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Basappa

Publications and source records attributed to Basappa.

10 recordsLinked to original sources
PubMed2006

Synthesis, characterization, antimicrobial and single crystal X-ray crystallographic studies of some new sulfonyl, 4-chloro phenoxy benzene and dibenzoazepine substituted benzamides.

A new class of benzamide derivatives 3a(I-VI) and 3b(I-VI), bearing different bioactive moieties were synthesized and evaluated for their efficacy as antimicrobials in vitro. Compounds 3bVI, 3aII, 3aV, 3bIII, 3aVI, 3bII showed significant antibacterial activity and 3bIII, 3bII, 3aIV, 3bV, 3bVI, 3aI exhibit significant antifungal activity. The title compounds are characterized by spectral and elemental analysis. Compounds 2-methoxy-N-[4-(thiazol-2-yl-sulfamoyl)-phenyl]-benzamide 3aII and 2-(2-(2-ethoxybenzoylamino) phenethyl)-N-(2-ethoxybenzoyl) benzenamine 3bV are characterized by the single crystal X-ray studies. Compound 3aII crystallizes in monoclinic space group P2(1) and 3bV in triclinic space group P-1. Compounds 3aII and 3bV exhibit both inter and intra molecular hydrogen bonding.

Anti-Bacterial Agents↗
PubMed2006

Synthesis of pharmaceutically important condensed heterocyclic 4,6-disubstituted-1,2,4-triazolo-1,3,4-thiadiazole derivatives as antimicrobials.

The two series of 4,6-disubstituted 1,2,4-triazolo-1,3,4-thiadiazole derivatives 2(a-e) and 3(a-e) were synthesized and characterized using IR, (1)H-NMR, CHNS analysis and by single crystal X-ray crystallographic studies. The compound 6-(2-chloro-phenyl)-3-ethyl-[1,2,4]triazole[3,4-b]thiadiazole 2b has been characterized by single crystal X-ray diffraction method. The compound crystallizes in monoclinic space group P2(1)/c with a cell parameters a = 11.879(1) Angstroms, b = 15.112(2) Angstroms, c = 13.95(2) Angstroms, Z = 8 and the final R factor is R1= 0.0524. The structure exhibits both intra and intermolecular hydrogen bonds. The title compounds were checked for their efficacy as antimicrobials in vitro. Compounds 2b, 2c, 2d, 3b, 3c and 3d showed significant inhibition against all the strains tested, when compared to standard drugs.

Anti-Infective Agents↗
PubMed2005

Synthesis of new bioactive venlafaxine analogs: novel thiazolidin-4-ones as antimicrobials.

A one-pot, three-component, microwave irradiated and conventional solution-phase synthesis of bioactive venlafaxine analogs such as 2,3-disubstituted-1,3-thiazolidin-4-ones 3a-j under mild conditions and their characterization are reported. The novel thiazolidin-4-ones, 3-(2-(1-hydroxycyclohexyl)-2-(4-methoxyphenyl)ethyl)-2-phenyl-thiazolidin-4-one 3a, 2-(2,6-difluorophenyl)-3-(2-(1-hydroxycyclohexyl)-2-(4-methoxyphenyl)ethyl)thiazolidin-4-one 3c, and 2-(furan-2-yl)-3-(2-(1-hydroxycyclohexyl)-2-(4-methoxyphenyl)ethyl)thiazolidin-4-one 3i, were characterized by the single crystal X-ray diffraction method. The cyclohexane ring of all the three molecules is in chair conformation. All the synthesized compounds were screened for their efficacy as antimicrobials in vitro by the disk diffusion and microdilution method against pathogenic strains such as Bacillus subtilis, Escherichia coli, Pseudomonas fluorescens, Xanthomonas campestris pvs, Xanthomonas oryzae, Aspergillus niger, Aspergillus flavus, Fusarium oxysporum, Trichoderma species, and Fusarium monaliforme species. Among these compounds 3c, 3j, 3g, 3d, and 3e showed potent antimicrobial activity, when compared to standard drugs.

Anti-Bacterial Agents↗
PubMed2005

Microwave-assisted synthesis of N-alkylated benzotriazole derivatives: antimicrobial studies.

