Ethyl 3-amino-5-bromo-1-benzo-furan-2-carboxyl-ate.

The title compound, C11H10BrNO3, is close to planar with the benzo-furan unit and the ester group subtending a dihedral angle of 5.25 (2)°. The mol-ecular structure features an intra-molecular N-H⋯O inter-action. In the crystal, N-H⋯O hydrogen bonds involving carboxyl O-atom acceptors generate a chain extending along [201].

Ethyl 5-bromo-3-eth-oxy-carbonyl-amino-1-benzofuran-2-carboxyl-ate.

In the title compound, C14H14BrNO5, the ester group is disordered [occupancy ratio 0.52 (2):0.48 (2)]. The major component is nearly coplanar with the benzofuran plane, subtending a dihedral angle of 7.84 (2)°, while the amide group is twisted out of the benzofuran plane making a dihedral angle of 39.69 (2)°. An intra-molecular N-H⋯O hydrogen bond occurs. In the crystal, pairs of weak C-H⋯O hydrogen bonds link the mol-ecules into inversion dimers, which are further linked via strong N-H⋯O hydrogen bonds, generating a zigzag chain extending along [100].

Ethyl 5-bromo-naphtho-[2,1-b]furan-2-carboxyl-ate.

In the title compound, C(15)H(11)BrO(3), the dihedral angle between the naphtho-furan ring system (r.m.s. deviation = 0.022 Å) and the side chain is 4.50 (2)°. In the crystal, short Br⋯Br [3.4435 (7) Å] contacts propagating along [010] in a zigzag manner and weak π-π inter-actions [shortest centroid-centroid separation = 3.573 (2) Å] directedalong [100] are observed.

Ethyl 1-aminona-phtho[2,1-b]furan-2-carboxyl-ate.

In the title compound, C(15)H(13)NO(3), there is intra-molecular N-H⋯O hydrogen bond between the amino group and the ester carbonyl O atom and the dihedral angle between the aromatic ring and the ester group is 2.05 (15)°. In the crystal, mol-ecules are connected by N-H⋯O hydrogen bonds into chains parallel to [010]. In addition there are short C-H⋯O inter-actions and π-π stacking inter-actions with a distance of 3.555 (2) Šbetween the centroids of the furan and benzene rings.

N-(Phenyl-sulfon-yl)naphtho-[2,1-b]furan-1-carboxamide.

In the title compound, C(19)H(13)NO(4)S, the mol-ecule is twisted at the S atom with a C-S-N-C torsion angle of -65.2 (2)° between the benzene ring and the -SO(2)-NH-C=O segment. The dihedral angle between the benzene and the naphtho-furan ring system is 83.3 (1)°. In the crystal, mol-ecules are linked by N-H⋯O hydrogen bonds into chains running along the c axis. An intra-molecular N-H⋯O(furan) inter-action is also observed.

Screening of Bauhinia purpurea Linn. for analgesic and anti-inflammatory activities.

OBJECTIVES: Ethanol extract of the stem of Bauhinia purpurea Linn. was subjected to analgesic and anti-inflammatory activities in animal models. MATERIALS AND METHODS: Albino Wistar rats and mice were the experimental animals respectively. Different CNS depressant paradigms like analgesic activity (determined by Eddy's hot plate method and acetic acid writhing method) and anti-inflammatory activity determined by carrageenan induced paw edema using plethysmometer in albino rats) were carried out, following the intra-peritoneal administration of ethanol extract of Bauhinia purpurea Linn. (BP) at the dose level of 50 mg/kg and 100 mg/kg. RESULTS: The analgesic and anti-inflammatory activities of ethanol extracts of BP were significant (P < 0.001). The maximum analgesic effect was observed at 120 min at the dose of 100 mg/kg (i.p.) and was comparable to that of standard analgin (150 mg/kg) and the percentage of edema inhibition effect was 46.4% and 77% for 50 mg/kg and 100 mg/kg (i.p) respectively. Anti-inflammatory activity was compared with standard Diclofenac sodium (5 mg/kg). CONCLUSION: Ethanol extract of Bauhinia purpurea has shown significant analgesic and anti-inflammatory activities at the dose of 100 mg/kg and was comparable with corresponding standard drugs. The activity was attributed to the presence of phytoconstituents in the tested extract.

Synthesis of new 4-pyrrol-1-yl benzoic acid hydrazide analogs and some derived oxadiazole, triazole and pyrrole ring systems: a novel class of potential antibacterial and antitubercular agents.

