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Substituted Phenyl (substituted + phenyl)

Distribution by Scientific Domains

Chemistry	87%

Selected Abstracts

Synthesis and Antibacterial Activity of a New Series of 3-[3-(Substituted Phenyl)-1-Isonicotinoyl-1H -Pyrazol-5-yl]-2H -Chromen-2-one Derivatives

ARCHIV DER PHARMAZIE, Issue 6 2009
Prashant Aragade
Abstract A novel series of 3-[3-(substituted phenyl)-1-isonicotinoyl-1H -pyrazol-5-yl]-2H -chromen-2-one derivatives 4a,k have been synthesized by the reaction of 3-[2,3-dibromo-3-(substituted phenyl) propanoyl]-2H -chromen-2-one 3a,k and isonicotinic acid hydrazide in the presence of triethylamine in absolute ethanol, characterized by spectral data and screened for their in-vitro antibacterial activity against Gram-positive and Gram-negative bacteria. Among the series, compounds 4e, 4i, and 4k displayed an encouraging antibacterial activity profile as compared to the reference drug ampicillin against tested bacterial strains. [source]

ChemInform Abstract: New Novel Synthesis and Antibacterial Activity of 1-(Substituted phenyl)-2-phenyl-4- (3,-halo-4,-hydroxy-5,-methoxybenzylidene)-imidazol-5-ones.

CHEMINFORM, Issue 16 2002
S. A. Siddiqui
Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a "Full Text" option. The original article is trackable via the "References" option. [source]

Highly Efficient Pd/C-Catalyzed Suzuki Coupling Reaction of p -(un)Substituted Phenyl Halide with (p -Substituted phenyl) Boronic Acid

CHINESE JOURNAL OF CHEMISTRY, Issue 8 2007
Ming-Gang Hu
Abstract A highly efficient Pd/C-catalyzed ligandless, heterogeneous Suzuki reaction of p -(un)substituted phenyl halide with (p -substituted phenyl)boronic acid in DMF/H2O solvent in a short reaction time (0.5 h) at 75 °C was developed. The key for such a catalytic system was the addition of 1 equivalent of tetrabutylammonium bromide. A wide variety of substituents can be tolerated and high yields of cross coupling products were achieved. The palladium catalyst can be easily recovered and reused without significantly decreasing its efficiency. [source]

Synthesis of novel thiazole and pyrrolothiadiazine derivatives from aldehyde thiosemicarbazones

HETEROATOM CHEMISTRY, Issue 4 2006
Mohsen A.-M.
Substituted thiosemicarbazones 7a,e reacted with ethenetetracarbonitrile (TCNE) in ethyl acetate with formation of 5-amino-3-(substituted ben-zylidene-amino)-2-phenylimino-2,3-dihydrothiazole-4-carbonitrile 8a,e 2-amino-6-phenyl-imino-1,6- dihydropyrrolo[1,3,4]thiadiazine-3-carbonitrile 9, and phenyl-(5-{substituted phenyl}-3H-[1,3,4]thiadiazole-2-ylidene)amines 10a,e. Rationales for the observed conversations are presented. © 2006 Wiley Periodicals, Inc. Heteroatom Chem 17:261,266, 2006; Published online in Wiley InterScience (www.interscience.wiley.com). DOI 10.1002/hc.20198 [source]

New synthetic route towards 2,2-dimethylchromene and synthesis of substituted 7-(dimethylpropargyl)chromene

JOURNAL OF HETEROCYCLIC CHEMISTRY, Issue 3 2008
Babak H. Alizadeh
Trifluoromethansufonic acid (TFA) was found a proper reagent for regioselectively ring closure of resorcinol to afford 7-hydroxy-2,2-dimethyl-2,3-dihydrochromen-4-one 3. The propargylation of 3 gave rise to 2,2-dimethyl-7-(2-methylbut-3-yn-2-yloxy)-2,3-dihydrochromen-4-one 4. Condensation of 4 with substituted phenyl or benzyl Grignard reagents afforded substituted phenyl or benzylidene chromenes 6a-d and 4-(substitutedbenzylidene)-3,4-dihydro chromenes 8a-e, respectively. [source]

1,1-bis(3,-indolyl)-1-(p- substituted phenyl)methanes decrease mitochondrial membrane potential and induce apoptosis in endometrial and other cancer cell lines

