Studies of the stability properties of 2-docosylamino-5-nitropyridine monolayers have shown that three-dimensional structures are formed from the monolayer material over a wide surface pressure region between 2 and 25 mN m−1. Constant surface pressure relaxation experiments are analysed on the b...

Azanucleosides, sugar-modified nucleoside analogues containing a 4′ nitrogen atom, have shown a lot of therapeutic potential, e.g. as anti-cancer and antiviral agents. We report the synthesis of a series of 2’-homoazanucleosides, in which the nucleobase is attached to the 2’-position of the p...

The hydrogenation of 5,5-dimethyl-2-phenyl-[1,3]dioxane to 3-benzyloxy-2,2-dimethyl-propan-1-ol has been investigated within the temperature range from 150°C to 220°C over copper-loaded catalysts. Under elevated pressure in a continuous flow reactor, good results have been obtained using the c...

As an integrator of multiple nociceptive and/or inflammatory stimuli, TRPV1 is an attractive therapeutic target for the treatment of various painful disorders. Several TRPV1 antagonists have been advanced into clinical trials and the initial observations suggest that TRPV1 antagonism may be asso...

Gain-of-function mutations of receptor tyrosine kinase KIT play a critical role in the pathogenesis of systemic mastocytosis (SM) and gastrointestinal stromal tumors. D816V KIT mutation, found in ∼80% of SM, is resistant to the currently available tyrosine kinase inhibitors (TKIs) (e.g. imatini...

Peptidomimetic-based macrocycles typically have improved pharmacokinetic properties over those observed with peptide analogs. Described are the syntheses of 13 peptidomimetic derivatives that are based on active sansalvamide A structures, where these analogs incorporate heterocycles (triazoles, ...

Searching novel, safe and effective anti-inflammatory agents has remained an evolving research enquiry in the mainstream of inflammatory disorders. In the present investigation series of thiazoles bearing pyrazole as a possible pharmacophore were synthesized and assessed for their anti inflammat...

Organic compounds containing five-membered aromatic heterocyclic rings play an important role in life science. Among them thiazole and isothiazole heterocycles are present in many pharmaceutical drugs and crop protection compounds and have sparked over past years an enormous interest on these sc...

BackgroundAbolition of cancer warrants effective treatment modalities directed towards specific pathways dysregulated in tumor proliferation and survival. The antiapoptotic Bcl-2 proteins are significantly altered in several tumor types which position them as striking targets for therapeutic int...

Novel N-methylated valine-thiazole cyclic octa- and dodecapeptides are produced by cyclooligomerisation of a N-methylated-l-valine thiazole amino acid HCl in the presence of pentafluorophenyl diphenylphosphinate (FDPP).

The 4,5-dihydro-1,3,4-oxadiazole-2-thiones derivatives, 2-phenyl-1-(5-sulfanylidene-4,5-dihydro-1,3,4-oxadiazol-2-yl)ethenyl]benzamide(Ic), 4-methyl-N-[(Z)-1-(5-sulfanylidene-4,5-dihydro-1,3,4-oxadiazol-2-yl)-2-(thiophen-2-yl)ethenyl]benzamide-N,N-dimethylform amide (1/1) (IIc) and 1-(5-sulfanyl...

Combined nano zinc oxide and titanium dioxide [nano (ZnO–TiO2)] has been reported first time for the synthesis of novel series of 4,5,6,7-tetrahydro-6-((5-substituted-1,3,4-oxadiazol-2-yl)methyl)thieno[2,3-c]pyridine. All the synthesized compounds (7a–7m) are novel and were screened for their ...

Two novel series of 3-((5-phenyl-1,3,4-oxadiazol-2-yl)methyl)-2-thioxothiazolidin-4-one derivatives were designed and synthesized, and their anti-bacterial activities evaluated. These compounds showed broad-spectrum inhibitory activities against both Gram-positive and Gram-negative bacteria with...

This article demonstrates the synthesis, characterization and the study of in vitro antitubercular activities of twenty four new N-(4-(5-aryl-3-(5-methyl-1,3,4-oxadiazol-2-yl)-1H-pyrazol-1-yl)phenyl)-4-amide derivatives (8a–x). The antitubercular activity of the compounds against Mycobacterium ...

Bioisosteric replacement of acylureido moiety in 6-acylureido-3-pyrrolylmethylidene-2-oxoindoline derivatives resulted in a series of malonamido derivatives with indolin-2-one scaffold (11–14). Further conformational restrictions of the malonamido moiety led to 2-oxo-1,2-dihydropyridine (21–25...

A series of 1-aroylindoline-hydroxamic acids have been synthesized in the present study. The results of the biological evaluation led to the identification of compound 12 as dual HDAC6/HSP90 inhibitor. Compound 12 displayed striking inhibitory effects towards the HDAC6 isoform and HSP 90 protein...

A simple and efficient cascade Michael/cyclization reaction of 3-aminoindolin-2-ones with enones/enals was identified for the synthesis of potentially biologically active 3′,4′-dihydrospiro[pyrrol-3,2′-oxindoles], using DBU as an efficient catalyst and ethylene glycol as an environmentally be...

The 1,3-dipolar cycloaddition of an azomethine ylide, generated from isatin and benzylamine by a 1,5-prototopic shift route with various p-substituted 2,6-bis(arylmethylidene)cyclohexanones under different conditions, proceeded regioselectively to give novel dispiroheterocycles. The product on s...

We previously showed that 2,6-bis-(4-hydroxyl-3-methoxybenzylidine)cyclohexanone (BHMC), suppressed the synthesis of various proinflammatory mediators. In this study we explain the mechanism of action of BHMC in lipopolysaccharide (LPS)-induced U937 monocytes and further show that BHMC prevents ...

Differential scanning calorimetry and wide-angle X-ray diffractometry first revealed the formation of hetero-stereocomplex (HTSC) between biodegradable, optically active, and isotactic poly(2-hydroxyalkanoic acid)s having different chemical structures and opposite configurations, i.e., l-configu...