The ac conductivity and dielectric response of bulk vanadyl 2,3-naphthalocyanine (VONPc) were investigated from 1 Hz to 106 Hz, at temperatures range from 288 K to 403 K. Thermal stability of the material was studied using thermogravimetric analysis (TGA). The structure phase was investigated us...

Following i.p. treatment with saline, 10 or 20 mg/kg 1-benzylpiperazine, or 1 or 2 mg/kg methamphetamine, hooded rats were observed in an open field, a light–dark box and (24 h after exposure to the drugs) a Y maze with one novel and one familiar arm. Both drugs increased open-field rearing and...

From 30 days after birth until the completion of the study, male and female rats were caged in same-sexed twos or threes either with (enriched cages, EC) or without several objects for them to explore (standard cages, SC). From 41 to 50 days of age (late adolescence), they received a daily intra...

There is diversity in clinical outcome of Helicobacter pylori infection in different regions. Microbial, host and environmental factors seem to be reason of such variation. Considering microbial factors, we studied H. pylori genotypes and their association with clinical feature of the infection....

Conformationally restricted analogues of the positive inotropic agent 1 have been synthesized in order to determine its biologically active conformation. Comparison of the distance maps (as a tool for the allowed conformations) with the biological activity give new insights in the biologically a...

The design, synthesis and evaluation of novel thieno[2,3-d]pyrimidin-4-yl hydrazone analogues as cyclin-dependent kinase 4 (CDK4) inhibitor are described. Focusing on the optimization of the heteroaryl moiety at the hydrazone with substituted phenyl groups, 4-[(methylamino)methyl]benzaldehyde (2...

The wide spectrum antibacterial 3-fluoro-d-alanine (S)-9 has been stereoselectively synthesized via “chiral sulfoxide chemistry”. Key steps are the azidation of the α-fluoro α′ -sulfinyl alcohol (2S,Rs)-1 under Mitsunobu conditions and the one-pot transformation of the N-Cbz α-sulfinyl ami...

We have previously discovered nicotinic acid derivative 1 as a structurally novel dipeptidyl peptidase IV (DPP-4) inhibitor. In this study, we obtained the X-ray co-crystal structure between nicotinic acid derivative 1 and DPP-4. From these X-ray co-crystallography results, to achieve more poten...

Nitroterephthalic acid (H2ntp), 2,5-dibromoterephthalic acid (H2bdc) and N,N′-donor ligands have been employed to synthesize three uranyl compounds: (H2-tmp)[(UO2)(ntp)2]·H2O (1), (2,2′-Hbpy)[(UO2)2(ntp)2.5]·H2O (2) and [(UO2)(bdc)(4,4′-bpy)0.5] (3) [where 2,2′-bpy = 2,2′-dipyridyl, 4,4′...

A facile, efficient and environment-friendly protocol for the synthesis of 4-hydroxy-6-methyl-3-(1-(phenylimino)ethyl)-2H-pyran-2-one derivatives has been developed by the convenient ultrasound-mediated condensation of amine with dehydroacetic acid. This method provides several advantages over c...

An investigation of absorption and fluorescence behaviour of 6-amino-3-methyl-4-(4-nitrophenyl)-1,4-dihydropyrano[2,3-c]pyrazole-5-carbonitrile (NDPPC) at room temperature was carried out using a series of twelve organic solvents with different polarities. Ground and excited state dipole moments...

A collection of paullones was tested for inhibitory activity against mitochondrial malate dehydrogenase (mMDH) as a biological target for antiproliferative activity. Based on the results of this screening, 5-benzylpaullones and paullone-9-carboxylic acid alkyl esters were developed as selective ...

Diaryl piperazine acetamides were identified as potent and selective dopamine D4 receptor agonists. Our strategy is based on an amide bond reversal of an acid sensitive, dopamine D4 receptor partial agonist, PD 168077. This reversal provided compounds with excellent potency and improved stabilit...

The design, synthesis, and SAR study of a new series of HIV-1 protease inhibitors incorporating stereochemically defined tetrahydrofuran-tertiary amine-acetamide P2-ligand are described. Various substituent effects on the tertiary amine P2-ligand and phenylsulfonamide P2′-ligand were investigat...

2,5-Disubstituted 1,3,4-oxadiazole compounds are one of the most attractive classes for researchers due to their pharmacological activities. In the current research, a new series of 2-[[5-alkyl/aralkyl-1,3,4-oxadiazol-2-yl]thio]-N-[4-(4-morpholinyl)phenyl]acetamides (6a–m) were prepared by conv...

A new series of N-substituted derivatives of 2-[(5-{1-[(4-chlorophenyl)sulfonyl]-3-piperidinyl}-1,3,4-oxadiazol-2-yl)sulfanyl]acetamide (6a-w) has been designed and synthesized with multifunctional moieties. The synthesized compounds were evaluated for their antibacterial and anti-enzymatic pote...

The conformational analysis of some N,N-diethyl-2[(4′-substituted)phenylthio]acetamides bearing the substituents OMe 1, Me 2, H 3, Cl 4, Br 5 and NO2 6, was performed by νCO IR analysis, along with B3LYP/6-311++G(d,p) and Polarisable Continuum Model (PCM) calculations, as well as NBO analysis ...

Current study is based on the sequential conversion of indolyl butanoic acid (1) into ethyl indolyl butanoate (2), indolyl butanohydrazide (3), and 1,3,4-oxadiazole-2-thiol analogs (4) by adopting chemical transformations. In a parallel series of reactions, 2-bromo-N-phenyl/arylacetamides (7a-l)...

A series of novel N-substituted N′-(2-arylmethylthio-4-chloro-5-methylbenzenesulfonyl)guanidines 9–41 have been synthesized and investigated as inhibitors of four isoforms of zinc enzyme carbonic anhydrase (CA.EC 4.2.1.1), that is the cytosolic CA I and II, and cancer-associated isozymes CA IX...

In the continuation of our investigations on the structure of platelet-activating factor (PAF)-receptor, 25 additional 2-substituted 1,4-bis-(poly- and mono methoxybenzoyl)-piperazines were synthesized and their in vitro biological activities measured. Substituent at position 2 is representative...