Abstract: 5-(3,5-Dibromo-2-hydroxyphenyl)-2,3,4-trihydro-1,2,4-triazole-3-thione(4) and 3-[(5-bromo-or 3,5-dibromo-2-hydroxy-phenylmethylene)-amino]-4-oxo-imidazolinidin-2-thiones(7a,b)were prepared via the reaction of 2,3,5trisubstituted benzaldehyde thiosemicarbazones(2a,b)with bromine in acetic acid and ethylchloroacetate in presence of fused sodium acetate. While 5-(4-methylphenyl-2-[3,5-dibromo-2-hydroxy-phenylmethylene)-hydrazion]-thiazole(5) prepared via reaction of (2b) with 4-methyl phenacylbromide. Acylation of (2b) and (5) with acetic anhydride gave the corresponding diacetyl derivatives (3) and (6).

Abstract: 2-(5-Mercapto-4-phenyl-4H-[1,2,4]triazol-3-ylmethyl)-6-p-tolyl-4,5-dihydro-2H-pyridazin-3-one (3) was prepared according to the established sequenced procedures 1-3 . Subsequently by using selected alkylating agents; compounds 4a-c were prepared via regioselective S alkylation procedure4. Alternatively, compounds 5a-c were prepared via regioselective addition procedure 4 . Under Mannich condition, some interesting compounds 7a,b and 8a,b were successfully prepared. On the other hand, the azides 10 and 15 coupled with amino acid esters 11a-d and 15a- d to give amino acids derivatives 12a-d and 16a-d in good to moderate yield respectively. The structural elucidation of products is reported and also some of the products were screened for their antimicrobial activity.

Abstract: 1-acetyl-3-[(5-bromo-2-acetoxy-phenylmethylene)-amino]-4-oxo-imidazolidin-2-thione (2) and 5-acetyl-3-[(5-bromo-2-hydroxy-phenylmethylene)-amino]-4-oxo-imidazolidin-2-thione(3)prepared by Acylation of 3-[(5-bromo-2-hydroxy-phenylmethylene)-amino]-4-oxo-imidazolidin-2-thione(1) by different method. The reaction of 3-[(5-bromo-2-hydroxy-phenylmethylene)-amino]-4-oxo-imidazolidin-2-thione (1) with bromine in presence of glacial acetic acid resultthe 5-bromo- 3-[(5-bromo-2-hydroxy-phenylmethylene)-amino]-4-oxo -imidazolidin-2-thione (4). The Acylation of compound (4) with acetic anhydride led to formation 5-bromo-1,5-diacetyl-3-[(5-bromo-2-acetoxy-phenylmethylene)-amino]-4-oxo-imidazolidin-2-thione (5). The hydrazinolysis of compound (1) with hydrazine hydrated led to formation of 2, 4-dihydrazino-3-[(5-bromo-2-hydroxy-phenylmethyl)-amino]-imidazolidine (6). The condensation of compound (1) with different aldehyde led to formation of (7a-c). The action of acetic anhydride on compounds (7a-c) under reflux led to formation of (8a-c).

Abstract: Two new disazo compounds containing 4,4'-diaminostilbene- 2,2'-disulfonic acid and 4,4'-diaminobenzanilide as middle components were synthesized and characterized by thin layer chromatography (TLC), electronic spectra (VIS), FT/IR and 13 C-NMR spectroscopy. According to the results of the colouristic evaluation, the studied azo compounds can be ranged in the direct dye's class. The individual human skin tolerance for these azo compounds was evaluated by in vivo imagistic skin studies and the obtained results indicate that, from dermatologic point of view, the azo compounds may be used as textile dyes. Further, the compounds were evaluated for antibacterial activity against Staphylococcus aureus, Streptococcus pyogenes, Escherichia coli, Pseudomonas aeruginosa and Proteus vulgaris by the disk diffusion method. The screening data releaved that the studied azo compounds exhibited antimicrobial activity against most of the tested species, presenting a particular interest against Staphylococcus aureus and Escheria coli.

Abstract: Starting from 7-hydroxy-4-methylcoumarin which was prepared via pechmann condensation, some comarin derivatives were synthesized depending on several reactions which are condensation with aldehydes, Mannich reaction, alkylation and reaction with hydrazine hydrate. The prepared compounds were evaluated for their microbiological activity against Grame +ve bacteria Bacillus Subtilis, Gram –ve bacteria Serratia marcenses and fungi Trichoderma Sp.

