Synthesis and Antimicrobial Activity of 3-Hydroxy- and 3-Arylamino-5-aryl-4-acyl-1-(pyridyl)-3-pyrrolin-2-ones

Pharmaceutical Chemistry Journal -     

Synthesis and Antimicrobial Activity of 5-Aryl-4-acyl-1-(N,N-dimethylaminoethyl)-3-hydroxy-3-pyrrolin-2-ones

Pharmaceutical Chemistry Journal -     

Synthesis and Antimicrobial Activities of Some New Azetidin-2-ones and Thiazolidin-4-ones

Various (4-substituted) phenyl-3-β-[(N-benzenesulphonyl/tosyl)-4-(un)substituted anilino]propionylamido-1,3-thiazolidine-4-ones (3a-x) and 1-β-[(N-benzenesulphonyl/tosyl)-4-(un)substituted anilino]-propionylamido-3-chloro-4-(4-substituted)phenyl-azetidin-2-ones (4a-x) have been synthesised by the cyclocondensation of Schiff bases (2a-x) with thioglycolic acid and chloroacetyl chloride, respectively. The structures of the newly synthesised compounds have been established on the basis of their spectral data and elemental analysis. All compounds were evaluated for antimicrobial activities against Escherichia coli, Bacillus cirroflagellosus, Aspergillus niger and Colletotrichum capsici. Most compounds investigated exhibited significant antifungal activity against Colletotrichum capsici, comparable to that of fluconazole, the standard used.     

Synthesis and Antimicrobial Activity of Some New 2-(3-(4-Aryl)-1-phenyl-1H-pyrazol-4-yl) Chroman-4-ones

Seven new 2-(3-(4-aryl)-1-phenyl-1H-pyrazol-4-yl) chroman-4-ones (4a-4g) have been synthesized by cyclization of 2-hydroxychalcone analogues of pyrazole 3a-3g using conc. HCl in acetic acid. The structures of the compounds 4a-4g were established by the combined use of (1)HNMR, IR and mass spectra. All the seven compounds were tested in vitro for their antibacterial activity against two Gram positive bacteria namely Staphylococcus aureus and Bacillus subtilis and two Gram negative bacteria Escherichia coli and Pseudomonas aeruginosa. The compounds 4b, 4c, 4e, 4f, 4g have displayed good antibacterial activity when compared with commercially available antibiotic, ciprofloxacin. These compounds also were screened for their antifungal activity against two ear pathogenic fungi, namely Aspergillus Niger and A. flavus. The compounds 4a, 4c, 4d, 4g exhibited good antifungal activity when compared with commercially available antifungal, fluconazole.     

Synthesis and Antiinflammatory and Analgesic Activity of 1-(2-aminoethyl)-5-aryl-4-acyl-3-hydroxy-3-pyrrolin-2-ones

4,5-Disubstituted 1-(2-aminoethyl)-3-hydroxy-3-pyrrolin-2-ones have been synthesized via reactions of acylpyruvic acid methyl esters with a mixture of an aromatic aldehyde and ethylenediamine. Some of the synthesized compounds display pronounced antiinflammatory and analgesic activity at a relatively low toxicity. __________ Translated from Khimiko-Farmatsevticheskii Zhurnal, Vol. 39, No. 9, pp. 33 – 36, September, 2005.     

Synthesis and antimicrobial activity of 1-(4-hydroxyphenyl)-4-acyl-5-aryl-3-hydroxy-3-pyrrolin-2-ones

The reaction of methyl esters of acylpyruvic acids, 4-aminophenols, and aromatic aldehydes leads to the formation of 1-(4-hydroxyphenyl)-4-acyl-5-aryl-3-hydroxy-3-pyrrolin-2-ones. The proposed structures of the synthesized compounds were confirmed by IR and PMR spectroscopy. The antibacterial activity of some of the newly synthesized compounds was studied.     

Synthesis and Antimicrobial Activity of 4-(4-Acetylphenyl)-3-Hydroxy-2H-Chromen-2-One Derivatives

Pharmaceutical Chemistry Journal - Reactions of 4-(4-bromoacetylphenyl)-3-hydroxy-2H-chromen-2-one with Py, 4-methylpyridine, quinoline, and benzo[f]quinoline produced quaternary salts; with...     

Synthesis and biological activity of 4-acyl-5-aryl-3-hydroxy-1-(2-hydroxyethylaminoethyl)-3-pyrrolin-2-ones

A series of 4-acyl-5-aryl-3-hydroxy-1-(2-hydroxyethylaminoethyl)-3-pyrrolin-2-ones (I) and their hydrochlorides (II) were synthesized via reactions of methyl esters of acylpyruvic acids with a mixture of aromatic aldehyde and N-hydroxyethylethylenediamine. The antibacterial activity of compounds I and the influence of compounds I and II on blood coagulation were studied. All compounds demonstrate pronounced anticoagulant or hemostatic action. __________ Translated from Khimiko-Farmatsevticheskii Zhurnal, Vol. 41, No. 9, pp. 22–25, September, 2007.     

Synthesis and CNS Activity of N,N-Disubstituted 1-(Aminomethyl)-5-alkyl-3-(aryloxyacetylhydrazono)indolin-2-ones

Isatin and 5-methylisatin were condensed with various aryloxyacetylhydrazides to furnish the 3-(aryloxyacetylhydrazono)-5-alkylindolin-2-ones 1–4 . When 1–4 were subjected to Mannich reaction, the N,N-disubstituted 1-(aminomethyl)-5-alkyl-3-(aryloxyacetylhydrazono)indolin-2-ones 5–8 were obtained. The compounds were CNS active and relatively non-toxic (albino mice).     

Synthesis and Pharmacological Evaluation of Azetidin-2-ones and Thiazolidin-4-ones Encompassing Benzothiazole

Various 7-chloro-6-fluoro-2-arylidenylaminobenzo(1,3)thiazole (2a-h) have been synthesized by the condensation of 7-chloro-6-fluoro-2-aminobenzo(1,3)thiazole (1) with different aromatic aldehydes. The Schiff's bases on reaction with acetyl chloride, chloroacetyl chloride and phenyl acetyl chloride yielded 1-(7-chloro-6-fluorobenzothiazol-2-yl)-3,4-substituted-aryl-azetidin-2-ones (3a-x). Similarly, cyclization of Schiff's base with thioglycolic acid furnished 3-(7-chloro-6-fluoro-benzothiazol-2-yl)-2-substituted-arylthiazolidin-4-ones (4a-h). The structures of the newly synthesized compounds have been established on the basis of their spectral data and elemental analysis. Some selected compounds were evaluated for antiinflammatory, analgesic, CNS depressant and skeletal muscle relaxant activity.     

Synthesis and Antimicrobial Activity of 2-(4-Halophenyl)-2-(oxyaryl)propanes

Pharmaceutical Chemistry Journal -     

Synthesis and antileukemic activity of new 3-(1-phenyl-3-methylpyrazol-5-yl)-2-styrylquinazolin-4(3H)-ones

3-(1-Phenyl-3-methylpyrazol-5-yl)-2-styrylquinazolin-4(3H)-ones 14a-q and 15a-q were synthesized by refluxing in acetic acid the corresponding 2-methylquinazolinones 12 and 13 with the opportune benzoic aldehyde for 12 h. The synthesized styrylquinazolinones 14a-q and 15a-q were tested in vitro for their antileukemic activity against L1210 (murine leukemia), K562 (human chronic myelogenous leukemia) and HL60 (human leukemia) cell lines showing in some cases good activity.