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Arylsydnone 1 a‐b is ring transformed to 1,3,4‐oxadiazole 2 a‐b and further converted to 1,2,4‐triazolones 3 a‐b. Condensation of compound 3 a‐b with aromatic aldehydes followed by reduction yielded a secondary amine derivative 5 a‐d. Subsequent reaction of compound 5 a‐d with formaldehyde and various secondary amines in presence of an acid catalyst afforded mannich bases 6 a‐p. Single crystals of the intermediate compounds (Schiff bases) 4 a and 4 b are obtained and confirmed by x‐ray crystallographic studies. All the final compounds are tested for anti‐tubercular and anti‐fungal activity. Almost all compounds have exhibited good pharmacological activity. In anti‐tubercular activity, especially compounds 6 d and 6 f have shown excellent activities at the drug concentrations 3.12 μg/ml and 6.25 μg/ml respectively. While in antifungal activity against C. albicans, compounds 6 d and 6 m have exhibited good activities at the drug concentrations 6.25 μg/ml and 12.50 μg/ml where as in the antifungal activity against A. fumigatus, only the compounds 6 b and 6 g have exhibited promising activity at the drug concentration 0.20 μg/ml. A series of novel mannich bases were synthesized and characterized by spectral analysis and X‐ray crystallographic studies (intermediate compound 4a and 4b). Mannich bases were screened for antifungal and anti‐tubercular activity. Some of the mannich bases have exhibited potent antifungal and anti‐tubercular activity. [ABSTRACT FROM AUTHOR]

Microwave-assisted green approach is developed for an efficient synthesis of thiazol-2-imines under catalyst-free conditions. The desired products are formed by one-pot three-component reaction which is an improvised method for Hantzsch thiazole synthesis. The microwave-assisted protocol gives excellent yields with high purity in just 10-15 min. All the synthesized compounds have been screened for antifungal activity and some of the derivatives show a broad spectrum against fungal pathogens. [ABSTRACT FROM AUTHOR]

A series of novel coumarin pyrazoline moieties combined with tetrazoles, 3-(1-phenyl-4-(1H-tetrazol-5-yl)-1H-pyrazol- 3-yl)-2H-chromen-2-one, 6-chloro-3-(1-phenyl-4-(1H-tetrazol- 5-yl)-1H-pyrazol-3-yl)-2H-chromen-2-one, 6-bromo-3-(1-phenyl- 4-(1H-tetrazol-5-yl)-1H-pyrazol-3-yl)-2H-chromen-2-one and 6-bromo-3-(1-(4-bromophenyl)-4-(1H-tetrazol-5-yl)-1H pyrazol- 3-yl)-2H-chromen-2-one 7(a-d), were designed and synthesized. Single crystal X-ray diffraction and their interactions were studied by Hirshfeld surface analysis. Thermal stabilities and electrochemical properties of these compounds were examined from differential scanning calorimetry (DSC), thermogravimetric (TGA) and cyclic voltammetric (CV) studies. Their spectroscopic properties were analyzed in various alcohols and general solvents by UV-Vis absorption, fluorescence and time-resolved spectroscopy. In addition, the ground and excited state electronic properties were investigated using density functional theory (DFT). The calculated highest occupied molecular orbital (HOMO) and lowest unoccupied molecular orbital (LUMO) and energy band gap (Eg) values have revealed the effect of substitution of halogens. The substitution has equally affected the ground and excited states of 7(a-d) compounds. The solvatochromism on absorption, fluorescence spectra and fluorescence lifetimes of these compounds was investigated. All these results showed the chromen-2-one of pyrazoline tetrazole derivatives could play an important role in photonic and electronic devices. [ABSTRACT FROM AUTHOR]

Abstract: A series of novel 2,3‐dihydroquinazolin‐4(1H)‐ones 7 a‐g were designed, synthesized and were characterized by IR, 1H & 13C NMR, MS, and elemental analysis. The optical and electrochemical properties have been studied using UV‐Vis absorption, fluorescence spectroscopy, life time and cyclic voltammetry (CV) measurements. Quantum yield and effect of solvents for the compounds 7 a‐g were investigated. Density Functional Theory (DFT) computations have been carried out for all the synthesized compounds and the computed values found to be approximately in close agreement with the experimental results. Further, the compounds 7 a, 7 d, 7 f and 7 g were evaluated for their anticancer activity at National Cancer Institute, NIH, Bethesda, USA and have shown moderate to good anticancer activities. [ABSTRACT FROM AUTHOR]

The present study emphasizes on the dealklylation of 3-aryl-5-alkyl-2-oxo-Δ4-1,3,4-oxadiazoles when reacted with formamide resulting in the formation of 2-aryl-2 H-1,2,4-triazol-3(4 H)-ones as major product. Subsequent reactions of 2-aryl-2 H-1,2,4-triazol-3(4 H)-one gave triazolo[3,4- b][1,3,4]thiadiazoles and triazolo[3,4- b][1,3,4]thiadiazines derivatives incorporated with 1,2,4-triazol-3-one. [ABSTRACT FROM AUTHOR]

In the present paper 5-[4′-({4-[(4-aryloxy)methyl]-1 H-1,2,3-triazol-1-yl}methyl)[1,1′-biphenyl]-2-yl]-1 H-tetrazoles ( 5a- g) and [2′-(1 H-tetrazol-5-yl)[1,1′-biphenyl]-4-yl]methyl-substituted-1-carbodithioates ( 11h- q) have been designed and synthesized. These compounds were subjected to docking (against AT receptor protein enzyme in complex with Lisinopril), in vitro angiotensin converting enzyme inhibition, anti-proliferative, anti-inflammatory screening (through egg albumin denaturation inhibition and red blood cell membrane stabilization assay) and finally anti-fungal activity analyses. Some of the compounds have shown significant pharmacological properties. [ABSTRACT FROM AUTHOR]

A series of novel benzo[ a]xanthen-11(12 H)-one derivatives 4a- m were designed and subjected to docking studies. The title compounds were synthesized from 3-aryl-4-formylsydnones 1a- m, β-naphthol and dimedone in presence of molecular iodine as a catalyst and evaluated for their in vitro inhibitory effects on the hyaluronidase. [ABSTRACT FROM AUTHOR]

Coumarins appended to benzimidazole through pyrazole are designed and synthesized using microwave irradiation. These compounds were analyzed for phosphodiesterase (PDE) inhibition indirectly by motility pattern in human spermatozoa. Some of the synthesized compounds, namely, 5d, 5e, 5f, 5g, 5h, and 5k, have exhibited potent inhibitory activity on PDE. [ABSTRACT FROM AUTHOR]