MOLECULAR CARCINOGENESIS, Issue 7 2008
Jun Hong
Abstract 1,1-Bis(3,-indolyl)-1-(p -substituted phenyl)methanes, containing p-t- butyl (DIM-C-pPhtBu) and phenyl (DIM-C-pPhC6H5) substituents, are peroxisome proliferator-activated receptor , (PPAR,) agonists; however, DIM-C-pPhtBu-induced growth inhibition and cell death in human HEC1A endometrial cancer cells is PPAR,-independent. DIM-C-pPhtBu decreased mitochondrial membrane potential (MMP) and promoted the release of cytochrome c and caspase activation and nuclear uptake of endonuclease G leading to apoptosis of HEC1A cells. DIM-C-pPhtBu specifically targeted the mitochondrial permeability transition pore complex (PTPC) because the DIM-C-pPhtBu-induced pro-apoptotic responses were inhibited by atractyloside (Atra), a compound that specifically interacts with the inner mitochondrial membrane adenine nucleotide transport (ANT) proteins. At the dose of Atra used in this study (300 µM), this compound alone did not alter the PTPC but inhibited the mitochondriotoxic effects of DIM-C-pPhtBu. DIM-C-pPhtBu/DIM-C-pPhC6H5 and Atra also differentially affected the ability of eosin-5-maleimide (EMA) to alkylate Cys160 in the ANT protein and Atra, but not DIM-C-pPhtBu, inhibited the exchange of ATP/ADP in isolated mitochondria suggesting that these pharmacophores act on different sites on the ANT protein. Results of this study show that the receptor-independent proapoptotic activity of DIM-C-pPhtBu and DIM-C-pPhC6H5 were related to novel mitochondriotoxic activities involving inner mitochondrial ANT proteins. © 2007 Wiley-Liss, Inc. [source]

CP-MLR/PLS Directed Structure-Activity Modeling of the HIV-1 RT Inhibitory Activity of 2,3-Diaryl-1,3-thiazolidin-4-ones

MOLECULAR INFORMATICS, Issue 4 2004
Yenamandra
Abstract A detailed structure-activity relationship study of the HIV-1 Reverse Transcriptase (RT) inhibitory activity of two series of compounds, 2-(2,6-dihalo phenyl)-3-(substituted pyridin-2-yl)-thiazolidin-4-ones and 2-(2,6-Dihalophenyl)-3-(substituted phenyl)-thiazolidin-4-ones, belonging to 2,3-diaryl-thiazolidin-4-ones in terms of physicochemical and structural descriptors have been carried out using combinatorial protocol interfaced multiple linear regression (CP-MLR) and partial least squares (PLS) analysis. The models developed in the study indicate a preference for hydrophobic compounds for better inhibitory activity. Also, a positive regression coefficient of I2,3, an indicator descriptor meant for the joint disposition of substituents of 2,3-diaryl moieties of thiazolidinones to address their ability in taking a butterfly like conformation, is in agreement with all earlier observations that compounds having the ability to take butterfly like conformation will be showing better inhibitory activity. The identified models suggest that the meta-positions of 3-aryl moiety has the ability to accommodate hydrophobic/ steric groups. The replacement of C2, of 3-phenyl by nitrogen resulted in 3-pyridyl variants of these analogues. Even though from geometry point of view, the phenyls and pyridyls span almost the same structural space and steric features, presence of nitrogen in pyridyls gave them a blend of polarity, electronic features and a different hydrophobicity profile when compared to corresponding phenyl analogue. Furthermore the PLS models, developed from those descriptors took part in CP-MLR models, indicate that most of the descriptors have almost equal influence in accounting for the variation in the activity of these compounds. This suggests that the factors responsible for the variation in the activity have been uniformly distributed across the varying centers of the molecule. The study suggests that thiazolidinones with 3-(pyridin-2-yl) moiety provide scope for further substituent variation to modulate the HIV-1 RT inhibitory activity. [source]

Ortho Effects in Quantitative Structure Activity Relationships for Lipase Inhibition by Aryl Carbamates

