Ca(II)-Catalyzed Cascade Reaction of Tryptamines with Propargylic Alcohols: Temperature-Driven Ring Opening and Closing via the Allene Migration Pathway for the Synthesis of Pyrrolo[1,2-a]indoles.

A temperature-dependent cascade of reactions between tryptamines and propargylic alcohols was developed to achieve selective formation of pyrroloindoline and pyrrolo[1,2-a]indole heterocycles by Ca(II) catalysis. The cascade consists of electrophilic addition of allene at the C3 carbon of indole followed by intramolecular cyclization at 60 °C to yield pyrroloindolines. Furthermore, simultaneous 1,2-allene migration and pyrrolidine ring opening were followed by intramolecular cyclization via C-N bond formation at reflux temperature to obtain pyrrolo[1,2-a]indole scaffolds. A wide range of substrates, a clean reaction profile, scalability, and good to excellent yields are the advantages of this protocol.

Na2S-promoted reduction of azides in water: synthesis of pyrazolopyridines in one pot and evaluation of antimicrobial activity.

Reduction of various azides using Na2S has been accomplished in water, and, in situ, the resulting amines on reaction with various ketones lead to pyrazolo[3,4-b]pyridines in one pot. Thus, a number of new trifluoromethyl-substituted pyrazolo[3,4-b]pyridine compounds have been prepared and screened for antimicrobial activity against different Gram-positive and Gram-negative strains. A good number of compounds, 4a, 4b, 4d, 4f, 4i, 4k, 4l, 4m, 4r and 4s, were found to possess promising activity. Notably, Na2S on hydrolysis in water generates H2S and NaOH, which facilitate the reduction of azides followed by intramolecular cyclization leading to the title compounds. To the best of our knowledge, this is the first report of the synthesis of the title compounds in aqueous medium in a one-pot reaction.

A study on zoonotic tuberculosis in selected rural areas of Bagalkot and Belgaum districts of Karnataka state.

The close association of cattle/buffaloes to farmers and their family members is a well-known phenomenon in rural India. Cattle are major contributors to the income for the sustenance of families, and for many landless farmers, often the only source of livelihood. The animals are sheltered under the same roof where the family members sleep, cook and eat. This close proximity of humans to cattle/buffaloes exposes farmers and family members to tuberculosis (TB), especially if they are vulnerable (e.g. malnourished children along with adults, diabetics, people with HIV/AIDS, people with addiction to alcohol, or smokers) . Several studies have examined the risk factors that are associated with TB, such as crowding (slum dwellers), poor living conditions, alcohol, and tobacco . Other studies have found a significant proportion of diabetic patients with coexistent TB. This study examines the spread of TB from animals to humans and its public health significance. To achieve this, selected numbers of cattle/buffaloes were tested for TB and the association with humans and animals was examined.

A simple, one pot synthesis of furo[3,2-c]chromenes and evaluation of antimicrobial activity.

Synthesis of a number of 2-cyano-4-oxo-3-phenyl-3,4-dihydro-2H-furo[3,2-c]chromene-2-carboxylate compounds (5) have been accomplished by a simple, multicomponent one pot reaction and evaluated for in vitro antimicrobial activity against different Gram-positive and Gram-negative bacterial strains. The outcome of the screening study showed that compound 5c exhibited promising activity against Micrococcus luteus MTCC 2470 and Klebsiella planticola MTCC 530. Whereas, compound 5g exhibited excellent activity against Bacillus subtilis MTCC 121, Micrococcus luteus MTCC 2470, Klebsiella planticola MTCC 530, Escherichia coli MTCC 739 and displayed a moderate activity against Staphylococcus aureus MTCC 96 and Candida albicans MTCC 3017 when compared with Ciprofloxacin (standard control).

One pot oxidative N-S bond formation to access 2-sulfenylimine chromenes.

The synthesis of 2-sulfenylimine chromene compounds (8) is accomplished by reacting benzaldehyde (1), malanonitrile (2) and dimedone (3) followed by sequential addition of N-chlorosuccinimide and thiophenols to the in situ formed 2-amino-4(H) chromenes (4) in a one pot, catalyst free, five component reaction in toluene medium. When aniline was employed as the nucleophile in place of thiophenol, the formation of hexahydrobenzofuran-2-N-phenyl carboxamide derivatives (5) was observed. Excellent yields, simple reaction conditions and high compatibility are the advantages of this protocol.

Physiological taste threshold in type 1 diabetes mellitus.

The sense of taste is one of the important oral chemical senses that play a critical role in human life. The taste threshold increases by number of factors such as age, local and systemic disease like diabetes, consumption of alcohol, smoking. The aim of the present study was to assess the relationship between taste threshold in type 1 diabetics and non diabetics for four basic taste modalities (i.e. sweet, salt, sour and bitter). We studied 70 cases of type 1 diabetic and 70 non diabetics. The taste threshold was evaluated using 7 different serially half diluted concentrations of glucose (2.00 M-0.031 M), Nacl (1.00 M-0.0156 M), citric acid (0.05 M-0.0007 M) and quinine sulphate (0.001 M-0.000015 M). A significant increase in taste threshold for sweet (P<0.0001), salt, sour and bitter (P<0.001) in type 1 diabetic was observed. We concluded that taste sensation was reduced in type 1 diabetics.