Synthesis and characterization of N-alkylated benzotriazole derivatives 2(a-g) bearing pharmaceutically important bioactive substituents and their antimicrobial studies in vitro are described. The syntheses of the compounds were achieved by N-alkylation of the benzotriazole with different bioactive alkyl halides in presence of powdered K2CO3 in DMF solution and by microwave irradiation method with good yield compared to conventional method. The crystal structure analysis shows that compound 4'-benzotriazol-1-yl-methyl-biphenyl-2-carbonitrile 2a crystallizes in the space group P1 with cell parameters a = 8.526 (3) A, b = 12.706 (3) A, c = 7.966 (2) A, alpha = 100.89 (2) degrees , beta = 101.63 (3) degrees , gamma = 102.20(2) degrees, Volume = 801.7(4) A degrees , Z = 2 and the final R factor is 0.0559 for 6130 reflections with 218 parameters and zero restraint. This structure exhibits intermolecular hydrogen bonding. Compounds 2e, 2a showed significant antimicrobial activity.

Anti-Bacterial Agents↗
PubMed2005

Synthesis and characterization of novel 6-fluoro-4-piperidinyl-1,2-benzisoxazole amides and 6-fluoro-chroman-2-carboxamides: antimicrobial studies.

Novel derivatives of 6-fluoro-4-piperidinyl-1,2-benzisoxazole amides 4(I-VI) were obtained by the condensation of different acid chlorides with 6-fluoro-3-piperidin-4yl-benzo[d]isoxazole. Also, 6-fluoro-chroman-2-carboxamides 6(I-III) were synthesized by using nebulic acid chloride with different amines in presence of triethylamine as acid scavenger and dichloroethane as solvent. The synthesized compounds were characterized by IR, 1H NMR, and CHN analysis. These molecules were evaluated for their efficacy as antimicrobials in vitro by disc diffusion and microdilution method against pathogenic strains such as Bacillus substilis, Escherichia coli, Pseudomonas fluorescens, Xanthomonas campestris pvs, X. oryzae, Aspergillus niger, A. flavus, Fusarium oxysporum, Trichoderma species, F. monaliforme, and Penicillum species. Compounds 4I, 4IV, 4V, 6I, 6II and 6III showed better inhibitory activity than compared to standard drugs. Among these compounds, 4IV and 6III showed potent inhibitory activity against all the strains and found to be nonstrain dependent. The title compounds represent a novel class of potent antimicrobial agents.

Amides↗
PubMed2004

Novel delta2-isoxazolines as group II phospholipase A2 inhibitors.

The synthesized imidazolyl substituted delta2-isoxazolines were subjected to Phospholipase A(2) (PLA(2)) enzyme inhibitory activity against snake venom source and their structure-activity relationship with respect to different groups attached to this moiety is reported for the first time. The crystal structure of the compound 2-butyl-5-chloro-3H-imidazolyl-4-carbaldehyde oxime 2, an intermediate for the construction of isoxazolines is reported. These compounds exerted a significant PLA(2) enzyme inhibitory activity against group II PLA(2). The in vivo activity on mice of selected compounds 3bI and 3bIV shows the comparable anti-inflammatory activity with the known standard ursolic acid.

Aldehydes↗
PubMed2003

Solution-phase synthesis of novel delta2-isoxazoline libraries via 1,3-dipolar cycloaddition and their antifungal properties.

The synthesis of novel imidazolyl substituted delta2-isoxazoline libraries are currently of high interest. We report here in the full details of a study leading to the synthesis and antifungal activities of 3-(-2-butyl-4-chloro-1H-imidazolyl)-substituted delta2-isoxazolines. The solution phase synthesis of the title compounds was accomplished via 1,3-dipolar cycloaddition of in situ generated nitryl oxides from aldoximes with mono substituted alkenes to obtain the compound libraries contain an imidazole functionality in addition to the isoxazoline rings. The newly synthesized compounds when tested in vitro in solid agar culture exerted a potent antifungal activity against Aspergillus flavus, Fusarium moniliforme and Botrydiplodia theobromae also MIC values were determined. The title 5-substituted-3-imidazolyl-delta2-isoxazoline compounds represent a novel class of potent antifungal agents.

Animals↗
PubMed1996

Cobb syndrome.

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Adult↗