Synthesis and anticonvulsant activity of some ureido thiazolidine and thiohydantoin derivatives of furochromones

The synthesis of several urea derivatives 2,3a-c, 8a-i and 9a-b from 9-amino-4-hydroxy-7-methyl-5H-furo [3,2-g] [1] benzopyran-5-one is described. In addition, 2-[[4-hydroxy-5H-furo [3,2-g] [1] benzopyran-5-one-9-yl] imino] thiazolidin-4-one 5 and its thiohydantoin congener 6 have been prepared. Some of the synthesized compounds were tested for their anticonvulsant activity against pentylenetetrazole-induced seizures in albino mice. Compound 5 showed anticonvulsant activity comparable to that of phenobarbital. In addition, glutamate content of mice brains after treatment with 5 was determined. Anticonvulsants represent a group of diverse chemical compounds. The majority of conventional anticonvulsant drugs have a dicarboximido [-CONHCO-] or a ureido [-NHCONH-] function as in hydantoins, barbiturates, succinimides and oxazolidinediones. In addition, the anticonvulsant properties of certain carboxylic acids and their amides are well documented. The local anesthetic amides lidocaine is clinically effective in the treatment of status epilepticus. Furthermore, certain thiazolidinones and thiohydantoins are known to exert anticonvulsant activity. On the other hand, some aminochromones antagonize the action of leptazol and are therefore interesting as anticonvulsants. Consequently, the present article deals with the synthesis and the study of anticonvulsant activity of certain ureido, thiazolidinone and thiohydantoin derivatives of the aminofurochromone 1

Synthesis hypotensive and antispasmoclic activities of certain aminomethyl chromones

Several drugs available for the treatment of hypertension lower the peripheral vascular resistance either through an inhibition of the sympathetic activity via an influence on adrenoreceptors in the CNS or a direct vasodilating effect on the smooth muscles in the arterioles. Khellin, the most important furochromone isolated from Ammi visnaga L., and its analogues exert a direct spasmolytic action on a variety of smooth muscles including those of blood vessels. Some of 6-aminomethyl derivatives of khellin and a combination of khellin and barbiturates produced sustained hypotensive action. On the other h and, antispasmodic and beta-adrenergic blocking action have been reported in several types of amino chromones. Accordingly, in a sustained effort to find cardiovascular and antispasmodic agents certain new aminomethylchromones and furochromones have been synthesized and tested for their hypotensive and antispasmodic activities

Synthesis and pharmacological activities of certain new pyrazole and chromone derivatives

In this investigation, some new chromone and pyrazole derivatives have been synthesized by the action of hydrazine hydrate on certain substituted chromones. Some of the synthesized compounds showed marked analgesic, anti-inflammatory and antipyretic activities

Synthesis and antispasmodic effect of certain furochromones

Synthesis of certain 4-hydroxy or 4-methoxy-7-methyl-9-substituted 5- H-furo [3, 2-g] [1] benzopyran-5-one has been achieved. The antispasmodic activity of some representative examples was carried out and some of them showed marked activity

Synthesis and hypotensive activity of certain benzofuran derivatives

Some 6-hydroxy -4- methoxy -7- morpholinomethylbenzofuran derivatives with various 5- cinnamoyl or heterocyclic substituents have been prepared. The hypotensive activity of some of the synthesized compounds was evaluated

Synthesis and in vitro cytotoxic activity of 9- [substituted sulphonyl hydrazinomethylene] -10-methyl acridinium methosulphates and 9- [substituted sulphonyl hydrazinomethylene] acridine-10-oxides

The synthesis of two series of 9-[substituted sulphonyl hydrazinomethylene]-10-methyl acridinum methosulfates and 9-[substituted sulphonyl hydrazinomethylene] acridin-10-oxides was reported. Preliminary testing for the in vitro cytotoxic activity of 6 representative examples against Ehrlich asites carcinoma was carried out. All the tested compounds showed in vitro cytotoxic activity with reference to that of melphalan

9-substituted acridines: synthesis, antimicrobial and cytotoxic activities

1-[9-acridyl]-4-substituted thiosemicarbazides V and 1-[4-[9- acridylamino] benzoyl]-4-substituted thiosemicarbazides VI were prepared by condensation of 9-hydrazino acridine II and 9-[p- hydrazinocarbonyl anilino] acridine IV with alkyl or arylisothiocyanate. The 1,3-thiazolidin-4-one derivatives VII and VIII were prepared by cyclocondensation of V and VI with chloroacetyl chloride. Reaction of 9-acridine carboxaldehyde X with different arylsulphonyl hydrazides afforded N2-arylsulphonyl-9-acridine carboxaldehyde hydrazones XI. Antimicrobial and cytotoxic activities of some representative compounds were carried out

Hydrazones, thiosemicarbazides, thiosemicarbazones and 1,3-thiazolidin-4-ones derived from acridine synthesis, cytotoxic and antimicrobial activities

Reaction of 9-hydrazinomethylacridine and 9-acridine carboxaldehyde hydrazone III, IV with aromatic aldehydes or ketones afforded 9- arylidene hydrazinomethylacridines and N2-arylidene-9-acridine- carboxaldehyde hydrazones V, VIII, while reaction of III and IV with alkyl or aryl isothiocyanate afforded 1-[9-acridinomethyl]4-substituted thiosemicarbazides and 1-[acridine carboxaldehyde] 4-substituted thiosemicarbazones VI and IX. The 1,3-thiazolidin-4-one derivatives VII and X have been prepared by cyclocondensation of VI and IX with chloroacetyl chloride. Some of the prepared compounds were evaluated for their in vitro cytotoxic and antimicrobial activities

Synthesis cytoxic and antimicrobial activities of some 9-amilino acridines and 9- [p-arylidene hydrazine] acridines

The synthesis of three series of 9-[p-arylidene hydra- zinocarbonylanilino] acridines, 9-p-N2 substituted thiocarbamoylhydrazinocarbonylanilino] acridines and 9-p-arylidene hydrazino] acridines was described. Some of the synthesized compounds were screened for their cytotoxic and antimicrobial activities. The screening revealed that blocking of the hydrazino or the hydrazide groups decreases or abolishes both the cytotoxic and the antimicrobial activities