- DNA binding ligands targeting drug-resistant bacteria: Structure, activity, and pharmacology
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We describe the lead optimization and structure-activity relationship of DNA minor-groove binding ligands, a novel class of antibacterial molecules. These compounds have been shown to target A/T-rich sites within the bacterial genome and, as a result, inhibit DNA replication and RNA transcription. The optimization was focused on N-terminal aromatic heterocycles and C-terminal amines and resulted in compounds with improved in vivo tolerability and excellent in vitro antibacterial potency (MIC ≥ 0.031 μg/mL) against a broad range of Gram-positive pathogens, including drug-resistant strains such as methicillin-resistant Stapylococcus aureus (MRSA), penicillin-resistant Streptococcus pneumoniae (PRSP), and vancomycin-resistant Enterococcus faecalis (VRE). In a first proof-of-concept study, a selected compound (35) showed in vivo efficacy in a mouse peritonitis model against methicillin-sensitive S. aureus infection with an ED50 value of 30 mg/kg.
- Kaizerman, Jacob A.,Gross, Matthew I.,Ge, Yigong,White, Sarah,Hu, Wenhao,Duan, Jian-Xin,Baird, Eldon E.,Johnson, Kirk W.,Tanaka, Richard D.,Moser, Heinz E.,Bürli, Roland W.
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Read Online
- PYRIMIDONE DERIVATIVES CONTAINING TWO FUSED BICYCLIC RINGS
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The invention relates to a compound of formula (I), wherein the variables are defined in the specification. It also relates to a pesticidal mixture comprising the compound of formula (I); the use of compounds of formula (I) as an agrochemical pesticide; a method for combating or controlling invertebrate pests, a method for protecting growing plants from attack or infestation by invertebrate pests, seed comprising a compound of the formula (I); the use of a compound of the formula (I) for protecting growing plants from attack or infestation by invertebrate pests; and a method for treating or protecting an animal from infestation or infection by invertebrate pests.
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Page/Page column 128
(2021/05/29)
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- Synthesis and biological evaluation of novel imidazo[1,2-a]pyridine-oxadiazole hybrids as anti-proliferative agents: Study of microtubule polymerization inhibition and DNA binding
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Efforts towards the development of potential anticancer agents, a new series of imidazo[1,2-a]pyridine-oxadiazole hybrids were synthesized and evaluated for their in vitro anticancer activity against lung cancer (A549) and prostate cancer (PC-3, DU-145) cell lines. Amongst the compounds tested, 6d showed the highest potency on A549 cells with an IC50 value of 2.8 ± 0.02 μM. Flow cytometric analysis of compound 6d treated A549 cells showed apoptosis induction by annexin-v/PI dual staining assay and the effect of 6d on different phases of cell cycle was also analyzed. Target based studies demonstrated the inhibition of tubulin polymerization by 6d at an IC50 value of 3.45 ± 0.51 μM and its effective binding with CT-DNA. Further, the molecular modelling studies revealed that 6d has a prominent binding affinity towards α/β-tubulin receptor with admirable physico-chemical properties.
- Babu, Bathini Nagendra,Jadhav, Govinda Shivaji,Kadagathur, Manasa,Kiranmai, Gaddam,Nagesh, Narayana,Parimala Devi, G.,Sana, Sravani,Shankaraiah, Nagula,Sigalapalli, Dilep Kumar,Tangellamudi, Neelima D.,Tokala, Ramya,Tripura, Chaturvedula
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- Design, synthesis, in vitro evaluation and molecular docking study of N'-Arylidene imidazo [1,2-a] pyridine -2-carbohydrazide derivatives as novel Tyrosinase inhibitors
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A novel series of imidazo[1,2-a]pyridine 2-carbohudrazide derivatives bearing different arylidene pendantrs were designed, synthesized and evaluated for their inhibitory activity against mushroom Tyrosinase. It was found that compounds bearing 3-nitro (6j) and 4?hydroxy (6g) moieties on the arylidene pendant exhibited the best Tyrosinase inhibitory activity with IC50 values of 7.19 and 8.11 μM, respectively. These results were comparable to that of kojic acid as the reference drug (IC50 = 9.64±0.5 μM). Additionally, molecular docking analysis was performed to study the interactions and binding modes of compounds 6j, 6h and 6g which are showing the potential of two critical pi-pi interactions with His263 and Phe264 in the active site of Tyrosinase. The results indicated that 6j and 6g could be introduced as potent Tyrosinase inhibitors that might serve as promising candidates in medicine, cosmetics or food industry.
