Synthesis and Biological Evaluation of New 2,3-Dihydrothiazole Derivatives for Antimicrobial, Antihypertensive, and Anticonvulsant Activities

Omar, A.-Mohsen M.E.; Eshba, N. H.

doi:10.1002/jps.2600730837

Cited by 41 publications

(17 citation statements)

References 5 publications

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“…Various 2-imino-1,3-thiazolines are associated with diverse pharmacological activities such as antimicrobial, anti-inflammatory, antihistaminic, antihypertensive, hypnotic, and anticonvulsant activity [1][2][3][4][5][6]. Thiazolidinone derivatives of rhodanine are reported to have antibacterial, antiviral, pesticidal, anti-inflammatory and anti-diabetic properties [7][8][9][10].…”

Section: Introductionmentioning

confidence: 99%

Synthesis, crystal structure of some new 2‐(4‐methylbenzoylimino)‐3‐aryl‐4‐methyl‐1,3‐thiazolines

Saeed

Parvez

2006

Journal of Heterocyclic Chem

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, 4-Cl, 4-Br An efficient, straightforward synthesis of some new 2-(4-methylbenzoylimino)-3-aryl-4-methyl-1,3-thiazolines (2a-i) is described. The methodology involves the cyclization of 1-(4-methylbenzoyl)-3-arylthioureas with acetone in the presence of bromine and triethylamine. The structures were confirmed by spectroscopic data, elemental analyses and in one case (2i) by the single crystal X-ray diffraction data.

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Section: Introductionmentioning

confidence: 99%

Synthesis, crystal structure of some new 2‐(4‐methylbenzoylimino)‐3‐aryl‐4‐methyl‐1,3‐thiazolines

Saeed

Parvez

2006

Journal of Heterocyclic Chem

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“…A QSAR is a mathematical relationship between a biological activity of a molecular system and its geometric and chemical characteristics. QSAR attempts to find consistent relationships between biological activity and molecular properties, so that these rules can be used to evaluate the activity of new compounds 3D models are more easily interpretable than 2D descriptor or fingerprint-based QSAR models, making it easier to suggest new compounds for synthesis [12,13].…”

Section: Introductionmentioning

confidence: 99%

“…In addition, many thiazoline derivatives exhibit a wide variety of biological activities such as antimicrobial [15], anti-inflammatory [16], antihistaminic [17], antihypertensive [18], hypnotic [19], and anticonvulsant [20], etc. In view of the fact that 4-hydroxybenzohydrazide ring possess antimycobacterial activity and as a part of our ongoing studies in the area of antibacterial and antitubercular agents [21] we have synthesized some N'-[3-(4-substituted alkyl/aryl-4-oxo-1,3-thiazolidin-2-ylidene]-4-hydroxy benzohydrazide (4a -i) and N'-[-(3,4 disubstituted)-1,3-thiazol-2ylidene)]-4-hydroxybenzohydrazide compounds from (5.a -i) to (10.a -i) with the aim of obtaining the new broad spectrum antimicrobial agents, which will devoid of side effects associated with current therapy.…”

Section: Introductionmentioning

confidence: 99%

Synthesis, Antimycobacterial Activity and 3‐D QSAR Studies of Some New Derivatives of p‐Hydroxybenzohydrazide

Bhole¹,

Bhusari²

2009

QSAR Comb. Sci.

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Various N'-[3-(4-substituted alkyl/aryl thiaiazolidin-2-ylidene]-4-hydroxy benzohydrazide (4.a -i) and N'-[-(3,4-disubstituted)-1,3-thiazolidin-2ylidene)]-4-hydroxybenzohydrazide from (5.a -i) to (10.a -i) were synthesized using appropriate synthetic route. The entire test compounds (4.a -i) and compounds from (5.a -i) to (10.a -i) were assayed in vitro against H 37 Rv strain of M. tuberculosis. The minimum inhibitory concentration (MIC) was determined for test compounds and for reference standards. The test compounds showed significant antimycobacterial activity against the microbial strains used, when tested in vitro. In general, p-hydroxybenzohydrazide ring and substituted thiazoline ring are essential for antimicrobial activity. Among the compounds tested, compounds 5.i, 6.f, 7.d, 8.g and 9.f were found to be most potent. The test compounds were found to be nontoxic up to a dose level of 1000 mg/mL. All compounds were then subjected for 3D-QSAR studies. 3D-QSAR study based on the principal of alignment of pharmacophoric features by Schrodinger PHASE module. The 3D-QSAR study allowed us to confirm the preferential binding mode of p-hydroxybenzohydrazide inside the active site.

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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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Synthesis and Biological Evaluation of New 2,3-Dihydrothiazole Derivatives for Antimicrobial, Antihypertensive, and Anticonvulsant Activities

Cited by 41 publications

References 5 publications

Synthesis, crystal structure of some new 2‐(4‐methylbenzoylimino)‐3‐aryl‐4‐methyl‐1,3‐thiazolines

Synthesis, crystal structure of some new 2‐(4‐methylbenzoylimino)‐3‐aryl‐4‐methyl‐1,3‐thiazolines

Synthesis, Antimycobacterial Activity and 3‐D QSAR Studies of Some New Derivatives of p‐Hydroxybenzohydrazide

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

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