Untreated Psychopathology of Candidates to "Normal Volunteers

Arkivoc, 2008

In the present investigation ethyl 2-(4-carboxyphenylazo)acetoacetate 1 on condensation with various aromatic aldehydes in ethanolic NaOH solution yielded the corresponding chalcones 2a-j. These chalcones were further reacted with urea in the presence of base in ethanol, which led to the formation of pyrimidine derivatives 3a-j. The newly synthesized heterocyles were characterized on the basis of their chemical properties and spectroscopic data. All newly synthesized compounds were evaluated for their antimycobacterial activities against Mycobacterium tuberculosis H 37 Rv.

2015

In the present investigation m-phenoxybenzaldehyde on condensation with various aromatic acetophenone in methanol and 40% aqueous solution of KOH has yielded the corresponding chalcones 4a-h. These chalcones have been further reacted with guanidine hydrochloride, thiourea and urea in the presence of alcoholic KOH, which has led to the formation of pyrimidine derivatives 5a-h to 7a-h. The newly synthesized heterocycles have been characterized on the basis of their chemical properties and spectroscopic data. All novel synthesized derivatives have been screened for their antimycobacterial activities against Mycobacterium tuberculosis H37Rv.

2016

In the present study, three new combinatorial libraries of substituted phenyl pyrazoline 5a-e, isoxazole 6a-e and 1,5benzodiazepine 7a-e derivatives have been synthesised via the reaction of chalcone 4a-e with phenylhydrazine hydrochloride, hydroxylamine hydrochloride and o-phenylenediamine respectively. The structures of all the newly synthesised compounds have been assigned on the basis of FTIR, H and C NMR, LC-MS, and elemental analysis. The title compounds have been screened for their preliminary in vitro antimicrobial activity against a panel of pathogenic strains S. aureus, S. pyogenus, E. coli, P. aeruginosa, C. albicans, A. niger and A. calavatus. Most of the compounds show appreciable antimicrobial activity against the tested strains. Compounds 8b, 8c, 9b, 9d, and 9f are considered as the best desired bioactive antimicrobial analogues of the series. In vitro antimycobacterial activity for all the synthesised compounds has been carried out against Mycobacterium tuberculosis ...

Chalcones are 1,3-diphenyl-2-propene-1-one, in which two aromatic rings are linked by a three carbon -unsaturated carbonyl system. Pyrimidines are one of the important heterocyclic compounds with various biological activites. In this view, it was proposed to synthesize some novel pyrimidines from chalcones. Chalcones are prepared by treating 4-imidazole-1-yl-acetophenone with different aromatic aldehydes. These chalcones on condensation with guanidine HCl and KOH gave 4-(4-(1H –imidazole-l-yl)-pyrimidin-2-amine derivatives. They have been screened for their antibacterial activity against Gram positive bacteria B.subtillis & B.pumilus and gram negative bacteria E.coli & P.vulgaris and antifungal activity against

composed of two nitrogen atoms at position 1 and 3. Pyrimidines have been subjected to a large number of different modifications to obtain derivatives having different biological properties. Several groups have studied the chemistry and pharmacological properties of pyrimidine derivatives. [19-24] MATERIALS AND METHODS Chemicals In the present study, all chemicals have been provided from (Merck group, BDH and Fluke Company, Germany). Laboratory Devices In this study, the Fourier-transform infrared (FT-IR) spectroscopy provided from (Bruker\OPUS_7.5.1.8, Germany) was used to characterize all derivative compounds. Synthesis Method General procedure [25] Acetophenone (0.01 mol) and aromatic aldehydes (0.01 mol) have been taken in equal amounts, were ABSTRACT Objectives: This research involves synthesis of some chalcones derivatives from Acetophenone as starting material. Methods: The derivatives of chalcone compounds [Ch 1-Ch 4 ] has been prepared by reaction benzaldehyde derivatives like [4-chlorobenzaldehyde, 4-bromobenzaldehyde, 2-hydroxy1-naphthaldehyde. 3-hydroxybenzaldehyde] with acetophenone. the compound [Ch 1 ,Ch 2 and Ch 4 ] enter reaction with urea ,thiouria and guanidine to product pyrimidine derivatives. These compounds [Ch 1-Ch 4 ] has been characterized by melting points, [FT.IR] spectroscopy, H 1 NMR spectroscopy and thin layer chromatography technique (TLC) has been used for reactions steps and sequence by using solvent [benzene: methanol, 4:1]. Antibacterial activity test of three derivative compounds (Ch 1 a, Ch 2 b and Ch 4 c) were done against two multi-drug resistance pathogenic bacteria isolated from patients infected with burn infection. Results: The results proved that Ch 4 c compound with concentration 200 mg/ml provided best antibacterial activity with inhibition zone diameter 22.62 ± 0.1551 mm and 24 mm against staphylococcus aureus and pseudomonas aeruginosa, respectively.