Abstract: 0-N-Methylpurpuramine E has been successfully synthesized in 2 steps in good yield from readily available starting materials. Structural elucidation has been confirmed through direct comparison with spectroscopic data of isolated natural product.20-N-Methylpurpuramine E has been shown to have MIC = 5 μg mL^-1 against Mycobacterium bovis.

Abstract: The title compound, 3-chlorohimacha-3-one has been synthesized by catalytic oxidation with ruthenium trichloride and sodium periodate of 3-chlorhimachl-6,13-ene(1). .The structure of this new compound was confirmed by elemental analysis, IR, ¹H-NMR, ¹³C-NMR and EI-Ms spectral analysis.

Abstract: We have generated different resveratrol-coumarin hybrids with the aim of evaluate their biological applications and their pharmacological properties, particularly the inhibitory activity of monoamine oxidase enzyme. According to that, a first series of 3-aryl-4-hydroxycoumarins has been synthesized starting from aryl boronic acids and phenyliodonium zwitterions precursors by a palladium-catalyzed coupling reaction.

Abstract: novel oleanen type triterpenoid, has been isolated from butanolic extract of the seeds of Ricinus communis. Its structure was elucidated as 3-O-[β -D-glucoronopyranosyl-(1→ 3)-α –L-rhamnopyranosyl-(1→ 2)β-D-glucopyranosyl]-4α,20α-hydroxy methyl olean-12-ene-28-oic acid on the basis of spectral evidences i.e. FTIR, ¹H NMR, ¹³C NMR and FAB-MS data. The isolated saponin was tested for its antibacterial and antifungal activity, where the growth of microbes was found to be inverse function of concentration of saponin. The MIC value for E.coli was found to be 260µg/mL and that of Staphylococcus aureus was 350µg/mL

Abstract: We report that the clinically used antitumor drug mitomycin C is reductively activated in vitro by simple thiols; a mechanism for this activation is proposed based on kinetic data and the identification of mitosene metabolites. The biological implications of these findings are discussed.

Abstract: Glycosyl (iso) thioureas being an important intermediate in the synthesis of thioureido carbohydrates herein we reported the synthesis of per–O–acetyl lactosyl aryl isodithiobiuret derivatives. These compounds were synthesized by nucleophilic addition of per-O-acetyl lactosyl aryl isothiourea to tolyl isothiocyanate. Structures of these compounds were confirmed on the basis of IR, HNMR, Mass spectra and elemental analysis. These compounds were also screened for their in vitro antimicrobial activities against bacteria S. aureus, E. coli, P. vulgaris, P. aeruginosa and fungi A. niger, Penicillium.

Abstract: The enzyme thymidine phosphorylase (TPase) is involved in the metabolism of thymidine. It catalyses the phosphorolysis of several nucleoside analogues serving as antiviral or antitumour agents. Besides, it also plays an important role in the angiogenesis. Thus, inhibition of TPase activity may serve as a plausible therapeutic strategy for the treatment of cancer. In this report, the structure-based design, synthesis, and anti-TPase activity of a class of novel inhibitors of TPase are described using fused bicyclic 1,3,5-triazine-2,4-dione or 1,3,5-triazine-2-thioxo-4-one as the core scaffold, and the latter scaffold shows some activity in TPase enzyme assay.

Abstract: We report that the clinically used antitumor drug mitomycin C reacts with excess dithiols to give dithiol cross-links as major products. Mechanistic studies reveal that three dithiol molecules participate at different stages of the reaction: in the reductive activation of mitomyicin C, in an alkylation at C1, and in an additional reduction that activates C10 for the second-arm alkylation by the dithiol. We hypothesize that the reactions reported here indicate that mitomycin C could act as a mechanism-based inhibitor of enzymes containing a dithiol active site.

Abstract: We report two unexpected findings ocurring after treatment of the antitumor drug mitomycin C with dithiols. The first finding relates to the reaction of mitomycin C with exactly one molar equivalent of dithiol to form a mitosene-like material with unusual physico-chemical properties. The second finding was the formation of unexpected dimeric mitosenes when the reaction of MC with dithiols was quenched at short reaction times. We hypothesize that both events are originated by an unprecedetended deaziridination reaction.

Abstract: 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 2^nd 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.