- Damghani, Tahereh,Edraki, Najmeh,Hadaegh, Saba,Khoshneviszadeh, Mehdi,Pirhadi, Somayeh,Sabet, Razieh,khoshneviszadeh, Mahsima
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- Upscaling Photoredox Cross-Coupling Reactions in Batch Using Immersion-Well Reactors
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Herein we describe a straightforward approach for the scale-up of photoredox cross-coupling reactions from milligram to multigram scale using immersion-well batch reactors with minimal reoptimization of the reaction conditions. This approach can be applied to both homogeneous and, more significantly, heterogeneous reaction mixtures. Furthermore, we have used an immersion-well side-loop reactor to perform a reaction on a 400 mmol scale (86 g of aryl bromide).
- Candish, Lisa,Collins, Karl D.,Grimm, Isabelle,Hauer, Simone T.,Lovis, Kai,Schulte, Tim,Wycich, Gina
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supporting information
p. 1185 - 1193
(2020/07/08)
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- Efficient Access to Imidazo[1,2- a] pyridines/pyrazines/pyrimidines via Catalyst-Free Annulation Reaction under Microwave Irradiation in Green Solvent
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An expeditious catalyst-free heteroannulation reaction for imidazo[1,2-a]pyridines/pyrimidines/pyrazines was developed in green solvent under microwave irradiation. Using H2O-IPA as the reaction medium, various substituted 2-aminopyridines/pyra
- Rao, R. Nishanth,Mm, Balamurali,Maiti, Barnali,Thakuria, Ranjit,Chanda, Kaushik
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supporting information
p. 164 - 171
(2018/03/21)
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- Synthesis and biological evaluation of curcumin inspired imidazo[1,2-a]pyridine analogues as tubulin polymerization inhibitors
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With an aim to develop new curcumin inspired analogues as potent anticancer agents, we synthesized a series of (1E,4E)-1-phenyl-5-(3-phenylimidazo[1,2-a]pyridin-2-yl)penta-1,4-dien-3-ones (12a–t) as tubulin polymerization inhibitors. An initial screening was carried out to evaluate their cytotoxic potential on a panel of six cancer cell lines namely, cervical (HeLa), gastric (HGC-27), lung (NCI-H460), prostate (DU-145 and PC-3) and breast (4T1), using MTT assay. Among the compounds tested, compounds 12e, 12r and 12t showed potent growth inhibition and 12t {(1E,4E)-1-(3-(3,4-difluorophenyl)imidazo[1,2-a]pyridin-2-yl)-5-(2,4,6-trimethoxyphenyl)penta-1,4-dien-3-one} being the most active member of the series inhibited the growth of all the tested cell lines with IC50 values varying from 1.7 – 2.97 μM. Moreover, 12t showed promising cytotoxicity on PC-3, HGC-27 and HeLa cell lines with IC50 values of 2.11 ± 0.27 μM, 2.21 ± 0.25 μM and 2.53 ± 0.01 μM respectively. The results from aqueous solubility test showed that compounds 12e and 12t have 1.7 and 2.8 times more aqueous solubility than curcumin. Interestingly, the most active compound 12t was found to be nearly 2 times more selective on PC-3 cells as well as safe on normal human prostate (RWPE-1) cells. In addition, compound 12t efficiently inhibited tubulin polymerization with IC50 value of 8.44 ± 0.13 μM and molecular modelling studies disclosed that 12t binds at the colchicine binding site of the tubulin. Cell cycle analysis revealed that 12t arrests PC-3 cells in G2/M phase in a dose dependant manner. Further, treatment of PC-3 cells with 12t showed typical apoptotic morphology, also led to the impairment of mitochondrial membrane potential (DΨm) and increased levels of reactive oxygen species (ROS). Altogether, the results from acridine orange/ethidium bromide (AO-EB) and DAPI staining studies, annexin V-FITC/propidium iodide staining assay, analysis of mitochondrial membrane potential (DΨm) and reactive oxygen species (ROS) levels undoubtedly demonstrated the induction of apoptosis in PC-3 cells by compound 12t.