In the present study, a novel series of 4-pyrrol-1-yl benzoic acid hydrazide analogs, some derived 5-substituted-2-thiol-1,3,4-oxadiazoles, 5-substituted-4-amino-1,2,4-triazolin-3-thione and 2,5-dimethyl pyrroles have been synthesized in good yields and characterized by IR, NMR, mass spectral and elemental analyses. Compounds were evaluated for their preliminary in vitro antibacterial activity against some Gram-positive and Gram-negative bacteria and compounds were screened for antitubercular activity against Mycobacterium tuberculosis H37Rv strain by broth dilution assay method. Some compounds showed very good antibacterial and antitubercular activities.

Synthesis and Activity Evaluation of 2-(1-naphtho[2,1-b]furan-2-yl-carbonyl)-3,5-disubstituted-2,3-dihydro-1H-pyrazoles.

Ethyl naphtho[2,1-b]furan-2-carboxylate (2) on reaction with hydrazine hydrate in presence of acid catalyst in ethanol medium affords naphtho[2,1-b]furan-2-carbohydrazide (3). The reaction of substituted acetophenones (4a-c) with aromatic aldehydes (5a-e) produces chalcones (6a-o) via the Claisen condensation. The reaction of naphtho[2,1-b]furan-2-carbohydrazide (3) with chalcones (6a-6o) in presence of acetic acid as catalyst in dioxane produces 1-(naphtho[2,1-b]furan-2-yl-carbonyl)-3,5-disubstituted-2,3-dihydro-1H-pyrazoles (7a-o). The structures of newly synthesized compounds have been established by elemental analysis and spectral studies. The compounds 7a-o have been evaluated for their antimicrobial activity and some selected compounds evaluated for antiinflammatory, analgesic, anthelmintic, diuretic and antipyretic activities.

Antioxidant, cytotoxic and genotoxic evaluation of alcoholic extract of Polyalthia cerasoides (Roxb.) Bedd.

Antioxidative potential of alcohol extract of Polyalthia cerasoides was evaluated using 1,1-diphenyl-2-picrylhydrazyl (DPPH), hydroxyl radical, superoxide anion scavenging, and reducing power assays were performed. The extract showed significant reactive oxygen species (ROS) scavenging activity in all in vitro antioxidant assays and contained high level of total phenolic content. For in vivo genotoxic evaluation, Swiss albino mice were treated with alcohol extract at the concentration of 40mg/kg body weight. Frequency of aberration was compared with control. Both the sets did not showed genotoxic effect. Further the extract was subjected to cytotoxic study using 3-(4,5-dimethyl thiazol-2-yl)-2,5-diphynyl tetrazolium bromide (MTT) assay, the extract confirmed to show moderate cytotoxicity against L929 cell line.

Studies on synthesis and pharmacological activities of 3,6-disubstituted-1,2,4-triazolo[3,4-b]-1,3,4-thiadiazoles and their dihydro analogues.

Several 3,6-disubstituted-1,2,4-triazolo[3,4-b]-1,3,4-thiadiazole and their dihydro analogues were synthesized from hetero aromatic acids and hetero aromatic aldehydes, respectively, by microwave-assisted dry media and conventional methods. Elemental analysis, IR, (1)H NMR, (13)C NMR and mass spectral data elucidated the structures of all newly synthesized compounds. Synthesized compounds are studied for their antibacterial, antifungal, anti-inflammatory and analgesic activities. Some of the tested compounds showed significant pharmacological activities.

Heterocyclic system containing bridgehead nitrogen atom: synthesis and pharmacological activities of some substituted 1,2,4-triazolo[3,4-b]-1,3,4-thiadiazoles.

Several 3,6-disubstituted-1,2,4-triazolo[3,4-b]-1,3,4-thiadizoles were prepared by the condensation of 4-amino-3-aryl/aralkyl substituted-5-mercapto-1,2,4-triazoles 3(a-c) with various substituted aromatic/hetero aromatic acids through a single step reaction. Elemental analysis, IR, 1H NMR and mass spectral data confirmed the structure of the newly synthesized compounds. Synthesized triazolo thiadiazoles investigated for their antibacterial, antifungal, anti-inflammatory and analgesic activities. Some of the tested compounds showed moderate antimicrobial activity against various tested bacterial and fungal strains. None of the synthesized compounds have significant anti-inflammatory and analgesic activities.