Current Issue : April - June Volume : 2011 Issue Number : 2 Articles : 11 Articles
A new convenient method for the synthesis of 6-amino-2H,4H-pyrano[2,3-с] pyrazole-5-carbonitriles, namely, four component condensation of aromatic aldehydes, activated methylene reagent, ethyl acetoacetate, and hydrazine hydrate in water in the presence of triethylamine as a catalyst....
A new titanocenyl amide containing flavone as pendant group has been synthesized by reaction of titanocenyl carboxylic acid chloride and 7-Aminoflavone and structurally characterized by spectroscopic methods. This species and eight previously synthesized titanocenyl amide complexes have been tested in breast adenocarcinoma cancer cell line, MCF-7. The functionalization of titanocene dichloride with amides enhances the cytotoxic activity in MCF-7. Two sets of titanocenyl amides can be identified, with I C 5 0 < 1 0 0 ? ?? M and I C 5 0 > 1 0 0 ? ?? M. The most cytotoxic species is Cp(CpCO-NH- C 6 H 4 - ( C H 2 ) 2 C H 3 ) T i C l 2 with an I C 5 0 of 24(2)? ?? M, followed by Cp(CpCO-NH- C 6 H 4 -Br) T i C l 2 , I C 5 0 of 46(4)? ?? M and Cp(CpCO-NH- C 6 H 4 - O C F 3 ) T i C l 2 , I C 5 0 of 49(6)? ?? M. There is no correlation between the nature of the para substituent on the phenyl ring and the cytotoxic properties on MCF-7 cell line....
In the present study we have designed a new pharmacophore ‘Chalconesemicarbazone’ by pharmacophore hybridization approach of drug design. The possible metabolites of some selected synthesized chalconesemicarbazones were predicted by computational method using Pallas version-3.1 ADME-Tox prediction (metabolism prediction by Mexalert/RetroMex) software. A series of chalconesemicarbazones was synthesized and evaluated for their antifungal activity by paper disk diffusion method. Based on the results of an antifungal study, 1-[1-(2-hydroxyphenyl)-3-(4-methoxyphenyl) allylidene]-4-(4-methylphenyl) semicarbazide (compound 16) was the most active compound. The highest activity observed in compound 16 is probably due to the presence of methoxy group in aldehydic moiety of the chalcone. Unsubstituted compounds or lengthening of carbon chain or chloro substitution showed very less activity....
Tuberculosis (TB) is an important disease that causes thousands of deaths around the world. Resistance against antitubercular available drugs has been reported; so, research on new effective antimycobacterial molecules is needed. Antimycobacterial activity of three lignans and two synthetic hydrazones was assessed against Mycobacterium tuberculosis H37Rv by antimycobacterial microdilution assay (TEMA). An oxadiazoline (AC451) and a lignan (ethoxycubebin) were the most active compounds (MIC 6.09 and 62.4?�µM, resp.). Several changes in mycolic acid profile of treated bacteria were detected with both compounds by mass spectrometry analysis. Additionally, the level of reduction of mycolic acids in ethoxycubebin treatment was correlated to disruption in bacterial morphology....
In order to develop new antimicrobial agent, a series of N1- substituted 3, 5 diphenyl pyrazolines were prepared and evaluated for their antimicrobial activity. The SAR analysis showed that the antimicrobial activity was highly dependent on the substitution pattern of the aryl rings and correlated to a large extent with the ability of compounds to interact with sulfhydryl group. All the synthesized compounds have been characterized by spectral analysis and have been screened for their antimicrobial activity against Gram–ve bacteria (E.coli) of clinical relevance and also against strain of fungi (S.cerevisae). Among the prepared compounds those with electron withdrawing groups located in the p-position in the ring B, and hydroxyl group at ortho position had a powerful accelerating effect on the reactivity of the sulfhydrl group....
3,4-Epoxy-2-dodecanone, a major component in the preorbital gland of the African grey duiker (Sylvicapra grimmia), showed antimicrobial activity in preliminary tests. The C11 to C17 homologues of this compound were prepared and their activity against several pathogenic dermal bacteria and fungi was tested. 3,4-Epoxy-2-dodecanone and 3,4-epoxy-2-tridecanone inhibited the growth of Trichophyton mentagrophytes at 25 �µg/mL. Moderate inhibition of the growth of the bacteria Propionibacterium acnes and the lipophilic yeast, Pityrosporum ovale, was seen for several of the homologues....
