Current Issue : October - December Volume : 2014 Issue Number : 4 Articles : 7 Articles
A series of novel benzamide appended heterocyclic thiadiazole were synthesized and evaluated for their angiotensin-I-converting enzyme (ACE-I) inhibitory activity. Furthermore their antioxidant activity by DPPH assay, lipid peroxidation assay and super radical scavenging activity is described. The reaction of compounds (6a-i) in the presence of conc. H2SO4 proceeded efficiently to give the respective benzamide embedded thiadizole in very good yields. Screening of all the new compounds using ACE-I inhibition assay, when compared to the standard lisinophril resulted the following. Among the compounds, 7i was the marginally active ACE-I inhibitor with IC50 of 40.98 μg/μl and compounds 7b-f were moderate ACE-I inhibitors when compared to standard lisinopril (IC50 value = 40.40 μg/μl). Antioxidant activity, by DPPH assay revealed that compounds 7b-7g were moderate radical scavengers with IC50 value in the range of 31.5-35 μg/μl when compared to standard Ascorbic acid (IC50 value = 24.0 μg/μl). The compounds 7a-7g showed moderate anti-lipid peroxidation activity when compared to standard α-Tocopherol (% activity 49.82) with % activity in the range of 40-45%. By Superoxide radical scavenging assay, compounds 7a-7g were found to be moderate superoxide radical scavengers with % activity in the range of 38-49% when compared to standard Butylated hydroxyanisole (23.55%). Compound 7h exhibited better antioxidant properties by DPPH assay, anti-lipid peroxidation activity and Superoxide radical scavenging assay....
Azetidinones have been known to posses’ antibacterial activity, but recently some new pharmacological activities like antitubercular, carbonic anhydrase inhibitors, local anaesthetics, anti-inflammatory, antihelmintic, anticonvulsant and hypoglycemic activity, have been reported. They posses broad spectrum of activity and are in use as an analgesic agent since very long like few coxibs. Inspired by the above observations, synthesis of new derivatives of 3-(3-chloro-2-oxo-4-substituted phenylazetidin-1-yl)-2-isonicotinoyl-1,2-dihydropyrazol-5-one (3) and 2 - isonicotinoyl - 3 - (3-methyl - 2 - oxo - 4 - substituted phenylazetidin-1-yl)-1,2-dihydropyrazol-5-one (4) were synthesized using microwave as an alternate source of energy. Synthesis of effective COX-2 inhibitors was achieved by attachment of azetidinones with pyrazolones. Synthesized compounds were tested for their analgesic activity and it was found that activity of compound (4f) was comparable to that of the standard used. These compounds therefore, will be used as a prototype to computationally design similar analogues and synthesize those which score well so that, a potent analgesic compound can be obtained....
A series of novel 4-substituted-N-(phenyl(2,4,5-triphenyl-1H-imidazol-1-yl)methyl)benzenamine have been synthesized and evaluated for antidiabetic activity on male wistar rats by oral glucose tolerance test (OGTT) method using pioglitazone as standard. The newly synthesized compounds have been characterized by IR, mass and 1H NMR spectroscopic studies and report of them supports the structures of compounds. Comparison of data was performed by one way ANOVA followed by post test, dunnett’s multiple comparision tests....
Basic NSAIDs are gaining interest because of their improved biological properties with the aim of improving the therapeutic index through prevention of gastrointestinal complications. Pyrazole and benzothiazoles are well established in literature as important biologically active heterocyclic compounds. A series of some novel 2-aminobenzothiazole derivatives were synthesized. These substituted 2-aminobenzothiazoles (Ia-f) has been reacted with acetyl acetone and different hydrazines to give various (3,5-dimethyl-1-substitutedphenyl-1H-pyrazole-4-yl)-(substituted benzothiazole-2-yl)-diazene (IIIa-r). The purity of the synthesized compounds was checked by TLC. All the synthesized compounds were characterized by IR, 1H NMR and mass spectral studies and screened for their anti-inflammatory activity by in-vitro method using analgin as a standard drug. Out of the eighteen test compounds, compounds IIIa, IIIb, IIIh, IIIn showed good anti-inflammatory activity....
A new route have been developed for synthesis of 6,8-dichloro-3-[(E)-1,2-diphenylethenyl] [1,2,4]triazolo[3,4-b][1,3]benzoxazole derivatives 7(a-f). The compound (3) treating with Phenylacetic acid (4) in ethanol yield3-benzyl-6,8-dichloro[1,2,4]triazolo[3,4-b][1,3]benzoxazole (5). The compound (5) further reacting with different aromatic aldehydes to form target molecules 7(a-f) by Knoevenagel condensation method. The obtained products have been characterized by IR, 1H NMR, 13C NMR and Mass spectral studies. The synthesized molecules subjected for antimicrobial and antioxidant activity to know the efficacy of molecules....
A series of 2-substituted benzylidene-tetralone was prepared from tetralone by using an aldol condensation and then these synthesized benzylidene-tetralone derivatives were further condensed with phenyl hydrazine to give various substituted pyrazoline derivatives. All of these compounds have been characterized by IR, NMR and mass spectral analysis for structure establishment and further evaluated for their antifungal activity against Aspergillus niger (MTCC-282) and Candida albicans (MTCC-227) by agar diffusion method using fluconazole as standard drug. Among benzylidiene derivatives; compounds C1, C2, were least active and compounds C3, C4, C5, were moderately active while among pyrazoline derivatives; compounds C6, C7 were least active and compounds C8, C10, were moderately active and compounds C9 were highly active. When electron-withdrawing substitutions were made on both ring antifungal activity increased in (NO2 > F> Cl) order. The maximum zone of (56%, 69%) was shown by compound C4 among benzylidiene derivative and (76%, 76%) by compound C9 among pyrazoline derivative against Aspergillus niger and Candida albicans respectively....
Hydrazones are a class of reactive organic compounds present in various therapeutically active molecules. They were reported to possess antimicrobial, anti-inflammatory, anti-tubercular, anticonvulsant and anticancer activity. Therefore, an attempt is made to synthesize new hydrazones from different aldehydes and phenyl hydrazine. All these synthesized compounds were characterized by means of IR, 1H NMR, 13C NMR and MASS spectrum data. These compounds were evaluated for antimicrobial activity by cup plate method, antitubercular activity by alamar blue dye method and anti-inflammatory activity by gelatin gel zymography....
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