CNS Depressant Activity of Pyrimidylthiazolidones and their Selective Inhibition of NAD‐Dependent Pyruvate Oxidation

Chaudhary, Mahima; Parmar, Surendra S.; Chaudhary, Sunil Kumar; Chaturvedi, Arvind; Sastry, B. V. Rama

doi:10.1002/jps.2600650336

Cited by 43 publications

(16 citation statements)

References 10 publications

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“…In addition, 2-iminothiazolidin-4-ones exhibit remarkable hypnotic [7–8], antitubercular [9], cardiovascular [10] and cyclooxygenase (COX) inhibitory [11] activities (Fig. 1).…”

Section: Introductionmentioning

confidence: 99%

A facile, rapid, one-pot regio/stereoselective synthesis of 2-iminothiazolidin-4-ones under solvent/scavenger-free conditions

Sathishkumar¹,

Nagarajan²,

Shanmugavelan³

et al. 2013

Beilstein J. Org. Chem.

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SummaryA rapid and efficient one pot solvent/scavenger-free protocol for the synthesis of 2-iminothiazolidin-4-ones has been developed. Interestingly, the regio/stereoselective synthesis affords the regioisomeric (Z)-3-alkyl/aryl-2-(2-phenylcyclohex-2-enylimino)thiazolidin-4-one as the sole product in good yield. The selectivities observed have been rationalized based on the relative magnitude of the allylic strains developed during the course of the reaction. This is the first report wherein the impact of allylic strains in directing the regiocyclization has been noted.

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“…In addition, 2-iminothiazolidin-4-ones exhibit remarkable hypnotic [7–8], antitubercular [9], cardiovascular [10] and cyclooxygenase (COX) inhibitory [11] activities (Fig. 1).…”

Section: Introductionmentioning

confidence: 99%

A facile, rapid, one-pot regio/stereoselective synthesis of 2-iminothiazolidin-4-ones under solvent/scavenger-free conditions

Sathishkumar¹,

Nagarajan²,

Shanmugavelan³

et al. 2013

Beilstein J. Org. Chem.

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“…Thus 4-[(2-(3,4-dimethoxyphenyl)ethyl]-3-thiosemicarbazide (2) obtained from a one-pot reaction [9] was condensed with appropriate aldehydes to afford 1-substituted benzylidene/furfurylidene-4-[2-(3,4-dimethoxyphenyl)-ethyl]-3-thiosemicarbazides (3). Cyclization of 3 with chloroacetic acid and oxalyl chloride furnished 2-(substituted benzylidene)/furfurylidenehydrazono-3-[2-(3,4-dimethoxyphenyl)ethyl]thiazolidin-4-ones (4) and 1-(substituted benzylidene)/furfurylideneamino-3-[2-(3,4-dimethoxyphenyl)-ethyl]-2-thioxo-4,5-imidazolidinediones (5), respectively (Scheme 1 and Table 1).…”

Section: Chemistrymentioning

confidence: 99%

“…4-Thiazolidinones are reported to possess anticonvulsant [1] and hypnotic properties [2,3] . Hypnotic activity of cyclic ureides, exemplified by barbiturates which exert their effects mainly by potentiating and/or prolonging the action of the inhibitory transmitter GABA by influencing conductance at the chloride channel associated with the GABA receptor, is well known [4,5] .…”

Section: Introductionmentioning

confidence: 99%

Synthesis and Hypnotic Activity of New 4-Thiazolidinone and 2-Thioxo-4,5-imidazolidinedione Derivatives

Ergenç

Çapan²,

Gunay

et al. 1999

Arch. Pharm. Pharm. Med. Chem.

145

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Conveniently accessible 4‐[(2‐(3,4‐dimethoxyphenyl)ethyl]‐3‐thiosemicarbazide (2) was converted to new 1‐substituted benzylidene/furfurylidene‐4‐[2‐(3,4‐dimethoxyphenyl)ethyl]‐3‐thiosemicarbazides (3) which furnished 2‐(substituted benzylidene/furfurylidene)hydrazono‐3‐[2‐(3,4‐dimethoxyphenyl)ethyl]thiaz‐olidin‐4‐ones (4) and 1‐(substituted benzylidene/furfurylidene)‐amino‐3‐[2‐(3,4‐dimethoxyphenyl)ethyl]‐2‐thioxo‐4,5‐imidazol‐idinediones (5) on reaction with chloroacetic acid and oxalyl chloride, respectively. The structure of 5 was confirmed by X‐ray diffraction studies performed on 5a. 4 and 5 were evaluated for their potentiating effects on pentobarbital induced hypnosis. Most of the compounds caused remarkable increases in pentobarbital sleeping time.

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“…[1] They possess antiinflammatory, [2] antitumor, [3] antihistaminic, [4] antihypertensive, [5] antimicrobial, [6] hypnotic, [7] anticonvulsant, [8] antiparkinsonian [9] activities. Among these starting materials for generating diverse pyrrolidne derivatives, pyrrolidinones [10] showed to be attractive ones as they possess both electrophilic and nucleophilic centers enabling them to react with various reagents.…”

Section: Introductionmentioning

confidence: 99%

Synthesis, Characterization and antimicrobial activity of novel pyrrolidine-3-carbonitrile derivatives,

2018

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NEWLY synthesized pyrrolidine-3-carbonitrile derivatives were evaluated as antimicrobial activity. The structures of these derivatives were derived from reactions of 1-(4-methoxyphenyl)-4-oxopyrrolidine-3-carbonitrile (1) with the stabilized phosphorus ylides, Wittig-Horner reagents, trialkylphosphites, as well as tris(dialkylamino)phosphines. The antimicrobial activity of the synthesized compounds was evaluated against Gram positive, Gram negative bacteria and fungi. The results showed comparable antibiotic activity to the reference antibiotic compound used in the study.

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CNS Depressant Activity of Pyrimidylthiazolidones and their Selective Inhibition of NAD‐Dependent Pyruvate Oxidation

Cited by 43 publications

References 10 publications

A facile, rapid, one-pot regio/stereoselective synthesis of 2-iminothiazolidin-4-ones under solvent/scavenger-free conditions

A facile, rapid, one-pot regio/stereoselective synthesis of 2-iminothiazolidin-4-ones under solvent/scavenger-free conditions

Synthesis and Hypnotic Activity of New 4-Thiazolidinone and 2-Thioxo-4,5-imidazolidinedione Derivatives

Synthesis, Characterization and antimicrobial activity of novel pyrrolidine-3-carbonitrile derivatives,

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