Tartte Vijaya

Synthesis and antimicrobial activity of 3-aroyl-4-heteroaryl pyrroles and pyrazoles

Abstract A variety of bis heterocycles-heteroaryl pyrazoles (5) and pyrroles (6) were prepared from heteroaryl chalcones adopting 1,3-dipolar cycloaddition reaction and studied their antimicrobial activity. The compounds 5d and 5f having bromo and nitro substituents on the aromatic ring are the potent antimicrobial agents against Bacillus subtilis and Aspergillus niger.

Microwave-assisted neat synthesis of α-aminophosphonate/phosphinate derivatives of 2-(2-aminophenyl)benzothiazole as potent antimicrobial and antioxidant agents

GRAPHICAL ABSTRACT ABSTRACT A series of diethyl/ethylphenyl {2-(benzo[d]thiazol-2-yl)phenylamino}phosphonates and phosphinates were synthesized under microwave irradiation and neat conditions via Kabachnik-Fields reaction in high yields (80%–93%). The compounds were screened for antimicrobial and antioxidant properties. A few compounds showed effective antibacterial and antifungal activities at MIC value 12.5 μg/mL as compared with the standard at MIC value 6.25 μg/mL.

Synthesis and antioxidant activity of bis and tris heterocycles.

A variety of bis heterocycles, oxazolyl/thiazolyl/imidazolyl oxadiazoles having a styryl sulfonylmethyl group at the 5‐position of oxadiazole and tris heterocycles having a pyrrolyl/pyrazolyl sulfonylmethyl group at the 5‐position of oxadiazole were prepared adopting simple and versatile synthetic methodologies. All the compounds were screened for their antioxidant activities. Compound 5b displayed radical scavenging activity in all the three methods greater than the standard ascorbic acid, whereas compounds 8b and 14b showed activities equal to the standard ascorbic acid.

Leptin inhibitors from fungal endophytes (LIFEs): Will be novel therapeutic drugs for obesity and its associated immune mediated diseases.

Treatment of obesity and its associated immune mediated diseases is challenging due to impaired function of leptin system. Thus leptin is providing an interesting target for therapeutic intervention. Leptin, an adipose tissue-derived adipokine, displays a variety of immune functions, and regulate both innate and adaptive immune responses. The increased secretion of leptin (hyperleptinemia) and production of proinflammatory cytokines has been implicated in the pathogenesis of obesity-related immune diseases such as diabetes mellitus, hypertension, atherosclerosis, cancer, systemic lupus erythematosus, rheumatoid arthritis, crohns disease and multiple sclerosis. These disorders are managed through antibiotics and by cytokines replacement. However, the effectiveness of cytokines coupled to the complexity of the cytokine network leads to severe side-effects, which can still occur after careful preclinical evaluation. In addition, synthetic immunotherapeutics carries a degree of risk, is time-consuming and expensive. Hence, the complexity of existing therapy and adverse effects emphasizes the need of an alternative approach for the management of immune dysfunction associated with obesity and its related diseases. For the aforementioned diseases that are related to leptin overabundance, new drugs blocking leptin signaling need to be generated. The research on the discovery of clinically important novel compounds from natural source is expanding due to their safety and no side effect. The fungal endophytes are the microbes that colonize internal tissue of plants without causing negative effects to the host. They produce plethora of substances of potential use to modern medicinal and pharmaceutical industry. The increasing body of evidence associated with application of bioactive metabolites derived from fungal endophytes in diverse disease states merits its use as therapeutic drugs. In particular, the saponins have been extensively proved to modulate the immune system, which has raised a significant interest in their potential as immunomodulators. Thus, our hypothesis is that the saponins derived from fungal endophytes can be explored as clinical applicable leptin inhibitors for treating immune mediated diseases.

Synthesis and characterization of new thiourea and urea derivatives of 6-fluoro-3-(piperidin-4-yl)benzo[d] isoxazole: In vitro Antimicrobial and Antioxidant activity

AbstractA new class of antimicrobial and antioxidant agents, based on thiourea and urea derivatives of 6-fluoro-3-(piperidin-4-yl)benzo[d] isoxazole were synthesized by adopting a simple and efficient method. Synthesized compounds were characterized by spectral data of IR, 1H, 13C NMR and mass spectra. The compounds were evaluated for their efficacy as antimicrobial and antioxidant agents. A few compounds showed good antibacterial, antifungal and antioxidant activity when compared to standard drugs and thus represent a new class of promising lead compounds. Graphical AbstractA new series of thiourea and urea derivatives of 6-fluoro-3-(piperidin-4-yl)benzo[d] isoxazole were synthesized in a convenient way. The in vitro antimicrobial activity of the title compounds were screened against selected organisms by disc diffusion technique and the antioxidant activity were evaluated by H2O2 and DPPH Methods.

Isolation and characterization of plumbagin (5- hydroxyl- 2- methylnaptalene-1,4-dione) producing endophytic fungi Cladosporium delicatulum from endemic medicinal plants

Graphical abstract

Synthesis of Novel 2-Amino-N-hydroxybenzamide Antimicrobials

Abstract New 2-amino-N-hydroxybenzamide derivatives (3a–j) have been synthesized in good to excellent yields from the reaction of isatoic anhydride with different hydroxamic acids. All the compounds of the series were screened against both Gram-positive and Gram-negative bacteria and fungi, and some of them have antibacterial and antifungal activities compared to the standard drugs. GRAPHICAL ABSTRACT