• Archives of Pharmacal Research
• /
• v.15 no.1
• /
• pp.104-108
• /
• 1992

2, 3-Diphenyl-6-formyl-5-methoxyindole reacts with ethyl cyano acetate to yield the arylidene derivative which forms with urea and thiourea the corresponding pyrimidine derivatives. The arylidene derivatives react with hydrazines and with active methylenes to form the respective pyrazole derivatives and the $\alpha, \;\beta$-disubstituted acrylonitriles. Seven new compounds were tested for their effects on the arterial blood pressure of rats and analgesic activity.

• Bulletin of the Korean Chemical Society
• /
• v.31 no.5
• /
• pp.1135-1142
• /
• 2010

A series of N(2)-benzothiazolyl substituted tetrahydroindazoles has been synthesized via cyclic ${\beta}$ keto esters. Optimum reaction condition was found as acidic toluene and effect of higher acidity towards substituted hydrazines in situ was described. Synthesized compounds have been achieved as single isomer and characterized by using 1D and 2D NMR spectral reports. Antimicrobial screening was carried out for the synthesized compounds along with a series of N(2)-pyridyl tetrahydroindazoles.1 The results of the in vitro antimicrobial screening studies revealed that compounds 13, 16 against Staphylococcus aureus, 11 against Escherichia coli, 10-12, 16 against Pseudomonas aeruginosa and 12 against Klebsiella pneumoniae recorded almost two-fold better activity compared to the standard drug used.

• Bulletin of the Korean Chemical Society
• /
• v.32 no.11
• /
• pp.3914-3922
• /
• 2011

3-Chloro-1-benzothiophene-2-carbonyl chloride 1 was reacted with glycine in acetone to give 3-chloro-1-benzothiophen-2-yl-carbonylaminoacetic acid 2. Various aldehydes on treatment with compound 2 in acetic anhydride to gave 1,3-oxazol-5-ones 3a-d. These oxazolones was treated with aromatic amines or hydrazides to get various imidazol-4-ones 4a-t or 5a-l. Oxazolones 3a-d was also treated with aromatic hydrazines, expansion of five member oxazole ring to six member triazine ring occurs to yield 1,2,4-triazin-6-ones 6a-h. The structures of all the synthesized compounds were confirmed by spectral data and had been screened for antibacterial activity.

• Archives of Pharmacal Research
• /
• v.27 no.9
• /
• pp.885-892
• /
• 2004

Due to the rapidly growing number of resistant strains of bacteria, the search for antibacterial agents with new modes of action will always remain an important and challenging task. Thus, the reaction of 2-substituted or. unsubstituted-4-(4-acetylanilino)-5,6,7,8-terahydrobenzo［b］ thieno［2,3-d］pyrimidine derivatives 1-3 with the hydrazine derivatives, semi and / or thiosemi-carbazides, provided the corresponding hydrazones 4-6 and semi and/or thiosemicarbazones 7-9. Claisen-Schmidt condensation of compounds 1 or 2 with the appropriate aldehyde yielded the chalcones 10, 11 which, when treated with hydroxylamine hydrochloride gave rise to the isoxazoline-containing compounds 12, 13. Furthermore, reacting the respective chalcones 10, 11 with different hydrazines, urea and/or thiourea, furnished compounds 14, 15, 16, and 17 respectively. Representative compounds were tested for their antimicrobial activity against Candida Albicans and certain gram-positive and gram-negative bacteria. Their MICs were then determined. Compound 15e, showed a broad spectrum of activity while most of the other com-pounds showed varying antimicrobial activity.

• Journal of the Korean Chemical Society
• /
• v.54 no.4
• /
• pp.411-413
• /
• 2010

A simple, efficient and an environmental friendly method have been developed for the synthesis of substituted indole from aryl hydrazines and aldehydes/ketones with HPA-phosphomolybdic acid as a heterogeneous catalyst. The catalyst is nontoxic and recyclable.

