DESIGN, SYNTHESIS AND PSYCHOPHARMACOLOGICAL ACTIVITY OF QUINOLIN-2-ONE DERIVATIVES

Starting material 4-hydroxy-1-phenyl/methyl-quinolin-2-(1H)-one was treated with phosphorous oxychloride and then subjected to Mannich reaction to yield title 4-chloro-1-phenyl/methyl-3-[3- (substituted) propanoyl] quinolin-2(1H)-one derivatives compounds IIa (1-7)/ IIb (1-7). Molecular docking studies of the compounds were carried out using Molegro Virtual Docker. All the synthesized compounds were characterized by IR, 1H-NMR and Mass Spectral data and were tested for their antidepressant activity. Amongst the synthesized compounds, compound 4-chloro-1-phenyl-3-[3-(morpholinopropanoyl] quinolin-2(1H)-one [IIa4] was found to show the most potent antidepressant activity with immobility time of 98.17± 4.806. Compound 4-chloro-1-phenyl-3-[3-(4- methylpiperazin-1-yl) propanoyl] quinolin-2(1H)- one [IIa 3] and 4-chloro-1-methyl-3-[3-(pyrrolidin-1-yl) propanoyl] quinolin-2(1H)-one [IIb 2] showed moderate antidepressant activity with immobility time of 126.5 ± 1.945s and 120.3 ± 2.376s, respectively, compared to standard imipramine.

Synthesis, Antibacterial Activity and Molecular Docking of Phospholidinones in Stigmastane Series

<P>Introduction: Steroid compounds are widely distributed in nature throughout scientific history. Living organisms such as animals and vegetables have steroids that show a significant effect on their vital activities. Sterols are key components of all eukaryotic cell membranes. Methods: Steroidal compounds; 3β-oxo-[1’,3’,2’-oxathiaphos-phalidine-2’-one] stigmast-5-ene and 3β- oxo[1`,3`,2`-dioxaphosphalidine-2`-one]-stigmast-5-ene were successfully prepared using easily accessible 3β-hydroxy stigmast-5-ene with phosphorous oxychloride (POCl3), 2- mercaptoethanol/ethylene glycol and triethylamine (Et3N) in dry diethyl ether. Products were obtained in semi-solid state and characterized using physicochemical techniques. Results: The results of the bioassay showed that the synthesized compound containing the sulfur atom had antibacterial activity. Molecular docking was also done in order to show in silico antibacterial activity and to make out the probable binding mode of compound with the amino acid residues of protein. Conclusion: The results of the docking study showed that synthesized compound 2 had minimal binding energy with substantial affinity for the active site.</P>

3-(3,5-Difluorophenyl)-1-phenyl-1H-pyrazole-4-carbaldehyde

Vilsmeier&ndash;Haack reaction of (E)-1-(1-(3,5-difluorophenyl)ethylidene)-2-phenylhydrazine (1) using dimethyl formamide in excess of phosphorous oxychloride by conventional method, resulted in the synthesis of title compound 3-(3,5-difluorophenyl)-1-phenyl-1H-pyrazole-4- carbaldehyde (2) in good yield and high purity. Structure characterization of the novel title compound was done by IR, 1H NMR, 13C NMR and mass spectral analysis.

Synthesis, Characterization and Study of Mesomorphic Behavior of New Bent and Liner Core Compounds Containing Heterocyclic

