Synthesis, anti-inflammatory, ulcerogenic and cyclooxygenase activities of indenopyrimidine derivatives.

Objective of the present work was to evaluate the anti-inflammatory, ulcerogenicity and cyclooxygenase activity of indenopyrimidine derivatives. Anti-inflammatory activity of the tested compounds is investigated by carrageenan-induced rat paw edema assay. Compounds A1, A6, A7 and A12 exhibit the comparable anti-inflammatory activity (79.33-81.33%) to the standard drug diclofenac sodium (85.33%), while A6, A7, A9, A12 and A14 show better ulcer index than the reference standard diclofenac sodium. To rationalize the anti-inflammatory activity, docking experiments are performed to study the ability of these compounds to bind into the active site of COX-2 enzyme.

Synthesis of some novel quinone diimine derivatives of benzo-15-crown-5 for application in Hg(2+) recognition.

A series of novel fluoroionophore bearing derivatives of benzo-15-crown-5 were synthesized by the amination of benzo-15-crown-5 followed by condensation with different quinones in the presence of titanium tetrachloride (TiCl4 ) and 1,4-diazabicyclo-[2.2.2]octane. The compounds were characterized by infrared, (1) H and (13) C nuclear magnetic resonance, mass spectroscopy and elemental analysis. Absorption and fluorescence spectral characteristics of these compounds were studied. It was observed that the anthraquinone derivative was acting as an Hg(2+) ion sensor.

Synthesis and Antimicrobial Screening of Pyrazolo-3-Aryl Quinazolin-4(3H)ones.

2-thio-3-aryl quinazolin-4(3H)one (1) was synthesized by reacting anthranilic acid with thiocarbamate salts of substituted aniline and carbon disulphide, which on reflux with excess of hydrazine hydrate to form 2-hydrazino quinazolin-4(3H)one derivatives (2). The reaction of (2) with variously substituted aryl aldehydes gave the corresponding hydrazones (3). Further, the cyclization of compound (3) in acetic anhydride gave tricyclic pyrazoloquinazolinones (4). All newly synthesized compounds have been tested for their antibacterial activity against gram +ve bacteria B. substilis, S. aureus and gram -ve bacteria E. coli, P. vulgaris. The species used for antifungal activity are Aspergillus niger and Phytophora. Introduction of -OCH3, -OH and -Cl groups to the heterocyclic frame work enhanced antibacterial and antifungal activities.

A novel and efficient one step synthesis of 2-amino-5-cyano-6-hydroxy-4-aryl pyrimidines and their anti-bacterial activity.

The first simple and efficient approach towards one step synthesis of 2-amino-5-cyano-6-hydroxy-4-aryl pyrimidines has been developed by three component condensation of aromatic aldehydes, ethyl cyanoacetate and guanidine hydrochloride in alkaline ethanol. The synthesized compounds evaluated for their anti-bacterial activity against gram-positive and gram-negative bacteria. The some of the compounds showed excellent zone of inhibition against tested bacteria.

Histological changes in thyroid of rat under the acute exposure of O-chloro-benzylidine malononitrile.

This communication describes histological changes in the thyroid gland of rats under the acute stress of O-chlorobenzylidene malononitrile (CS) 10 mg/kg and 20 mg/kg). It has been observed that CS, when injected, causes histological changes in the thyroid of varying degrees, depending on the dose used.

Cellular changes of adrenal under the acute stress of O-chlorobenzylidene malononitrile (CS).

This investigation describes histological and cytometrical changes of cortical and medullary tissue of adrenal in rats under the acute stress of O-chlorobenzylidene malononitrile (10 mg/kg and 20 mg/kg). It has been observed that after injection of CS, the adrenal gland showed histological changes both in the cortical and medullary region.