• Journal of the Korean Chemical Society
• /
• v.19 no.1
• /
• pp.38-42
• /
• 1975

Chloral-2-acetothienone was synthesized from the condensation of 2-acetothienone with chloral, and trichloroethylidene-2-acetothienone was obtained from the dehydration of chloral-2-acetothienone. From the reaction of trichloroethylidene-2-acetothienone with phenylhydrazine or substituted phenylhydrazines 2-aryl-6-(2-thienyl)-3(2H)-pyridazinones were obtained. 3-(2-Thienyl)-5-trichloromethyl-2-pyrazoline was synthesized from the reaction of trichloroethylidene-2-acetothienone with hydrazine hydrate.

• Archives of Pharmacal Research
• /
• v.16 no.3
• /
• pp.180-185
• /
• 1993

The acid dissociation constants of certain Schiff bases derived from isatin with p-substituted benzoyl hydrazines and somee amino acids of glycine, $\beta$-and $\alpha$-alanine, valine, $\beta$-phenyl-$\alpha$-alanine and anthranilic acid have been detemined potentiometrically at different temperatures in different aquo-organic solvent mixtures (ethnol, dioxane, dimethyl formamide, methanol, acetone and tetrahydrofurance). The pKa values were demonstrated on the light of the different electornic and steric effects of the substituents and the sovlent characteristics. In all the mixed media used, ionization of the compounds decreased by increasing the mole fraction of the organic cosolvent. Theemodynamic parameters $(\Delta{H}^\circ,\;\Delta{G}^\circ,\;\Delta{S}^\circ)$ were evaluated. The structural effects of the investigated compounds on these parameters were reported and discussed.

• Journal of the Korean Chemical Society
• /
• v.14 no.1
• /
• pp.61-64
• /
• 1970

3-Phenyl-5-trichloromethyl-2-pyrazoline was synthesized from the reaction of trichloroethylideneacetophenone with hydrazine hydrate. Pyridazinone derivatives were synthesized from the reaction of trichloroethylideneacetophenone with phenylhydrazine or substituted phenylhydrazines.

• Bulletin of the Korean Chemical Society
• /
• v.31 no.12
• /
• pp.3530-3538
• /
• 2010

In this study 1-[4-(2-methoxy benzyl)-6-aryl-pyridazin-3(2H)-ylidene] hydrazines were used for the synthesis of new heterocyclic systems such as thiazolidine, phthalazine, pyrazolo, tetrazolo, hydrazide and new pyridazine derivatives to explore the effect of silver nanoparticles on their biological activity efficiency. Structures of the new heterocycles were characterized by the aid of several analytical techniques including; $^1H$-NMR, FTIR and mass spectra. Silver nanoparticles were synthesized by a simple methodology and the formation of silver nanoparticles was confirmed by transmission electron microscopy (TEM) and UV studies. Most of the new prepared heterocycles were evaluated in vitro as new antimicrobial agents. Combination effects of the silver nanoparticles on the antimicrobial activity of the new heterocycles were investigated using the disk diffusion method. Compound 10a exhibited the strongest enhancing effect of silver nanoparticles solution against Aspergillus flavus and Candida albicans.

• Journal of the Korean Chemical Society
• /
• v.17 no.1
• /
• pp.25-30
• /
• 1973

2,6-Disubstituted-3-pyridazinones were synthesized by the reactions of $\gamma$,$\gamma$,$\gamma$-trichloroethylidene-m-nitroacetophenone with phenylhydrazine and substituted phenylhydrazines, and hydrazone was isolated as an intermediate from the reaction with 2, 4-dinitrophenylhydrazine. From the reaction with hydrazine hydrate 3-(m-nitrophenyl)-5-trichloromethyl-2-pyrazoline was obtained in good yield. The effect of substituents on phenyl group in the reaction of $\gamma$,$\gamma$,$\gamma$-trichloroethylidene-m-nitroacetophenone with substituted phenylhydrazines was also discussed.