Synthesis, biological evaluation of new oxazolidino-sulfonamides as potential antimicrobial agents

Kamal, Ähmed; Swapna, P.; Shetti, Rajesh V.C.R.N.C.; Shaik, Anver Basha; Rao, Ming; Gupta, Soma

doi:10.1016/j.ejmech.2013.01.034

Cited by 47 publications

(33 citation statements)

References 32 publications

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“…Their work included docking studies using the crystal structure of an agonistb ound to the ligand-binding domain of the PPARa receptor.T he docking study revealed that the carbonyl group of the oxazolidinone was in close proximity to the hydroxy group of the lateral chain of Tyr464, which donated ah ydrogen bond and stabilised the complex. [58,59] In one, Bhattaraie tal. Their modulard esign comprised three parts-a polar head, al inker,a nd ah ydrophobic tailand in the majority of the ligands, they incorporated the oxazolidinone moiety as anovel polar head group.…”

Section: Pharmacological Profile Of Oxazolidinone Derivativesmentioning

confidence: 99%

The Current Status of O‐Heterocycles: A Synthetic and Medicinal Overview

Singh

Silakari

2018

ChemMedChem

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O-Heterocycles have been explored in the field of medicinal chemistry for a long time, but their significance has not been duly recognised and they are often shunned in favour of N-heterocycles. The design of bioactive molecules for nearly every pathophysiological condition is primarily focused on novel N-heterocycles. The main reasons for such bias include the ease of synthesis and possible mimicking of physiological molecules by N-heterocycles. But considering only this criterion rarely provides breakthrough molecules for a given disease condition, and instead the risks of toxicity or side effects are increased with such molecules. On the other hand, owing to improved synthetic feasibility, O-heterocycles have established themselves as equally potent lead molecules for a wide range of pathophysiological conditions. In the last decade there have been hundreds of reports validating the fact that equally potent molecules can be designed and developed by using O-heterocycles, and these are also expected to have comparably low toxicity. Even so, researchers tend to remain biased toward the use of N-heterocycles over O-heterocycles. Thus, this review provides a critical analysis of the synthesis and medicinal attributes of O-heterocycles, such as pyrones, oxazolones, furanones, oxetanes, oxazolidinones, and dioxolonones, and others, reported in the last five years, underlining the need for and the advantages guiding researchers toward them.

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Section: Pharmacological Profile Of Oxazolidinone Derivativesmentioning

confidence: 99%

The Current Status of O‐Heterocycles: A Synthetic and Medicinal Overview

Singh

Silakari

2018

ChemMedChem

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“…The precipitate obtained was filtered off and washed with cold water several times, dried and recrystallized from the appropriate solvent (Scheme 1 and 2). [1,2,4] triazolo [1,5- [1,5- …”

Section: General Procedures For Synthesis Of Compounds 4a 4b 10 and 14mentioning

confidence: 99%

“…Elemental analyses were carried out at the Microanalytical Center of Cairo University. Ethyl 6-cyano-7-(4-methoxyphenyl)-5-oxo-2-thioxo-1,2,3,5-tetrahydro [1,2,4]triazolo [1,5-a]pyridine-8-carboxylate [48] (1) and 2-(chloromethyl)benzimidazole or 2-(chloromethyl) benzooxazole (2a,b) were prepared according to the reported literature [49][50][51] (Scheme 1).…”

Section: Instrumentationmentioning

confidence: 99%

“…Heterocycles containing sulfonamide moieties have attracted obvious attention due to their significant biological properties and their role as pharmacohores [1][2][3][4][5][6]. Studies have shown that sulfonamide compounds were used as antibacterial [7][8][9], antifungal [9,10], antiviral [11], anticancer [12], antinflammatory, analgesic [13][14][15], and antibacterial agents [16].…”

Section: Introductionmentioning

confidence: 99%

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Synthesis and antimicrobial evaluation of some 1,2,4-triazolo[1,5-a]pyridine, pyrimidine sulfonamides and sulfinyl derivatives

Abdel-Motaal

Raslan

2014

Eur. J. Chem.

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“…Since it is not practical to perform experimental measurements, it is useful to rapidly predict molecular physicochemical properties before biological evaluation. In order to correlate the biological activity with T1 T2 T3 T4 T5 T6 T7 T8 T9 T10 T11 T12 T13 T14 T15 T16 T17 T18 T19 physicochemical properties, we performed an estimation of molecular properties based on chemical structures [10]. The structures and physicochemical properties such as CLogP, pK a solubility, and polar surface area (PSA) values are listed in Table 1.…”

mentioning

confidence: 99%

Design, Synthesis, and Biological Evaluation of Chalcone Derivatives as Novel Anticandidal Agents

et al. 2015

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Twenty chalcone derivatives were designed and synthesized with a view to developing novel anticandidal agents. All the compounds were evaluated for their antifungal activity against Candida albicans (ATCC 10231 and ten clinical isolates). Most of them exhibited moderate anticandidal potency with MIC values ranging from 2.0 to 32.0 Pg/mL. Four compounds (T4, T6, T19, T20) displayed potent anticandidal activity with MIC values of 2.0 Pg/mL. Compound T6 showed the most potent activity against Candida albicans (ATCC 10231 and four clinical isolates). In addition, attempts have also been made to correlate anticandidal activity to physicochemical properties. The results indicated that incorporation of halogen on the benzene ring is beneficial for anticandidal activity.

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Synthesis, biological evaluation of new oxazolidino-sulfonamides as potential antimicrobial agents

Cited by 47 publications

References 32 publications

The Current Status of O‐Heterocycles: A Synthetic and Medicinal Overview

The Current Status of O‐Heterocycles: A Synthetic and Medicinal Overview

Synthesis and antimicrobial evaluation of some 1,2,4-triazolo[1,5-a]pyridine, pyrimidine sulfonamides and sulfinyl derivatives

Design, Synthesis, and Biological Evaluation of Chalcone Derivatives as Novel Anticandidal Agents

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