- Ramya, P.V. Sri,Guntuku, Lalita,Angapelly, Srinivas,Digwal, Chander Singh,Lakshmi, Uppu Jaya,Sigalapalli, Dilep Kumar,Babu, Bathini Nagendra,Naidu,Kamal, Ahmed
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p. 216 - 231
(2017/11/27)
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- Process for synthesizing pharmaceutical intermediate ethyl imidazo[1, 2-A]pyridine-2-carboxylate
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The invention belongs to the field of pharmaceutical intermediates, and particularly relates to a process for synthesizing a pharmaceutical intermediate ethyl imidazo[1, 2-A]pyridine-2-carboxylate. The process provided by the invention comprises the following steps: firstly, mixing (2-oxo-1(2H)-pyridinyl)acetonitrile with ethyl formate at a low temperature for reaction; separating reactants generated in the reaction and then adding into ethanol; and adding potassium carbonate for reflux reaction to obtain a target product. The process provided by the invention has the advantages of simple operation, mild conditions, high yield, convenient purification, high product quality, good safety and less pollution.
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Paragraph 0021; 0023; 0024; 0025
(2018/07/30)
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- Inhibition of the Cysteine Protease Human Cathepsin L by Triazine Nitriles: Amide???Heteroarene π-Stacking Interactions and Chalcogen Bonding in the S3 Pocket
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We report an extensive “heteroarene scan” of triazine nitrile ligands of the cysteine protease human cathepsin L (hCatL) to investigate π-stacking on the peptide amide bond Gly67–Gly68 at the entrance of the S3 pocket. This heteroarene???peptide bond stacking was supported by a co-crystal structure of an imidazopyridine ligand with hCatL. Inhibitory constants (Ki) are strongly influenced by the diverse nature of the heterocycles and specific interactions with the local environment of the S3 pocket. Binding affinities vary by three orders of magnitude. All heteroaromatic ligands feature enhanced binding by comparison with hydrocarbon analogues. Predicted energetic contributions from the orientation of the local dipole moments of heteroarene and peptide bond could not be confirmed. Binding of benzothienyl (Ki=4 nm) and benzothiazolyl (Ki=17 nm) ligands was enhanced by intermolecular C?S???O=C interactions (chalcogen bonding) with the backbone C=O of Asn66 in the S3 pocket. The ligands were also tested for the related enzyme rhodesain.
- Giroud, Maude,Ivkovic, Jakov,Martignoni, Mara,Fleuti, Marianne,Trapp, Nils,Haap, Wolfgang,Kuglstatter, Andreas,Benz, J?rg,Kuhn, Bernd,Schirmeister, Tanja,Diederich, Fran?ois
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supporting information
p. 257 - 270
(2017/02/15)
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- The discovery of fluazaindolizine: A new product for the control of plant parasitic nematodes
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Fluazaindolizine is a new highly effective and selective product for the control of plant parasitic nematodes. Specificity for nematodes coupled with absence of activity against the target sites of commercial nematicides suggests that fluazaindolizine has a novel mode of action. The discovery, structure-activity development and biological properties for this new class of nematicides are presented.
- Lahm, George P.,Desaeger, Johan,Smith, Ben K.,Pahutski, Thomas F.,Rivera, Michel A.,Meloro, Tony,Kucharczyk, Roman,Lett, Renee M.,Daly, Anne,Smith, Brenton T.,Cordova, Daniel,Thoden, Tim,Wiles, John A.
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p. 1572 - 1575
(2017/03/17)
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- IAP BIR domain binding compounds
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A compound of Formula 1: (I) or salt thereof, as well as methods of making compounds of Formula 1, methods of using compounds of Formula 1 to treat proliferative disorders such as cancer, and related compounds, composition, and methods.
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- IMIDAZOPYRIDINE DERIVATIVES USEFUL IN TREATING DIABETES
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The present invention relates to imidazopyridine derivatives of the following general formula I: and to their use as a drug, in particular in treating and/or preventing diabetes, its complications and/or associated pathologies.
- -
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Paragraph 0204; 0205
(2015/07/15)
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- Discovery of imidazopyridine derivatives as highly potent respiratory syncytial virus fusion inhibitors
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A series of imidazolepyridine derivatives were designed and synthesized according to the established docking studies. The imidazopyridine derivatives were found to have good potency and physical-chemical properties. Several highly potent compounds such as 8ji, 8jl, and 8jm were identified with single nanomolar activities. The most potent compound 8jm showed an IC50 of 3 nM, lower microsome clearance and no CYP inhibition. The profile of 8jm appeared to be superior to BMS433771, and supported further optimization.
- Feng, Song,Hong, Di,Wang, Baoxia,Zheng, Xiufang,Miao, Kun,Wang, Lisha,Yun, Hongying,Gao, Lu,Zhao, Shuhai,Shen, Hong C.
