all morpholines, while a certain activity was still observable for piperidine derivatives.Regarding the serotonergic affinity, only chloro and methoxy derivatives (10a-d) were moderately active on the 5-HT1A receptor, either when the substituent was in the C-2 or C-3 position, whereas no tested compounds showed affinity toward the 5-HT2 receptor.
- Perrone, Roberto,Berardi, Francesco,Leopoldo, Marcello,Tortorella, Vincenzo,Lograno, Marcello D.,et al.
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p. 3045 - 3049
(2007/10/02)
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- Antibacterial monic acid derivatives
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A compound of the formula (I) STR1 wherein R is a group STR2 R1 is hydrogen, phenyl, C1-20 alkyl, C2-8 alkenyl or C2-8 alkynyl each of which may optionally be substituted; or C3-7 cycloalkyl, X is a divalent group --Y--C=C--, and Y is oxygen or sulphur, have antibacterial and/or antimycoplasmal activity.
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