A series of novel 1-(2'-α-O-D-glucopyranosyl ethyl) 2-arylbenzimidazoles has been prepared via one-pot glycosylation of ethyl-1-(2'-hydroxyethyl)-2-arylbenzimidazole-5-carboxylate derivatives. Synthesis of the 2-arylbenzimidazole aglycones from 4-fluoro-3-nitrobenzoic acid was accomplished in four high-yielding steps. The reduction and cyclocondensation steps for the aglycone synthesis proceede...

C-5-bromo-2-hydroxyphenylcalix[4]-2-methylresorcinarene (I) was synthesized by cyclocondensation of 5-bromo-2-hydroxybenzaldehyde and 2-methylresorcinol in the presence of concentrated HCl. Compound I was characterized by infrared and nuclear magnetic resonance spectroscopic data. X-ray analysis showed that this compound crystallized in a triclinic system with space group of Pī, a = 15.9592(16)...

The paper describes the synthesis, antivirus and antitumor evaluation of novel thiazolo[4,5-d]pyrim- idine derivatives. The target compounds 3a-h were synthesized by cyclocondensation of 4-amino-N'-(phenyl- methylidene)-3-phenyl-2-thioxo-2,3-dihydrothiazole-5-carbohydrazides 2a-d with aromatic aldehydes. The structures of new compounds were determined by IR, ¹H-NMR and elemental analysis. Thiaz...

A new series of NH-pyrazoline derivatives 6 was synthesized by cyclocondensation reaction of novel [(7-chloroquinolin-4-yl)oxy]chalcones 5 with hydrazine hydrate. The treatment of pyrazolines 6 with acetic anhydride or formic acid yielded the N-acetyl- or N-formylpyrazoline derivatives 7-8, respectively. These novel 2-pyrazoline derivatives 6-8 were evaluated by the U.S. National Cancer Institu...

Molecular chaperones, such as Hsp70 and Hsp90, are responsible for a variety of protective, anti-apoptotic functions. While inhibitors of Hsp90, such as geldanamycin and its derivative 17-AAG, are well known and important anti-cancer leads, Hsp70 has received less attention. Interesting lead candidates for Hsp70 share a dihydropyrimidine core; however, the preferred display of pendant functiona...

Substituted thiadiazines exert a reliable therapeutic effect in treating stress, and a schematic description of their ability to influence all aspects of a stress response has been depicted. This study was conducted to pharmacologically evaluate compound L-17, a substituted thiadiazine, (2-morpholino-5-phenyl-6H-1,3,4-thiadiazine, hydrobromide) for possible anti-psychotic/antidepressant activit...

The synthesis of novel 6,6'-methylene-bis-[3-(2-anilinoacetyl)-4-hydroxycoumarin] derivatives 6a-f was achieved in excellent yields from 6,6'-methylene-bis-[3-(2-bromoacetyl)-4-hydroxycoumarin] 5 and various arylamines. 5,5'-Methylene-bis-ethylsalicylate 3 was obtained by the esterfication of 5,5'-methylene-bis-salicylic acid 2 with ethanol, which was in turn obtained from salicylic acid 1 and ...

The key intermediate in this study is synthesis of pyrimidine-5-sulfonamides 2a,b. Further modification of starting material by treatment with ethanolamine, anthranilic acid and 3-bromopropanoic acid yielded the condensed pyrimidine derivatives incorporating sulfonamide moiety such as: imidazopyrimidine 3a,b, pyrimidoquinazoline 4a,b and pyrimidothiazine derivatives 5a,b, respectively, in good ...

The three components one pot synthesis of 2-amino-4H-benzo-[b] -pyran derivatives were obtained in good to excellent yields within short reaction time by condensing dimedone, aldehydes and malanonitrile or ethylcyanoacetate using a catalytic amount of (diacetoxyiodo)benzene as hypervalent iodine in aqueous ethanol under reflux conditions have been discussed. This aqua mediated Knoevenagel-cyclo...