Nutan Sharma

Synthesis and in vitro antimicrobial evaluation of novel fluorine-containing 3-benzofuran-2-yl-5-phenyl-4,5-dihydro-1H-pyrazoles and 3-benzofuran-2-yl-5-phenyl-4,5-dihydro-isoxazoles

In the present study, some novel fluorine-containing heterocycles incorporating benzofuran with dihydropyrazoles and dihydroisoxazoles have been synthesized and evaluated for their in vitro antibacterial and antifungal activities. 2-Acetylbenzofuran on treatment with fluorinated aldehydes afforded corresponding fluorine-containing 1-benzofuran-2-yl-3-phenyl-prop-2-en-1-ones (chalcones 5a–g). The cyclocondensation of chalcones (5a–g) with hydrazine hydrate under basic conditions resulted in formation of corresponding novel fluorine-containing 3-benzofuran-2yl-5-phenyl-4,5-dihydro-1H-pyrazoles (6a–g). Similar reaction with hydroxylamine hydrochloride yielded 3-benzofuran-2yl-5-phenyl-4,5-dihydro-isoxazoles (7a–g). All the synthesized compounds have been characterized on the basis of analytical and spectral data, and were screened for their antibacterial and antifungal activities. Some of the synthesized compounds showed good antibacterial and antifungal activities.

Synthesis of Some Salicylaldehyde-Based Schiff Bases in Aqueous Media

A new efficient and environmental friendly procedure for the synthesis of a series of salicylaldehyde-based schiff bases under microwave irradiation is described. The method is compared with the conventional method also. The present work involves condensation of salicylaldehyde with various aromatic amines in water under microwave irradiation. A judicious choice of the solvent and reaction conditions allowed the final products to be generated in excellent yields in a one-step procedure, whereas experiments under thermal conditions led to lower yields with tedious work-up. Microwave irradiation method gives advantages like reduction in reaction time, increase in conversion, reduced wastes, and good yields. The structures of synthesized compounds were confirmed by IR, 1HNMR, and Mass Spectra data.

Strategic synthesis and in vitro antimicrobial evaluation of novel difluoromethylated 1-(1, 3-diphenyl-1H-pyrazol-4-yl)-3, 3-difluoro-1, 3-dihydro-indol-2-ones

A strategic synthesis of 1-(1,3-diphenyl-1H-pyrazol-4-yl)-3,3-difluoro-1,3-dihydro-indol-2-ones has been achieved by the reaction of indole-2,3-dione (isatin) and substituted bromoacetyl benzene followed by cyclization reaction and evaluated for in vitro antibacterial and antifungal activities. Direct fluorination using diethylaminosulfur trifluoride as a nucleophilic fluorinating reagent was carried out in the present paper. Undoubtedly this methodology gives a facile and straightforward pathway to construct 1-(1,3-diphenyl-1H-pyrazol-4-yl)-3,3-difluoro-1,3-dihydro-indol-2-ones in good yields. The structure of new fluorinated 1-(1,3-diphenyl-1H-pyrazol-4-yl)-3,3-difluoro-1,3-dihydro-indol-2-ones was characterized based on 1H, 13C, and 19F nuclear magnetic resonance spectroscopy and mass spectrometry data. Structure of target compound was confirmed by Nuclear Overhauser Effect Spectroscopy spectra. Some of the synthesized compounds showed good antimicrobial activities against bacteria and fungi.

Microwave Assisted Synthesis and in vitro Antimicrobial Activities of Fluorine Containing 4-Benzofuran-2-yl-6-phenyl-pyrimidin-2-ylamines

A series of new analogs fluorine containing heterocyclic system viz. 4-benzofuran-2-yl-6-phenyl-pyrimidin-2- ylamine has been synthesized and evaluated for in vitro antibacterial and antifungal activities. Microwave assisted Claisen-Schmidt condensation of 2-acetylbenzofuran (3) with fluorinated benzaldehydes (4) afforded corresponding fluorinated chalcones (5a-g). The cyclocondensation of chalcones with guanidine hydrochloride in alkaline media under microwave resulted in the formation of corresponding fluorine containing 4-benzofuran-2-yl-6-phenyl-pyrimidin-2- ylamines (6a-g). All the synthesized compounds have been characterized on the basis of analytical and spectral data and were screened for their antibacterial and antifungal activities. Some of the synthesized compounds showed good antimicrobial activities against bacteria and fungi.

Solid support mediated chemo and regioselective synthesis of 3H-1,5- benzodiazepines from diversely substituted α-oxo ketene dithioacetals

Solvent free, dry media supported synthesis of a series of 4-aryl/heteroaryl-2-methylthio-3H-1,5-benzodiazepines by chemo- and regioselective cyclization of substituted α-oxoketene dithioacetals with o-phenylenediamines is described. The X-ray crystallographic studies confirmed the formation of the cyclized product.

Recent Advances in Development of GPR40 Modulators (FFA1/FFAR1): An Emerging Target for Type 2 Diabetes.

BACKGROUND GPR40, an orphan G-protein coupled receptor that is activated by medium and long-chain fatty acids and is highly expressed in pancreatic islets, adipose depots and the gastrointestinal tract are involved in energy source recognition, absorption, storage and/or metabolism. Since its deorphanization in 2003, G-protein-coupled receptor GPR40 has emerged as a potential target for type II diabetes because it has been hypothesized to participate in the adverse effects of chronic fatty acid exposure on function of β-cell. RESULTS This signifies that G-protein-coupled receptors have recently emerged as novel therapeutic targets in metabolic diseases, such as diabetes, obesity and the metabolic syndrome. Therefore it seems natural that GPR40 represents a potentially attractive target to best meet the need for novel treatments for Type II diabetes. CONCLUSION This review describes recent advances and novel drug discovery approaches in the antidiabetic area, focusing on GPR40 modulators which have been synthesized till date and their Structure-Activity Relationship (SAR).

Eco-friendly reactions in PEG-400: a highly efficient and green approach for stereoselective access to multisubstituted 3,4-dihydro-2(1H)-quinazolines using 2-aminobenzylamines

An efficient and stereoselective synthesis of novel 3,4-dihydro-2(1H)-quinazolines has been developed through cyclization reactions of 2-aminobenzylamines with α-oxoketene dithioacetals using PEG-400 as an inexpensive, easy to handle, non-toxic and recyclable reaction medium. The developed protocol is operationally simple and tolerates various substrates having different functionalities. This protocol features several attributes such as excellent yields, no work up, green reaction conditions, and being environmentally benign. The attractive feature of this new strategy is that all the reported final compounds have been isolated as single (E)-stereoisomeric forms, which was confirmed by 1HNMR and X-ray crystallographic studies.