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supporting information
p. 359 - 362
(2015/03/30)
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- General Method for the Preparation of Electron-Deficient Imidazo[1,2-a]pyridines and Related Heterocycles
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A new annulation method for the preparation of the imidazo[1,2-a]pyridine ring system under mild conditions is presented. Treatment of a 2-aminopyridine with a dimethylketal tosylate in acetonitrile at elevated temperature (80-140°C) in the presence of catalytic Sc(OTf)3 provides the imidazo[1,2-a]pyridine product in good yield. The annulation method is broadly applicable to electron-poor 2-aminopyridines and displays a complementary profile to the classic preparation of the imidazo[1,2-a]pyridine ring system by reaction of a bromoketone with electron-rich and -neutral substrates. The scope of the process and mechanistic considerations are discussed.
- McDonald, Ivar M.,Peese, Kevin M.
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supporting information
p. 6002 - 6005
(2016/01/09)
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- GLUCOSYLCERAMIDE SYNTHASE INHIBITORS FOR THE TREATMENT OF DISEASES
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Described herein are compounds of Formula I, methods of making such compounds, pharmaceutical compositions and medicaments containing such compounds, and methods of using such compounds to treat or prevent diseases or conditions associated with the enzyme glucosylceramide synthase (GCS).
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Paragraph 000820
(2015/04/15)
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- SUBSTITUTED PYRIDINE AND PYRAZINE BMI-1 INHIBITORS
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Amine substituted pyridine and pyrazine compounds and forms thereof that inhibit the function and reduce the level of B -cell specific Moloney murine leukemia virus integration site 1 (Bmi-1) protein and methods for their use to inhibit Bmi-1 function and reduce the level of Bmi-1 to treat a cancer mediated by Bmi-1 are described herein.
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Page/Page column 278
(2015/06/08)
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- Synthesis of novel imidazo[l,2-a]pyridines and evaluation of their antifungal activities
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New 2-(imidazo[1,2-a]pyridin-2-ylcarbonyl)-N-substituted hydrazinecarbothioamides (4a-j), N'-(3-substitu-ted-4-oxo-1,3-thiazolidin-2- ylidene)imidazo[1,2-a]pyridine-2-carbohydrazides (5a-f ), and N-(nonsubstituted/4-substitu-ted phenyl)-5-(imidazo[1,2-a]p
- Goektas, Fuesun,Cesur, Nesrin,Satana, Dilek,Uzun, Meltem
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p. 581 - 591
(2014/07/07)
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- Aerobic multicomponent tandem synthesis of 3-sulfenylimidazo[1,2-a] pyridines from ketones, 2-aminopyridines, and disulfides
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An aerobic CeCl3·7H2O/NaI-catalyzed C-H functionalization reaction was developed for the synthesis of 3-sulfenylimidazo[1,2-a]pyridines from easily available ketones, 2-aminopyridines, and disulfides without DMSO or peroxide as an ox
- Ge, Wenlei,Zhu, Xun,Wei, Yunyang
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supporting information
p. 6015 - 6020
(2013/09/24)
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- Effect of the lipophilic parameter (log P) on the anti-parasitic activity of imidazo[1,2-a]pyridine derivatives
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A number of imidazo[1,2-a]pyridine derivatives were selected and investigated in relation to antiparasitic (Trichomonas vaginalis) activity. After treatment with derivatives, biological activity was assessed by determination of the in vitro viability of c
- Lopez-Martinez, Margarita,Salgado-Zamora, Hector,Campos-Aldrete, Ma. Elena,Trujillo-Ferrara, Jose G.,Correa-Basurto, Jose,Mexica-Ochoa, Carlos
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scheme or table
p. 415 - 420
(2012/10/07)
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- HETEROARYL COMPOUNDS AND METHODS OF USE THEREOF
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Provided herein are heteroaryl compounds, methods of their synthesis, pharmaceutical compositions comprising the compounds, and methods of their use. In one embodiment, the compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, such as CNS disorders and metabolic disorders, including, but not limited to, e.g., neurological disorders, psychosis, schizophrenia, obesity, and diabetes.
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Page/Page column 49
(2012/07/27)
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- Identification of fused bicyclic heterocycles as potent and selective 5-HT2A receptor antagonists for the treatment of insomnia
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A series of fused bicyclic heterocycles was identified as potent and selective 5-HT2A receptor antagonists. Optimization of the series resulted in compounds that had improved PK properties, favorable CNS partitioning, good pharmacokinetic properties, and significant improvements on deep sleep (delta power) and sleep consolidation.
