Pyrazole derivatives from azines of substituted phenacyl aryl/cyclohexyl sulfides and their antimycobacterial activity

Manikannan, Ramaiyan; Venkatesan, Ragavendran; Muthusubramanian, Shanmugam; Yogeeswari, Perumal; Sriram, Dharmarajan

doi:10.1016/j.bmcl.2010.09.137

Cited by 58 publications

(21 citation statements)

References 14 publications

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“…Compounds (6) and (9), when reacted separately with different heterocyclic secondary amines, gave the corresponding desired products, (7a-d) and (10a-d), respectively, in good yields (Scheme 2). (1) and (E)-1,4-dibromobut-2-ene (8). Compounds (6) and (9), when reacted separately with different heterocyclic secondary amines, gave the corresponding desired products, (7a-d) and (10a-d), respectively, in good yields (Scheme 2).…”

Section: Chemistrymentioning

confidence: 99%

“…Similarly, ethyl 4-amino-1-[(2E)-(4-bromobut-2-en-1-yl)-3-(4-chlorophenyl)-1H-pyrazole-5-carboxylate (9) was prepared from (1) and (E)-1,4-dibromobut-2-ene (8). Compounds (6) and (9), when reacted separately with different heterocyclic secondary amines, gave the corresponding desired products, (7a-d) and (10a-d), respectively, in good yields (Scheme 2).…”

Section: Chemistrymentioning

confidence: 99%

“…Pyrazoles are one of the most common pharmaceutically active compounds, and have attracted much attention due to their broad spectrum of biological activities such as anti-inflammatory [2,3], COX inhibitory [4], hypoglycemic [5], CDK2/Cyclin A [6], p38 MAP kinase [7], and antidepressive activities [8], and have been widely used in biopharmaceutical and pesticides. Pyrazole plays a unique role in drug discovery programs.…”

Section: Introductionmentioning

confidence: 99%

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Synthesis and Biological Evaluation of N- Pyrazolyl Derivatives and Pyrazolopyrimidine Bearing a Biologically Active Sulfonamide Moiety as Potential Antimicrobial Agent

Hafez

El‐Gazzar

2016

Molecules

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Abstract:A series of novel pyrazole-5-carboxylate containing N-triazole derivatives 3,4; different heterocyclic amines 7a-b and 10a-b; pyrazolo [4,3-d]pyrimidine containing sulfa drugs 14a,b; and oxypyrazolo [4,3-d]pyrimidine derivatives 17, 19, 21 has been synthesized. The structure of the newly synthesized compounds was elucidated on the basis of analytical and spectral analyses. All compounds have been screened for their in vitro antimicrobial activity against three gram-positive and gram-negative bacteria as well as three fungi. The results revealed that compounds 14b and 17 had more potent antibacterial activity against all bacterial strains than reference drug Cefotaxime. Moreover compounds 4, 7b, and 12b showed excellent antifungal activities against Aspergillus niger and Candida albicans in low inhibitory concentrations but slightly less than the reference drug miconazole against Aspergillus flavus.

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Section: Chemistrymentioning

confidence: 99%

Section: Chemistrymentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

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Synthesis and Biological Evaluation of N- Pyrazolyl Derivatives and Pyrazolopyrimidine Bearing a Biologically Active Sulfonamide Moiety as Potential Antimicrobial Agent

Hafez

El‐Gazzar

2016

Molecules

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“…Results of a series of pyrazole derivatives, generally show that cyclohexylthio substituted pyrazole derivatives are more active than arylthio substituted systems. An excellent activity is presented when a para-nitrophenilthio ring is incorporated on a pyrazole ring (42, figure 12) (Manikannan et al, 2010). Thiazoles are compounds that contains sulfur and nitrogen atom in its structure, and have been the basis of clinically used compounds.…”

Section: Azoles Derivativesmentioning

confidence: 99%

Antitubercular Drugs Development: Recent Advances in Selected Therapeutic Targets and Rational Drug Design

Bocanegra-García¹,

García²,

Palma-Nicolás³

et al. 2011

Drug Development - A Case Study Based Insight Into Modern Strategies

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“…It has been reported that the class of pyrazoles represents structurally diverse molecules with widespread and diverse pharmacological properties such as anticancer [4], antimicrobial [5], antiviral [6], antidepressant [7], antimycobacterial [8], antiinflammatory [9], anti-angiogenic [10], and antiglaucoma activities [11]. Moreover, pyrazoles have found applications in drug development for the treatment of dyslipidemia [12], obesity [13], and neuropathic pain [14].…”

mentioning

confidence: 99%

Facile Synthesis, Single‐Crystal Structure, and Biological Evaluation of Novel Pyrazolo[5,1‐d][1,2,5]triazepin‐4‐ones

Zheng

Han

Liu

et al. 2012

Helvetica Chimica Acta

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A facile ring-enlargement reaction of 2,6-diphenyl-4H-pyrazolo [5,1-c] C-NMR, and HR-MS data. Moreover, the molecular structure was confirmed by the X-ray crystal-structure analysis of one compound that was prone to crystallization. Preliminary biological evaluation showed that the compounds 2e -2h promote the viability and inhibit the apoptosis of vascular endothelial cells at low concentration.Introduction. -Small-and medium-sized N-containing heterocyclic skeletons, such as fused triazepines with a bridgehead N-atom in the molecule exhibit remarkable biological properties [1]. Although several methods for constructing 1,3,5-triazepine can be found in the literature [2], the 1,2,5-triazepin skeleton has only received scant attention [3].It has been reported that the class of pyrazoles represents structurally diverse molecules with widespread and diverse pharmacological properties such as anticancer We previously reported our efforts to identify novel potential agents, which inhibited human umbilical vein endothelial cell (HUVEC) apoptosis, based on pyrazole heterocycles [15]. More recently, we became interested in exploring pyrazolefused heterocycles that contain more heteroatoms, ultimately discovering novel antithrombotic and anticancer agents [16]. In continuation of our search for biologically potent molecules, we hereby report the synthesis and structure characterization of pyrazolo [5,1-d][1,2,5]triazepin-4-one derivatives, which could inhibit endothelial cell apoptosis.

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Pyrazole derivatives from azines of substituted phenacyl aryl/cyclohexyl sulfides and their antimycobacterial activity

Cited by 58 publications

References 14 publications

Synthesis and Biological Evaluation of N- Pyrazolyl Derivatives and Pyrazolopyrimidine Bearing a Biologically Active Sulfonamide Moiety as Potential Antimicrobial Agent

Synthesis and Biological Evaluation of N- Pyrazolyl Derivatives and Pyrazolopyrimidine Bearing a Biologically Active Sulfonamide Moiety as Potential Antimicrobial Agent

Antitubercular Drugs Development: Recent Advances in Selected Therapeutic Targets and Rational Drug Design

Facile Synthesis, Single‐Crystal Structure, and Biological Evaluation of Novel Pyrazolo[5,1‐d][1,2,5]triazepin‐4‐ones

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