Medicinal Chemistry Research, 2012

In this study, novel series of chalcone derivatives, namely, 4-[4-(3-phenyl-acryloyl)-phenylamino]-chromen-2one (5a-k) have been synthesized from the intermediate 4-(4acetyl-phenylamino)-chromen-2-one (4). Cyclization reaction of chalcone (5a-k) with hydrazine hydrate, guanidine nitrate, and malononitrile gives the corresponding 4-[4-(1acetyl-5-phenyl-4,5-dihydro-1H-pyrazol-3-yl)-phenylamino]-chromen-2-one (6a-k), 4-[4-(2-amino-6-phenyl-pyrimidin-4-yl)-phenylamino]-chromen-2-one (7a-k), and 2-amino-6-[4-(2-oxo-2H-chromen-4-ylamino)-phenyl]-4phenyl-nicotinonitrile (8a-k) derivatives were synthesized. The newly synthesized compounds were evaluated for their antimycobacterial activity and antimicrobial activity against eight bacteria (S. aureus, B. cereus, E. coli, P. aeruginosa, K. pneumoniae, S. typhi, P. vulgaris, and S. flexneri) and four fungi (A. niger, C. albicans, A. fumigatus, and A. clavatus).

Asian Journal of Chemistry

Twenty novel pyrimidine derivatives were synthesized from 2,5-dichloro-3-acetylthienyl chalcones by reacting with guanidine HCl in presence of KOH and ethanol under reflux for 6 h. Their structural characterizations were evaluated by ATR-FTIR, 1H NMR, 13C NMR, mass spectroscopy. They were also screened for antifungal, antitubercular and cytotoxicity activities. They were displayed good antifungal activity (MIC = 32-125 μg/mL) against Aspergillus niger and Candida tropicalis fungal species except compound 15 with 4"-pyridinyl moiety (MIC = 8.00 μg/mL) being more potent. Compound 5 with 2",4"-dichlorophenyl moiety was shown with good antitubercular activity (MIC = 6.2 μg/mL) against Mycobacterium tuberculosis H37Rv (MTB) stain. They have also tested for in vitro cytotoxicity activity against DU-145 prostate cancer cell lines. In which the compound 15 with 4"-pyridinyl moiety (IC50 = 2.0 ± 0.1 μg/mL) and compound 17 with 2"-pyrrolyl moiety (IC50 = 6.0 ± 0.1 μg/...

2020

In the present study, a series of pyrazolines 2a-c, isoxazoline 5, pyrimidines 3aʹ-cʹ and benzoazepines 4aʹʹ-cʹʹ have been prepared from the cyclization reactions of biphenyl chalcone 1 with appropriate binucleophilic reagents. The chalcone 1 has been obtained by using the Claisen-Schmidt condensation reaction of 2-hydroxyacetophenone with biphenyl-4carboxaldehyde in EtOH/NaOH medium. The structural interpretations of the chalcone 1 and final heterocycles have been fully ascribed on the basis of their different spectroscopic parameters such as IR, 1 H and 13 C NMR, and ESI-MS. The in vitro antimicrobial evaluation of these heterocycles have also been carried out by using serial tube dilution technique against the selected number of bacterial and fungal strains and most of the studied products proved to be the potent antimicrobial agents. The newly prepared pyrazolines and isoxazoline exhibit noticeable antimicrobial properties.

Bioorganic & Medicinal Chemistry Letters, 2006

A series of amino-5-[(substituted) phenyl]-3-(4-hydroxy-3-methylphenyl)-4,5-dihydro-1H-1-pyrazolylmethanethione were synthesized by the reaction between thiosemicarbazide and chalcones and were tested for their antimycobacterial activity in vitro against Mycobacterium tuberculosis H 37 R v and INH resistant Mycobacterium tuberculosis using bactec method. Among the synthesized compounds, compound (4b), amino-5-(4-chlorophenyl)-3-(4-hydroxy-3-methylphenyl)-4,5-dihydro-1H-1-pyrazolylmethanethione was found to be the most active agent against Mycobacterium tuberculosis H37 Rv (MTB) and INH resistant Mycobacterium tuberculosis (INHR-MTB) with minimum inhibitory concentration of 0.43 µM . When compared to INH-compound (4b) was found to be 1.62 fold and 26.41 fold more active against MTB and INHR-MTB, respectively.

One of the most important classes of organic compounds present in nature or synthesized in the laboratory is heterocyclic systems. In the treatment of commonly occurring diseases and biological activities these compounds possess an array. Literature survey revealed that Chalcones and Pyrimidines possess a broad spectrum of biological activities like anti-inflamm atory, anti-malarial, antimicrobial, anti-depressant, anti-histamine, anti-tubercular and anti-cancer. This research is an endeavor in this direction of synthesis and characterization of such compounds based on Elemental analysis, IR, 1 H NMR and Mass spectroscopy. The pharmacological and anti-bacterial screening of synthesized compounds has also been included. To access many heterocyclic systems containing Nitrogen and Oxygen, chalcones afford a facile route. Hence an attempt is made to synthesize chalcones by the Claisen – Schmidt condensation from 4-Imidazolyl acetophenone with two substituted aromatic aldehydes. After purification and characterization by physical and spectral methods, the resulting chalcones have been converted successfully into Pyrimidines by treatment with Guanidine hydrochloride. Based on the reported literatureby physical and spectral methods the resultant compounds were identified also screened for antibacterial activity.