OF THE THESIS Synthesis, Characterization and Biological Activities Of Novel Hybrid Molecules Related to Substituted Hydrazones, Sulphonamides and Sulphonates of NonSteroidal Anti-Inflammatory Drugs CHAPTER 1 A Brief Overview of Synthesis and Pharmacological Activities of Substituted Hydrazones, Sulphonates and Sulphonamides This chapter deals with general survey of the literature related to th...

Hydrazines and their derivatives are versatile artificial and natural compounds that are metabolized by elusive biological systems. Here we identified microorganisms that assimilate hydrazones and isolated the yeast, Candida palmioleophila MK883. When cultured with adipic acid bis(ethylidene hydrazide) as the sole source of carbon, C. palmioleophila MK883 degraded hydrazones and accumulated adi...

Allylboronic acids directly react with acyl hydrazones, affording homoallylic amine derivatives. The reaction proceeds with very high syn selectivity, which is the opposite of the stereochemistry observed for allylboration of imines. The reaction can be carried out with both aromatic and aliphatic acyl hydrazones. Based on our studies the excellent syn stereochemistry can be explained by chelat...

There has been considerable interest in the development of novel compounds with anticonvulsant, antidepressant, analgesic, antiinflammatory, antiplatelet, antimalarial, antimicrobial, antimycobacterial, antitumoral, vasodilator, antiviral and antischistosomiasis activities. Hydrazones possessing an azometine -NHN=CH- proton constitute an important class of compounds for new drug development. Th...

Isoniazid (INH) is a first-line drug for tuberculosis control; the side effects of INH are thought to be associated with its metabolism, and this study was designed to globally characterize isoniazid metabolism. Metabolomic strategies were used to profile isoniazid metabolism in humans. Eight known and seven novel INH metabolites and hydrazones were identified in human urine. The novel products...

Transition metal complexes containing Schiff base ligands are of interest to model the active sites of biologically important molecules. In particular, Schiff base derivatives of hydrazones exhibit various bioactivities and play vital role in certain physiological functions as well. Hydrazones and their metal complexes exhibit wide range of biological and pharmaceutical activities that includes...

Benzotiazole and pyrimidine have been reported to act as effective pharmacophores. However, much less work as been carried out on these heterocycles fused with each other. In the present study, we report the synthesis of a series of 8-chloro-3(phenylcarbonoimidoyl)-10a-H-pyrimido [2,1-b][1,3]benzothiazole-2-thiol. This series was synthesized by the reaction of 8-chloro-2-sulfanyl-10a-H-pyrimido...

The effects of ethylene gas, 2-chloroethylphosphonic acid, and the auxin, benzothiazole-2-oxyacetic acid, on the ripening of grapes (Vitis vinifera L.) was investigated. Ethylene hastened the start of ripening of Doradillo grapes when it was aplied for 10 days starting midway through the slow growth phase. 2-Chloroethylphosphonic acid applied to Shiraz grapes showed the same effect, but when it...

Berries on field-grown Vitis vinifera cv. Doradillo were treated at different times during stage II with benzothiazole-2-oxyacetic acid or 2-chloroethylphosphonic acid, and measurements were made of their growth and hormone content. The concentration of ethylene was low during stage II and declined as berries ripened. Both 2-chloroethylphosphonic acid and benzothiazole-2-oxyacetic acid caused i...

2-Aminobenzothiazole-6-carboxylic acid (1), on condensation with chloroacetyl chloride yielded 2-(2-chloroacetylamino)benzothiazole-6-carboxylic acid (2), which on amination with hydrazine hydrate yielded in turn 2-(2-hydrazinoacetylamino)benzo-thiazole-6-carboxylic acid (3). Compound 3, on condensation with various aromatic aldehydes afforded a series of 2-{2-[N'-(arylidene)hydrazino]acetylami...