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Explore 4 research publications tagged with this keyword
Publications Tagged with "1"
4 publications found
2020
1 publicationSynthesis of Some Novel 1, 5-Benzothiazepine Derivatives Biological Screening For Anticonvulsant Activity
ABSTRACTThe presence of recurrent seizures is responsible for epilepsy, further which has been characterized in the era. A seizure can be mention as “an episodic disturbance of movement, feeling, or consciousness caused by sudden synchronous, inappropriate, and excessive electrical discharges in the cerebral cortex” 1. Epileptic convulsions are expected to have negative consequences on the patient’s psychological and social life such as relationships, education and employment. Uncontrolled seizures are associated with physical and psychosocial morbidity, dependent behavior, poor quality of life and an increased risk of sudden unexpected death. The heterocyclic compound is a potential compound for the development of chemotherapeutic and pharmacotherapeutic agents containing nitrogen and sulphur atoms2. Therefore the present investigation was made in direction to the synthesis of some newer 1, 5-benzothiazepine derivatives and their evaluation for anticonvulsant activity. Physicochemical and elemental analysis of all the 1, 5-benzothiazepine (1B-10B) is confirmed with a preliminary study like melting point, elemental analysis and hyphenated tool namely IR, NMR and Mass spectroscopy. Firstly Primarily, ?,?-unsaturated carbonyl compounds or chalcones were prepared by the well-known Claisen-Schmidt condensation of acetophenones and substituted aldehyde by using alcoholic KOH (10%) at room temperature. By adding diazonium salt in substituted chalcone ,substituted diazonium chalcone was prepared. A yield mixture and 0.01 mole of substituted mercapto anilines was dissolved in 2-methoxyethanol to get final product 1, 5-benzothiazepine derivatives. These molecules were evaluated for possible anticonvulsant activity. Anti-seizure activities of all synthesized compounds 101B to 110B were explored using MES. The synthesized compounds from (101B to 110B) 108B and 109B had shown significant activity against the tonic seizure as compared to the other synthesized compounds. Keywords
2015
1 publicationSynthesis, Characterization and Biological Evaluation of Novel Substituted 1,3,4-Oxadiazoles and 1,3,4-Thiadiazoles as Anthelmintic Agents
The aim of our study was to review on design, synthesis and various pharmacological activities associated with the substituted oxadiazoles and thaidiazoles. Series of 5-(2-Amino-4,5,6,7- tetrahydro-1-benzothien-3-yl) N-substituted 1,3,4-thaidiazole-2-amines(Va-e) were prepared from thiosemicarbazides (IIIa-e) by cyclization using phosphoric acid and 5-(2-Amino-4,5,6,7- tetrahydro-1-benzothien-3-yl) N-substituted 1,3,4-oxadiazole-2-amines (IVa-e) were preparedfrom substituted thiosemicarbazides (IIIa-e)by treating with Iodine &NaOH. Compounds (IIIa-e) were prepared by treating 2-amino-4,5,6,7-tetrahydrobenzo[b]thiophene-3-carbohydrazide (II) with isothiocyanates.Compound II was synthesized by treating ethyl 2-amino-4,5,6,7-tetra hydrobenzeno [b]thiophene-3-carboxylate (I) with hydrazinehydrate. Compound I was prepared by one pot synthesis fromcyclohexanone,sulphur,ethylcyanoacetate in presence of diethyl amine. All the synthesized compounds were charecterized by IR, NMR and mass spectrometry and screened for and in vitro-antihelmintic activity. They showed moderate to good anthelmintic activity against Indian earthworm Pheretimaposthuma.
2014
2 publicationsSynthesis, Characterization and Evaluation of Anti-Microbial Activity of Some Novel 1,2,4-Triazoles.
Some novel 4-(aryliidineamino)-5-(1-(4-isobutylphenyl) ethyl)-4-yl-4H-1,2,4-triazole-3-thiols were prepared from the reaction of carbon-di-sulphide and hydrazine hydrate in water to produce thiocarbohydrazides. The thiocarbohydrazides is then refluxed with ibuprofen for 2 hour, followed by cooling to room temperature and washing with sodium bicarbonate solution to produce 5-(1-(4-isobutylphenyl) ethyl)-4H-1,2,4- triazole-3-thiole. It is then refluxed with different aldehydes in the presence of ethanol and HCl to produce the title compounds. The synthesized compounds are recrystallized from ethanol and are analyzed for their physical and spectral data. They are screened for their anti-microbial activity and it was found that the title compounds are found to have moderate to good antimicrobial activity.
Synthesis and Biological study of Substituted 1, 2, 4-Triazolines and their acetyl derivatives
In the reaction of isoniazid with different aldehydes the respective N1-((un)-substituted benzilidene) isoniazid derivatives were obtained. Further reaction with N1-((un)-substituted benzilidene) isoniazids and hydrazine hydrate yielded dihydroformazans. These dihydroformazans on reaction with N-phenylisocynodichloride in chloroform medium led to the creation of 1, 2, 4-triazolines. All these 1,2,4-triazolines were further converted into their acetyl derivatives by reacting them with acetic anhydride. The structures of all new compounds were confirmed by using elemental and spectral analysis. All the compounds were screened for their antifungal activities.