MOLECULAR INFORMATICS, Issue 8 2003
Gialih Lin
Abstract Ortho -substituted phenyl- N -butyl carbamates (1,11) are synthesized and evaluated for their inhibition effects on Pseudomonas species lipase. Carbamates 1,11 are characterized as pseudo-substrate inhibitors of the enzyme. The logarithms of dissociation constant (Ki), carbamylation constant (k2), and bimolecular inhibition constant (ki) multiply linearly correlate with Hammett substituent constant (,), Taft-Kutter-Hansch ortho steric constant (ES), and Swan-Lupton field constant (F). For ,logKi -, logk2 -, and logki -correlations, values of ,, ,, f, ,XR are 0.2, ,0.06, ,1.7, 0.8; 0.0, 0.0, 1.0, ,0.07; and ,1.8, 7, 0.6, 5; respectively. The enzyme inhibition mechanism is composed of four steps: 1) the first step which is protonation of carbamates 1,11, 2) the second step (Ki1) which involves in the proton 1,3-shift of protonated carbamates 1,11 then the pseudo- trans to cis conformational change, 3) the third step (Ki2) which is formation of a negative charged enzyme-inhibitor tetrahedral intermediate, and 4) the fourth step (k2) which is the carbamylation step. The former three steps are likely composed of the Ki step. There is little ortho steric enhancement effect in the Ki step. From cross-interaction correlations, distance between carbamate and phenyl substituents in transition state for the Ki step is relatively short due to a large ,XR value of 7. The k2 step is insensitive to ortho steric effect. The k2 step involves in departure of leaving group, substituted phenol in which is protonated from the proton 1,3-shift but not from the active site histidine of the enzyme. From cross-interaction correlations, the distance between carbamate and phenyl substituents in transition state for the k2 step is relatively long due to a small ,XR value of 0.6. [source]

Benzothiazole Incorporated Barbituric Acid Derivatives: Synthesis and Anticonvulsant Screening

ARCHIV DER PHARMAZIE, Issue 8 2009
Nadeem Siddiqui
Abstract A series of 1-(6-substituted-1,3-benzothiazol-2-yl)-3-(substituted phenyl)hexahydro-2,4,6-pyrimidinetriones 4a,t were synthesized starting from substituted anilines. These compounds contained two active anticonvulsant pharmacophores, benzothiazole and barbituric acid. Structures of the compounds were confirmed on the basis of different spectroscopic techniques. All the compounds were evaluated for their anticonvulsant activity. Three compounds 4c, 4d, and 4s showed promising anticonvulsant activities in Maximal Electroshock Seizure test (MES) and subcutaneous pentylenetetrazole test (scPTZ). They also displayed a wide safety profile when tested for the minimal motor impairment test. [source]

Synthesis and Antibacterial Activity of a New Series of 3-[3-(Substituted Phenyl)-1-Isonicotinoyl-1H -Pyrazol-5-yl]-2H -Chromen-2-one Derivatives

ChemInform Abstract: Novel Acyl Coenzyme A: Diacylglycerol Acyltransferase 1 Inhibitors , Synthesis and Biological Activities of N-(Substituted heteroaryl)-4-(substituted phenyl)-4-oxobutanamides.

CHEMINFORM, Issue 43 2010
Yoshihisa Nakada
Abstract A series of novel N-(substituted hetaryl)-4-aryl-4-oxobutanamides are designed, synthesis and evaluated for their activity against DGAT-1 enzyme. [source]

ChemInform Abstract: Synthesis of 14-{[(Un)substituted phenyl] or alkyl}-14-H-dibenzo[a,j]xanthenes Using Yb(OTf)3 as an Efficient Catalyst under Solvent-Free Conditions.

CHEMINFORM, Issue 39 2008
Li-Min Wang
Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a "Full Text" option. The original article is trackable via the "References" option. [source]

Synthesis of Some Novel 5,6-Dihydro-6-[4,-substituted phenyl]-12H-indeno[2,1-c]-1, 5-benzodiazepin-7-ones.

CHEMINFORM, Issue 39 2006
Preeti Aggarwal
Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract, please click on HTML or PDF. [source]

Highly Efficient Pd/C-Catalyzed Suzuki Coupling Reaction of p -(un)Substituted Phenyl Halide with (p -Substituted phenyl) Boronic Acid

Simple Approach to the Highly Stereoselective Synthesis of trans -1,2-Cyclopropane Derivatives

CHINESE JOURNAL OF CHEMISTRY, Issue 8 2007
Hui Zhang
Abstract In the presence of KF·2H2O, furoylmethyltriphenylarsonium bromide (1a) or thienoylmethyltriphenylarsonium bromide (1b) reacted with 2-[(un)substituted benzylidene]malononitrile (2) in chloroform at room temperature to give trans -3,3-dicyano-1-furoyl-2-[(un)substituted phenyl]cyclopropane (3a) or trans -3,3-dicyano-1-thienoyl-2-[(un)substituted phenyl]cyclopropane (3b) respectively in good yield with high stereoselectivity. The structures of product 3 were confirmed by IR, MS, 1H NMR, 1H- 1H COSY and microanalysis. The relative configuration of product 3 was determined by 1H- 1H NOESY technique. The mechanism for the formation of product 3 was also proposed. [source]