Abstract: A series of benzothiazolylthioacetyl amino acid and peptide derivatives including glycoside, hydrazide and hydrazone moieties were synthesized with the aim of evaluating their antifungal activity. Their chemical structures were confirmed by 1 H NMR, IR, mass spectrometry and elemental analyses. Out of the thirty two tested compounds three derivatives have enhanced activity as fluconazole at 100 ppm and six at 1000 ppm toward Candida albicans whereas, they were actually inactive toward Aspergillus flavus.

Abstract: 1,2-O-(R)-Trichloroethylidene-α-D-xylo-1,4-furanodialdose hydrate was obtained fromα-chloralose via conventional sodium metaperiodate cleavage-oxidation reaction. 1,2-O-(R)-trichloroethylidene-α-D-xylo-1,4-furanodialdose thiosemicarbazonewas obtained from the reaction of 1,2-O-(R)-trichloroethylidene-α-D-xylo-1,4-furanodialdose hydrate with thiosemicarbazide in the presence of an acid catalyst. The structure of thiosemicarbazone product was characterized with NMR and FTIR spectroscopic methods. This new compound (5) was evaluated for its antimicrobial activity against Gram-positive, Gram-negative bacteria and C. albicans using the well diffusion and microdilution method. The thiosemicarbazone product shows significant growth inhibitory activity against bacteria Staphylococcus aureus, Escherichia coli, Kocuria rhizophila, Bacillus cereus, Enterobacter aerogenes and showed moderate activity against Candida albicans. The minimal inhibitory concentrations (MIC) experiments revealed that tested compound exhibited variable MICs and selective antimicrobial activity, depending on the microbial strains.

Abstract: A QSAR study has been performed on a series of substituted pyrido[3,2-b]pyrazinones as potent and selective PDE-5 Inhibitors. The compounds in the selected series were characterized by spatial, molecular and electrotopological descriptors using QSAR module of molecular design suite (V-Life MDS^TM 3.5). Correlations between inhibitory activities and calculated predictor variables were established through partial least square regression (stepwise forward) method. The generated QSAR models reveal that the topology of the molecules crucially influences the desired inhibitory activity of pyrido[3,2-b]pyrazinones. PDE-5 inhibition can be well defined by the models generated and the molecules are more selective towards PDE –5 while PDE –6 and PDE –11 inhibitory activities cannot be well delineated by the help of generated QSAR models. So PDE-5 selective compounds can be synthesized based on the assumption of the present QSAR analysis. The best model shows 90% correlation for PDE-5 inhibitory activity which explains good reliability of the model. However cross correlated regression coefficients (Q²) 0.5959 further validate the model significance. The present study imply that the PDE-5 inhibition can be augmented primarily by increasing molecular refractivity and number of carbons connected to the aromatic rings, single bonds and by decreasing number of carbons connected to the double bonds.

Abstract: Tetrabutylammonium phthalimide-N-oxyl (TBAPINO) was used as an efficient organocatalyst to catalyze the Strecker reaction of diverse aldimines with trimethylsilylcyanide (TMSCN) in EtOH. The reaction proceeded smoothly at room temperature to afford the corresponding α-aminonitriles in quantitative yields under mild reaction conditions.

Abstract: Novel transition metal(II) complexes, [M(L₁)₂Cl₂] and [M(L₂)₂Cl₂], were synthesized from the reaction of MCl₂.nH₂O (M = Co, Ni, Cu) with (Z)-1-(1-(1H-indol-3-yl)ethylideneamino)quinolin-2(1H)-one (L₁) or (E)-1-(2-hydroxybenzylideneamino)quinolin-2(1H)-one (L₂). The ligands were obtained from coumarin. N-amino quinoline-2-one (2) has been synthesized by the reflux of coumarin (1) with hydrazine hydrate in ethanol for 12 hr. The azomethines (L₁, L₂) were prepared from the corresponding aryl aldehydes. The synthesized compounds were and characterized by element chemical analysis, molar conductance, magnetic susceptibility measurements, and spectral (electronic, and FT-IR) studies. The IR spectral data suggest the involvement of sulphur and azomethane nitrogen in coordination to the central metal ion. On the basis of spectral studies, an octahedral geometry has been assigned for all complexes. The free ligands and its metal complexes have been tested in vitro against a number of microorganisms in order to assess their antimicrobial properties.