As benzothiazole has proven to be good antimicrobial agent, in the present study Benzothiazoles has been chosen as basic nucleus. The nucleus was reacted with p-nitro benzoyl chloride in the presence of TEA and 1,4 dioxane to obtain N-(6- fluorobenzo[d] thiazol-2-yl)-4-nitrobenzamide, which was subjected to reduction by Fe/ Hcl to obtain N-(6- fluorobenzo[d] thiazol-2-yl)-4-aminobenzamide. This product contains active site (-NH2) from which one water molecule was lost and Schiff bases were prepared by using various substituted benzaldehydes. Their purity and homogeneity were confirmed from their sharp physical constants and Rf values. All the Schiff bases were obtained in solid form with excellent yield. Structures of the synthesized compounds were elucidated on the basis of elemental analyses and spectral data. All the synthesized compounds were screened for their antitubercular and antibacterial activity....
A series of biologically active cinchophen analogues, 2-(1-benzofuran-2-yl) quinoline-4-carboxylic acid and 2-(5-bromo-1-benzofuran-2-yl) quinoline-4-carboxylic acid have been synthesized using Pfitzinger method. The structures were established by IR, 1HNMR and mass spectral data. Antibacterial results revealed that compounds 3a, 3b, 3e, and 3f possess good activity against Pantoea dispersa. Whereas, compounds 3a, 3c, 3g and 3h have showed good activity against Ochrobacterium species, Entercoccus species and Staphylococcus aureus at 100 μg/ml concentration. The compound 3g showed significant analgesic and anti-inflammatory activity at a concentration of 100 mg/kg body weight, when compared with other compounds....
A vast array of thiazole derivatives having excellent broad spectrum activity forms an invaluable part of the present armory of the clinicians. The synthesis and antibacterial activity of several new ethyl 2-amino-4-methylthiazole-5-carboxylate(1)5derivatives substituted at 2nd position by aryl aldehydes of the thiazole moiety have shown some to increase the antibacterial activity of thiazole. In this study we thought to synthesize thiazole system incorporating substituted aryl aldehydes. The most active compound was 4-methyl-5-hydrazine hydrate-2-(4-methoxy-3-hydroxy benzene) methyleneamino thiazole-5-carboxylate (3c) equipotent to Ciprofloxacin.C2 position of thiazole ring requires large hydrophilic, electronegative functional moieties like substituted phenyl ring etc for enhanced antibacterial activity of thiazole. In our compounds alkyl (methyl) group is present, still most of the compounds show good antibacterial activity.C5 position of thiazole ring requires small hydrophobic, electronegative functional moieties like amino, hydrazine hydrate attach with ester for antibacterial activity of thiazole in general....
A series of chalcone-based diarylpyrazoles containing a phenylsulphone or carbonitrile moiety was synthesized. Thus, 3-acetylpyrazoles 6aââ?¬â??c and 10aââ?¬â??c were used as useful substrates in facile synthesis of functional pyrazoles 7aââ?¬â??f and 11aââ?¬â??f, respectively. The anti-inflammatory activity and ulcerogenic effect were evaluated and some of the obtained products possessed a significant anti-inflammatory activity. 1-[1-(3-Methylphenyl)-5-phenyl-4-(phenylsulfonyl)-1H-pyrazol-3-yl]ethanone (6b) showed a high activity when compared with indomethacin as reference drug with lower gastrointestinal (GI) profile. Furthermore, molecular docking studies were performed in order to rationalize the obtained biological results....
Quinolones are well known for their antibacterial properties, differently substituted quinolones have been synthesized in the present research work by cyclization of parasubstituted aniline with diethylethoxymethylene malonate followed by alkaline hydrolysis and evaluated to explore the effect of substitution at different sites on the antibacterial activity. The present study was done to exploring the effect of different subtituents at 6 and 8 positions on the antibacterial activity. It was found that by substitution at 6 and 8 positions there is improvement in antibacterial activity. The compound B was found to be most effective against E.coli and b.subtillus in comparison to the standard drug at concentration 2µg/ml, 8µg/ml. The compound A was found to be least effective against E.coli and b.subtillus in comparison to standard drug .Antibacterial activity was evaluated by finding minimum inhibitory concentrations (MICs) of antibacterial agents by agar dilution method....
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