- Xiong, Yifeng,Ullman, Brett,Choi, Jin-Sun Karoline,Cherrier, Martin,Strah-Pleynet, Sonja,Decaire, Marc,Feichtinger, Konrad,Frazer, John M.,Yoon, Woo H.,Whelan, Kevin,Sanabria, Erin K.,Grottick, Andrew J.,Al-Shamma, Hussien,Semple, Graeme
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scheme or table
p. 1870 - 1873
(2012/04/17)
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- Direct arylation of imidazo[1,2-a ]pyridine at C-3 with aryl iodides, bromides, and triflates via copper(I)-catalyzed C-H bond functionalization
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A convenient method for the copper(I)-catalyzed arylation of substituted imidazo[1,2-a]pyridine has been developed. This method is applicable to a variety of aryl electrophiles, including bromides, iodides, and triflates. It represents the first general p
- Cao, Hua,Zhan, Haiying,Lin, Yuanguang,Lin, Xiulian,Du, Zuodong,Jiang, Huanfeng
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supporting information; experimental part
p. 1688 - 1691
(2012/06/18)
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- SUBSTITUTED HETEROARYL FUSED DERIVATIVES AS PI3K INHIBITORS
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The present invention provides fused derivatives of Formula (I) that modulate the activity of phosphoinositide 3-kinases (PI3Ks) and are useful in the treatment of diseases related to the activity of PBKs including, for example, inflammatory disorders, immune- based disorders, cancer, and other diseases.
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Page/Page column 50
(2011/07/07)
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- Tandem [8 + 2] cycloaddition-[2 + 6 + 2] dehydrogenation reactions involving imidazo[1,2- a ]pyridines and imidazo[1,2- a ]pyrimidines
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The reaction between benzynes and imidazo[1,2-a]pyridines (pyrimidines) to form benzo[a]imidazo[5,1,2-cd]indolizines and 2,3,9c-triazocyclopenta[j,k] fluorenes has been studied computationally and experimentally. It is found that these reactions take plac
- Aginagalde, Maialen,Vara, Yosu,Arrieta, Ana,Zangi, Ronen,Cebolla, Vicente L.,Delgado-Camon, Arantzazu,Cossio, Fernando P.
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supporting information; experimental part
p. 2776 - 2784
(2010/08/05)
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- NOVEL PIPERAZINE DERIVATIVES AS INHIBITORS OF STEAROYL-COA DESATURASE
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The present invention relates to piperazine derivatives that act as inhibitors of stearoyl-CoA desaturase. The invention also relates to methods of preparing the compounds, compositions containing the compounds, and to methods of treatment using the compounds.
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Page/Page column 31
(2010/07/04)
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- New opportunities with the Duff reaction
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(Chemical Equation Presented) The Duff reaction (HMTA, AcOH or TFA) was studied on substituted [6 + 5] heterocyclic compounds. This reaction provides a useful route to aldehydes for compounds bearing sensitive amide functions. It gives also access to tric
- Masurier, Nicolas,Moreau, Emmanuel,Lartigue, Claire,Gaumet, Vincent,Chezal, Jean-Michel,Heitz, Annie,Teulade, Jean-Claude,Chavignon, Olivier
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p. 5989 - 5992
(2008/12/21)
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- NOVEL FUSED IMIDAZOLE DERIVATIVE
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The present invention relates to a compound represented by the Formula [I]: Wherein: the A ring is a 5-membered aromatic heterocyclic group containing at least one hetero atom selected from a nitrogen atom, and the like; A1 and A2, are each a nitrogen atom, and the like; X2, X3, X4, and X5 are all carbon atoms, or alternatively any one of X2, X3, X4, and X5 is a nitrogen atom and the rest are all carbon atoms; R1 is a hydrogen atom, or the like; R2, R3, R4, and R5, are each a hydrogen atom, or the like; R6 and R6', are each a hydrogen atom, and the like; R7 is an aryl group and the like; and R8 is an amino group or a hydroxy group, or a pharmaceutically acceptable salt or ester thereof.
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Page/Page column 92
(2010/11/28)
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- Synthesis and phosphodiesterase 5 inhibitory activity of novel pyrido[1,2-e]purin-4(3H)-one derivatives
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Synthesis and primary SAR of a novel series of 2-phenylpyrido[1,2-e]purin- 4(3H)-one derivatives with piperazinyl sulfonamide substituents were described herein. As potential PDE5 inhibitors for erectile dysfunction (ED) treatment, representative compound
- Xia, Guangxin,Li, Jianfeng,Peng, Aiming,Lai, Shunan,Zhang, Shujun,Shen, Jingshan,Liu, Zhonghua,Chen, Xinjian,Ji, Ruyun
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p. 2790 - 2794
(2007/10/03)
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- Compounds
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This invention relates to nicotinamide derivatives of general formula (I): in which R1, Z and R2 have the meanings defined herein, and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of such derivatives.
