Sir Mv Government Science College

Bhadravathi, India

Sir Mv Government Science College

Bhadravathi, India
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Kumaraswamy M.N.,Sir Mv Government Science College | Vaidya V.P.,Kuvempu University | Chandrasekhar C.,Sdm College | Prathima Mathias D.A.,IDSG Government College | Mahadevan K.M.,Kuvempu University
Research Journal of Pharmaceutical, Biological and Chemical Sciences | Year: 2013

The reaction of naphtho[2,1-b]furan-2-carbohydrazide 2, which in turn was synthesized from ethyl naphtho[2,1-b]furan-2carboxylate 1, with various aromatic aldehydes in refluxing dioxane afforded N-[(aryl)methylene]naphtho[2,1-b] furan-2-carbohydrazides 3a-f. These hydrazones 3a-f on treatment with chloroacetyl chloride in presence of triethylamine produced, title compounds, azetidinone derivatives 4a-f. The structures of the newly synthesized compounds have been established by analytical and spectral studies and investigated for antibacterial, antifungal, anti-inflammatory, diuretic, anthelmintic and antipyretic activities.

Dharshan J.C.,Sir Mv Government Science College | Vishnumurthy K.A.A.,Sir Mv Government Science College | Bodke Y.D.,Kuvempu University | Vagdevi H.M.,Sahyadri Science College Autonomous | And 2 more authors.
Der Pharma Chemica | Year: 2012

A series of 7-methoxy quinoline-4-substituted 1, 2, 3-triazoles have been synthesized by 1, 3-dipolar cycloaddition reaction of 4-azido-7-methoxy quinoline 2 with acetyl acetone and ethyl acetoacetate, respectively. The reaction of 2 with acetyl acetone afforded 1-(1-(7-methoxyquinolin-4-yl)-5-methyl-1H-1, 2, 3-triazol-4-yl) ethanone 3 and with ethyl acetoacetate afforded ethyl 1-(7-methoxyquinolin-4-yl)-5-methyl-1H-1, 2, 3-triazol-4-carboxylate 5. Compound 3 upon condensation with aromatic aldehydes gave 1-aryl (1-(7-methoxyquinolin-4-yl)-5-methyl-1H-1, 2, 3-triazol-4-yl) prop-2-en-1-ones 4a-f. Compound 5 is converted into its hydrazide 6 which upon further reaction with different aromatic aldehydes furnished Schiff's bases, N-{1-arylmethylene}-1-(7-methoxy quinolin-4-yl)-5-methyl -1H-1,2,3-triazol-4-carbohydrazides 7a-f. The structure of newly synthesized 1, 2, 3-triazole derivatives have been characterized by IR, 1H NMR, 13C NMR and Mass spectral data. The synthesized compounds have been screened for antimicrobial activities.

Jayanna N.D.,Sahyadri Science College Autonomous | Vagdevi H.M.,Sahyadri Science College Autonomous | Dharshan J.C.,Sir Mv Government Science College | Prashith Kekuda T.R.,Sahyadri Science College Autonomous | And 2 more authors.
Journal of Chemistry | Year: 2013

A new class of 5,7-dichloro-1,3-benzoxazole derivatives 4-11 were synthesized by fusing 5,7-dichloro-2-hydrazino-1,3-benzoxazole 3 nucleus with aliphatic acids, active methylene compounds, and with selected esters to form heterocyclic ring systems like 1,2,4-triazoles, pyrazoles, and triazine moieties. The compound 3 on diazotization reaction affords the tetrazole compound. The synthesized compounds were characterized by 1H NMR, IR, Mass, and 13C NMR spectral data and screened for cytotoxic, antimicrobial, antioxidant, and antilipase activities. The compounds 4, 5, and 8 have shown significant antimicrobial activities, whereas compounds 6 and 8 have been emerged as leading cytotoxic agents. The compounds 9, 10, and 11 were found to be strong enzyme inhibitors. © 2013 N. D. Jayanna et al.

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 | Year: 2013

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.

Jayanna N.D.,Sahyadri Science College | Vagdevi H.M.,Sahyadri Science College | Dharshan J.C.,Sir Mv Government Science College | Kekuda T.R.P.,Sahyadri Science College
Journal of Chemistry | Year: 2013

Some novel 1-(5,7-dichloro-1,3-benzoxazol-2-yl)-1H-pyrazolo[3,4-b]quinoline derivatives 8(a-f) were synthesized by reacting 5,7-dichloro-2-hydrazino-1,3- benzoxazole 4 and substituted-2-chloro-3-quinoline carbaldehydes using p-toluenesulfonic acid (PTSA) as a catalyst for the cyclisation. The target molecules have been characterized by IR, 1H NMR, 13C NMR, and mass spectral studies. The synthesized compounds were screened for biological activities, and some of the compounds have exhibited encouraging antibacterial and antioxidant activities. The compounds 8a and 8e showed potent antibacterial activity, whereas the compounds 8e and 8f act as antioxidants. © 2013 N. D. Jayanna et al.

Bheemappa E.,Sir Mv Government Science College | Aswathanarayanappa C.,Kuvempu University | Bodke Y.D.,Kuvempu University | Peethamber S.K.,Kuvempu University
Der Pharma Chemica | Year: 2014

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.

Aswathanarayanappa C.,Biocon | Aswathanarayanappa C.,Kuvempu University | Bheemappa E.,Sir Mv Government Science College | Bodke Y.D.,Kuvempu University
Organic Process Research and Development | Year: 2011

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.

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 | Year: 2012

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.

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 | Year: 2013

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.

Shruthi S.D.,P.A. College | Shruthi S.D.,Kuvempu University | Shruthi S.D.,Indian Institute of Science | Sujan Ganapathy P.S.,Bangalore University | And 4 more authors.
Journal of Applied Pharmaceutical Science | Year: 2014

Kirganelia reticulata is a useful shrub having various medicinal properties. In vivo, in vitro and in silico antiarthritic activity of a phytoconstituent, ellagic acid (EA) isolated from the leaves of K. reticulata was screened. EA is a naturally occurring plant polyphenol found at high concentrations that act as potential protectors against variety of human diseases. Formaldehyde induced paw edema, assumed to be one of the most suitable test procedures to screen chronic anti-inflammatory agents as it closely resembles human arthritis, and was employed for this study. The course of treatment was followed for over and 4 weeks post inoculation period using health, clinical and behavioural methods of study. Estimation of change in body weight was considered as health parameters and clinical observations included paw edema volume, change in the movements was studied in behavioural observations. The effect of EA was compared with standard drug aspirin. Various in vitro models such as inhibition of protein denaturation, effect of membrane stabilization and proteinase inhibitory actions were studied. EA with two different concentrations (100 μg/ml and 250 μg/ml) was used and results were compared with acetyl salicylic acid. Hypoxia-inducible factor (HIF-2α) promotes degradative pathways that foster osteoarthritis. The inhibitory effect of EA was studied using automated docking and efficiency was compared with standard drug in terms of interaction and binding. The isolated compound EA showed anti-arthritic activity which was found to be significant to that of the standard drugs and supports the traditional use of plant for rheumatism. © 2014 Shruthi SD et al.

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