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Aswathanarayanappa C.,Biocon | Aswathanarayanappa C.,Kuvempu University | Bheemappa E.,Sir Mv Government Science College | Bodke Y.D.,Kuvempu University | And 5 more authors.
Medicinal Chemistry Research

Previously unknown biphenyl containing 5-phenyl-1-benzofuran-2-yl derivatives; methanones (2a-i), tertiary alcohols (3a-l), and carbinols (4a-f) were synthesized and evaluated for their antimicrobial and antioxidant activities to study the effect of functionalization at the carbonyl carbon and substitution at biphenyl ring on these activities. The introduction of hydroxyl group at carbonyl carbon enhanced the antioxidant property (3a, 3g, 3h, 4a, and 4b), while antimicrobial activity decreased; the carbinol and tertiary alcohols corresponding to methanone 2a and 2b showed no antimicrobial activity. Biphenyl methanones 1, 2a, 2f, and 2g exhibited antimicrobial activity with minimal inhibitory concentration ranging between 0.001 and 0.500 mg/mL, tertiary alcohols 3a, 3g, and 3h and carbinols 4a and 4b exhibited the promising antioxidant property. The mode of action of these active compounds was carried out by docking of receptor GlcN6P synthase with newly synthesized candidate ligands 1, 2a, 2e, 2f, 2g, 2h, 3a, 3g, 3h, 4c, and 4d. © 2012 Springer Science+Business Media, LLC. Source

Pradeepa S.M.,Kuvempu University | Bhojya Naik H.S.,Kuvempu University | Vinay Kumar B.,Kuvempu University | Indira Priyadarsini K.,Bhabha Atomic Research Center | And 3 more authors.
Spectrochimica Acta - Part A: Molecular and Biomolecular Spectroscopy

In the present investigation, a Schiff base N′1, N′3-bis[(Z)-(2-hydroxynapthyl)methylidene]benzene-1, 3-dicarbodihydrazide (L1) and its Co(ii), Ni(ii) and Cu(ii) complexes have been synthesized and characterized as novel photosensitizing agents for photodynamic therapy (PDT). The Interaction of these complexes with calf thymus DNA (CT DNA) has been explored using absorption, thermal denaturation and viscometric studies. The experimental results revealed that Co(ii) and Ni(ii) complexes on binding to CT DNA imply a covalent mode, most possibly involving guanine N7 nitrogen of DNA, with an intrinsic binding constant Kb of 4.5 × 104 M1 and 4.2 × 104 M 1, respectively. However, interestingly, the Cu(ii) complex is involved in the surface binding to minor groove via phosphate backbone of DNA double helix with an intrinsic binding constant Kb of 5.7 × 10 4M 1. The Co(ii), Ni(ii) and Cu(ii) complexes are active in cleaving supercoiled (SC) pUC19 DNA on photoexposure to UV-visible light of 365 nm, through 1O2 generation with quantum yields of 0.28, 0.25 and 0.30, respectively. Further, these complexes are cytotoxic in A549 lung cancer cells, showing an enhancement of cytotoxicity upon light irradiation. © 2013 Elsevier B.V. All rights reserved. Source

Bheemappa E.,Sir Mv Government Science College | Aswathanarayanappa C.,Kuvempu University | Bodke Y.D.,Kuvempu University | Peethamber S.K.,Kuvempu University
Der Pharma Chemica

The novel bridged bicyclic morpholine derivatives, 4-benzyloctahydropyrrolo-[3,4-b][1,4]oxazine derivatives (6a-j) have been synthesized in six steps. The target compounds (6a-j) were obtained by reacting active intermediate 4-benzyloctahydropyrrolo-[3,4-b][1,4]oxazine (5) with various alkyl or aryl halide substituents in the presence of potassium carbonate. Thesebridged bicyclic morpholineswhich were fused to an additional hetero ring, pyrrolidinewere screened for their antibacterial and antifungal potency. These derivatives,N-substituted with cyclohexomethyl, isopropyl, p-methylbenzyl and phenylethylexhibited promising antimicrobial activity; compounds 6a-c were effective against the tested bacterial strains; compounds 6a, 6c, 6g were effective against antifungal strains; and compounds 6d and 6e were not active for these studies. Source

Aswathanarayanappa C.,Kuvempu University | Aswathanarayanappa C.,Biocon | Bheemappa E.,Sir Mv Government Science College | Bodke Y.D.,Kuvempu University | And 2 more authors.
Der Pharma Chemica

Phenethylamidediesters (2-6) were synthesized by reacting [3-ethoxy-4-(ethoxycarbonyl)phenyl]acetic acid with a series of C-protected aminoacids viz., Alanine, Proline, Phenylalanine, Tyrosine and 2-amino-5-(benzyloxy)-5-oxopentanoic aciddiesters and these compounds were hydrolyzed using sodium hydroxide to their respective diacids (7-11). The newly synthesized compounds were tested for antimicrobial activity against Escherichia coli, Staphylococcus Aureus, Pseudomonas Aeruginos, Aspergillus Flavus, ChrysosporiumKeratinophilum, Candida Albicansand antioxidant activity by DPPH method. Compounds 6, 7, 8, and 11 were most active as antimicrobials and 6, 10 and 11have shown promising antioxidant activity. Source

Aswathanarayanappa C.,Biocon | Aswathanarayanappa C.,Kuvempu University | Bheemappa E.,Sir Mv Government Science College | Bodke Y.D.,Kuvempu University
Organic Process Research and Development

A scalable process for the diastereoselective reduction of the prochiral enone intermediate 1 has been developed with DEANB/(R)-methyl CBS as reducing agent, to obtain the key intermediate alcohol 15R-isomer 2, used in a process for the manufacture of Travoprost (3). Various advantages of this process against the DMSB reduction assisted by (R)-methyl CBS have been studied. Specific comparison has been made to highlight the salient features of the chosen process on yield and optical purity with those of the DMSB reduction. © 2011 American Chemical Society. Source

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