We described herein the synthesized and characterized of new bent and liner core compounds containing thiazolidin-4-one ring[XI-XIII] and [XIV-XVI] respectively. These compounds synthesized by sequence reactions starting from reaction resorcinol or hydroquinone with chloracetyl chloride to yield compounds [I] and [II] ,then the later compounds reactant with 4-hydroxybenzylaldehyde to product dialdehyde compounds [III] and [IV] .The Schiff bases compounds[V-VII] and [VIII-X] synthesized from reaction the compound [III] or [IV] with different aromatic amines, while the bent and liner core mesogens containing thiazolidin-4-one ring [XI-XIII] and [XIV-XVI] synthesized from reaction Schiff bases compounds[V-VII] or [VIII-X] with thioglycolic acid. In addition estrfecation of cinnamic acid with methanol to yield ester compound[XVII]which was converted to their acid hydrazid[XVIII] and the acid hydrazid reacted with glysine in phosphorous oxychloride to yield (5-styryl-1,3,4-oxadiazol-2-yl) methanamine [XIX]. Then reactant the1,3,4-oxadiazol compound[XIX] with dialdehyde compound [III] or [IV] to product new Schiff bases compounds [XX] and [XXI] , afterword added thioglycolic acid to give new thiazolidin-4-one derivatives [XXII] and [XXIII], respectively. The synthesized compounds were characterized by melting points , FTIR ,1HNMR and mass spectroscopy (of some of them).The liquid crystalline properties were studied by hot stage polarized optical microscopy (POM) and differential scanning calorimetry(DSC).All the Schiff bases compounds [V-X] showed liquid crystals phases while thiazolidin-4-one derivatives[XI-XIII],[XIV-XVI]and [XXIII] didn’t show any liquid crystals properties except the compound [XXII] showed enantiotropic nematic phase.

Crosslinking of starch and its effect on viscosity behaviour

Starch is a widely used component in the food industry. Native starch does not have the desired properties, so it is modified according to the required properties. Out of different methods, crosslinking is one of the widely used ones. There are different crosslinking agents available. The method and mechanism of widely used crosslinking agents like phosphorous oxychloride, adipate and epichlorohydrin are discussed and compared. When starch is crosslinked, its properties vary. The extent of crosslinking can be predicted with the help of properties like viscosity and swelling. They are also compared for crosslinking by different agents.

Synthesis and in vivo Anti-inflammatory and Analgesic activities of Oxadiazoles clubbed with Benzothiazole nucleus

The aim of the present work is to synthesize and evaluate the anti-inflammatory and analgesic activity of 2-(5-substituted-1,3,4-oxadiazole-2-yl)-1,3-benzathiazole derivatives. In the present investigation, a series of 2-(5-substituted-1,3,4-oxadiazole-2-yl)-1,3-benzathiazole derivatives (3a1-3a9) were synthesized by condensing benzothiazolyl carboxyhydrazide and appropriate aryl acids in the presence of phosphorous oxychloride. Structures of synthesized compounds were established on the basis of IR, 1H NMR, and Mass spectroscopy. All the synthesized compounds were screened for their in-vivo anti-inflammatory and analgesic activities at the dose of 50 mg/kg and 10 mg/kg po. The biological result shows that some compounds were good in their anti-inflammatory and analgesic actions.Kumar et al., International Current Pharmaceutical Journal, November 2015, 4(12): 457-461

Synthesis, Characterization and Screening of Anti-tubercular activity of 2, 5-Disubstituted-1, 3, 4-Oxadiazole

The synthesis of 2-furyl-5-(substituted)-1,3,4-oxadiazoles was carried out by microwave irradiation of 2-furoic acid and ethanol followed by subsequent hydrazinolysis with hydrazine hydrate. Finally furan-2-acid hydrazide was treated with appropriate carboxylic acid in the presence of phosphorous oxychloride to produce title compounds. The structures of the newly synthesized compounds were established on the basis of spectral analysis such as IR, H1NMR and Mass spectral data. The synthesized compounds were screened for their anti-tubercular activity.

Facile protection-free one-pot synthesis of 7-deaza-2′-deoxyguanosine-5′-triphosphate — A versatile molecular biology probe

A simple, straightforward, reliable, and efficient protection-free “one-pot, three-step” chemical synthesis of 7-deaza-2′-deoxyguanosine-5′-triphosphate (7-deaza-dGTP) is described. The reaction involves monophosphorylation of 7-deaza-2′-deoxyguanosine using phosphorous oxychloride as the phosphorylating agent, followed by reaction with tributylammonium pyrophosphate, and subsequent hydrolysis affords 7-deaza-2′-deoxyguanosine-5′-triphosphate in a 52% yield with high purity (>99.9%).