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Page/Page column 27
(2008/06/13)
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- Nicotinamide derivatives useful as PDE4 inhibitors
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This invention relates to nicotinamide derivatives of general formula (I): in which R1, R2 and R3 have the meanings defined herein, and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of such derivatives.
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- INHIBITORS OF HISTONE DEACETYLASE
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The invention relates to the inhibition of histone deacetylase. The invention provides compounds and methods for inhibiting histone deacetylase enzymatic activity. The invention also provides compositions and methods for treating cell proliferative diseases and conditions.
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Page/Page column 248-249
(2010/02/11)
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- Aminoimidazo[1,2-a]pyridines: Regioselective synthesis of substituted imidazonaphthyridines, azacarbolines and cyclazines
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In order to study the regioselectivity of thermal cyclocondensation, aminoimidazo[1,2-a]pyridines (AIP) 5a-e were prepared, further converted into iminophosphoranes 7a-e, and ultimately converted regioselectively in angular annulated imidazonaphthyridines (IN) 8a, 10a, 11a, 12a or linear annulated dipyridoimidazole (DPI) 17a. From 2-substituted derivative 23, the peri annulated product 24a was obtained. The starting amines 5a-f reacted with aldehydes to yield regioselectively IN 8a-c, 10a-c, 11a-c, 12a,b, DPI 16a-e, 17a-d and TIBO like structures (±)-13 and 24a-c, as proved by X-ray analysis. The 1,2- or 1,4-addition between amines and α,β-unsaturated aldehydes concerning the pyridine and imidazole moieties is discussed in the light of these results.
- Chezal, Jean M,Moreau, Emmanuel,Chavignon, Olivier,Gaumet, Vincent,Métin, Jacques,Blache, Yves,Diez, Anna,Fradera, Xavier,Luque, Javier,Teulade, Jean C
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p. 295 - 307
(2007/10/03)
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- Synthesis of acyclo-C-nucleosides in the imidazo[1,2-a]pyridine and pyrimidine series as antiviral agents
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The synthesis and the antiviral activities of C-3 acyclic nucleoside analogues of imidazo[1,2-a]pyridine and pyrimidine are reported. From these compounds, 20, 21, 22, 23, 28, and 34 showed a specific activity against cytomegalovirus and/or varicella-zoster virus.
- Gueiffier, Alain,Lhassani, Mohammed,Elhakmaoui, Ahmed,Snoeck, Robert,Andrei, Graciela,Chavignon, Olivier,Teulade, Jean-Claude,Kerbal, Abdelali,Essassi, El Mokhtar,Debouzy, Jean-Claude,Witvrouw, Myriam,Blache, Yves,Balzarini, Jan,De Clercq, Erik,Chapat, Jean-Pierre
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p. 2856 - 2859
(2007/10/03)
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- Synthesis and antibacterial activity of some imidazo[1,2-a[pyrimidine derivatives
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A series of 75 imidazo[1,2-a]pyrimidine derivatives were synthesized. The 'in vitro' antibacterial activity of these compounds and their corresponding α-bromoketones against a variety of gram (+), gram (-) bacteria and Mycobacterium species is reported. Some of the prepared derivatives exhibited potent antimicrobial activity.
- Rival,Grassy,Michel
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p. 1170 - 1176
(2007/10/02)
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- Synthesis and oral antiallergic activity of carboxylic acids derived from imidazo[2,1-c][1,4]benzoxazines, imidazo[1,2-a]quinolines, imidazo[1,2-a]quinoxalines, imidazo[1,2-a]quinoxalinones, pyrrolo[1,2-a]quinoxalinones, pyrrolo[2,3-a]quinoxalinones, and
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4H-Imidazo[2,1-c][1,4]benzoxazine-1-carboxylic acid (3) was found to possess potent activity in the IgE-induced rat passive cutaneous anaphylaxis model which may be predictive of clinical antiallergic activity. Compared to disodium cromoglycate (DSCG,1),
- Ager,Barnes,Danswan,Hairsine,Kay,Kennewell,Matharu,Miller,Robson,Rowlands,Tully,Westwood
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p. 1098 - 1115
(2007/10/02)
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