Abstract: A series of sixteen pyrazinamide analogues with the -CONH- linker connecting the pyrazine and benzene rings was synthesized by the condensation of chlorides of substituted pyrazinecarboxylic acids with ring-substituted (chlorine) anilines and characterized. The results of in vitro antimycobacterial screening indicated some interesting antimycobacterial activity. 6-Chloro-N-(4-chlorophenyl)pyrazine-2-carboxamide (6) has shown the highest activity against Mycobacterium tuberculosis strain H37Rv (65% inhibition at 6.25 μg mL^-1). The highest antifungal effect against Trichophyton mentagrophytes, the most susceptible fungal strain tested, was found for 6-chloro-5-tert-butyl-N-(3,4-dichlorophenyl)pyrazine-2-carboxamide (16) (MIC = 62.5 μmol mL^-1). 6-Chloro-5-tert-butyl-N-(4-chlorophenyl)pyrazine-2-carboxamide (8) was the most active in the inhibition of photosynthetic electron transport (PET) in spinach (Spinacia oleracea L.) chloroplasts (IC₅₀ = 43.0 μmol mL^-1). The compounds were analyzed using RP-HPLC to determine lipophilicity. Optimal log P value for studied series was not confirmed.For all the compounds, the relationships between the lipophilicity and the chemical structure of the studied compounds are discussed, as well as their structure-activity relationships (SAR).

Abstract: In this study, a series of nine 4-chloro-2-(3,4-dichlorophenylcarbamoyl)phenyl N-alkylcarbamates was prepared. The procedures for synthesis of the compounds are presented. The compounds were analyzed using RP-HPLC to determine lipophilicity. They were tested for their activity related to inhibition of photosynthetic electron transport (PET) in spinach (Spinacia oleracea L.) chloroplasts. For the compounds, the relationships between the lipophilicity and the chemical structure of the studied compounds are discussed, as well as their structure-activity relationships (SAR).

Abstract: This work involves to synthesisnovel organic compounds and studies their pharmacological. Approach: The title compound quinazolinone derivatives were prepared by reacting 3 amino of 3-amino-2-methylquinazolin-4(3H)-one (first) with various aldehydes and ketones, and second coupling through diazonium salts with resorcinol or with ethylacetoacetate then cyclized with hydrazine. The starting material 3-amino-2-methylquinazolin-4(3H)-one was synthesized by reacting hydrazine with 2-methyl-4H-benzo[d][1,3]oxazin-4-one, which in turn was prepared from anthranilic acid. The chemical structures of the synthesized compounds were confirmed on the basis of their spectral data (FT-IR, UV/visible, ¹HNMR, spectra and CHN analyss). All synthesized compounds were tested in vitro against a number of microorganisms (Staphylococcus aurous, E.coli, Proteus vulgaris, Pseudomonas, and Klebsiella) and two fungal Aspergillus niger and Candida albicans in order to assess their antimicrobial properties. Results: The study indicates that these compunds have high activity against tested bacteria. Aim: We aim to synthesize quinazolinone derivatives having active moieties to evaluate their antimicrobial activities. Conclusion/Recommendations: Based on the reported results, it may be concluded that 3-amino-2-methyl- quinazolin-3(4H)-one act as synthones for Schiff bases and for diazonium coupling. [Researcher 2010;2(4):82-88]. (ISSN: 1553-9865).

Abstract: Mesoporous Borosilicate (B-MCM-41) efficiently catalyzed the three-component Strecker-type reaction of different amines and aldehydes or ketones with trimethylsilyl cyanide (TMSCN) in CH₂Cl₂ at room temperature to afford the corresponding α-aminonitriles in excellent yields. The catalyst can be recovered and reuse for at least 5 reaction cycles without significant lose of its reactivity.

Abstract: Vilsmeier-Haack reaction conditions were applied on some methyl ketone aryl phosphonic dihydrazones to yield some interesting bis-pyrazole derivatives containing a hydro-phosphoryl unit. Bis-{4-formyl-3-aryl-1H-pyrazol-1-yl}phosphine oxides (4a,b) were condensed with some nucleophiles such as aniline, phenacyl triphenylphosphonium bromide and 4-phenylthiosemicarbazide followed by treatment with thioglycolic acid, diethyl phosphite and/or acetic anhydride to yield a novel class of bis-pyrazoles containing sulfur and phosphorus derivatives. Most of the newly synthesized compounds were evaluated for their in vitro antimicrobial activities.