Synthesis and analgesic and anti-inflammatory activities 6-substituted-3(2H)-pyridazinone-2-acetyl-2-(p-substituted/nonsubstituted benzal)hydrazone derivatives

Gökçe, Mehtap; Utku, Semra; Küpeli, Esra

doi:10.1016/j.ejmech.2009.04.048

Cited by 116 publications

(40 citation statements)

References 19 publications

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“…It has been reported in the literature that certain compounds bearing pyridine, pyridazine and pyridazinone heterocycles, possess significant analgesic and anti-inflammatory activities. [13][14][15][16] Niflumic acid and flunixin are two traditional NSAIDs belonging to the class of fenamates enclosing pyridine nucleus in their structure (Fig. 1).…”

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confidence: 99%

Synthesis and Biological Evaluation of New Heteroaryl Carboxylic Acid Derivatives as Anti-inflammatory-Analgesic Agents

Abouzid

Khalil

Ahmed

et al. 2013

CHEMICAL & PHARMACEUTICAL BULLETIN

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A series of nicotinic acid derivatives structurally related to niflumic acid and certain pyridazine-containing compounds have been synthesized and characterized by analytical and spectral data. All compounds were screened for their potential analgesic and anti-inflammatory activities. The compounds which displayed analgesic and anti-inflammatory activities were tested for ulcerogenicity and screened for in vivo inhibition of certain inflammatory cytokines such as tumor necrosis factor-alpha (TNF-α), interleukin-6 (IL-6), and cyclooxygenase-2 (COX-2). Compounds 1c, 2a, 2b, and 5a have shown potent analgesic and anti-inflammatory activities.

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confidence: 99%

Synthesis and Biological Evaluation of New Heteroaryl Carboxylic Acid Derivatives as Anti-inflammatory-Analgesic Agents

Abouzid

Khalil

Ahmed

et al. 2013

CHEMICAL & PHARMACEUTICAL BULLETIN

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“…It is also reported that hydrazones possess a diverse range of bioactivities in the medicinal and agrochemical elds, such as anticancer, 13) anti-in ammatory, 14) antimicrobial, 15) herbicidal, 16) fungicidal 17) and insecticidal 18) activities. In addition, hydrazones are very useful starting materials in many reactions in the synthesis of various bioactive molecules.…”

Section: Introductionmentioning

confidence: 99%

“…Its favorable bioactivity has prompted widespread studies on benzothiazole derivatives in the past two decades. For example, a number of benzothiazole derivatives are shown to have antitumor, 6) antimicrobial, 7) antifungal, 8) anthelmintic, 9) anti-in ammatory, 10) cardiovascular 11) and antitubercular 12) activities.It is also reported that hydrazones possess a diverse range of bioactivities in the medicinal and agrochemical elds, such as anticancer, 13) anti-in ammatory, 14) antimicrobial, 15) herbicidal, 16) fungicidal 17) and insecticidal 18) activities. In addition, hydrazones are very useful starting materials in many reactions in the synthesis of various bioactive molecules.…”

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Synthesis and fungicidal activity of hydrazones containing 4-methylbenzo[d]thiazole moiety

2012

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A new series of hydrazone derivatives containing 4-methylbenzo [d]thiazole moiety was synthesized. e structures of the title compounds were characterized by 1 H NMR, FTIR, MS and elemental analysis. Fungicidal activities of the title compounds were investigated. e results indicated that some of these compounds exhibit excellent fungicidal activities. © Pesticide Science Society of Japan Keywords: hydrazone, benzothiazole, synthesis, fungicidal activity. IntroductionSulfur-and nitrogen-linked heterocyclic compounds have received considerable attention in recent years because of their pharmacological and pesticidal importance. [1][2][3][4][5] Benzothiazole is one of the oldest and potent heterocyclic compounds displaying interesting medicinal and agricultural activities. Its favorable bioactivity has prompted widespread studies on benzothiazole derivatives in the past two decades. For example, a number of benzothiazole derivatives are shown to have antitumor, 6) antimicrobial, 7) antifungal, 8) anthelmintic, 9) anti-in ammatory, 10) cardiovascular 11) and antitubercular 12) activities.It is also reported that hydrazones possess a diverse range of bioactivities in the medicinal and agrochemical elds, such as anticancer, 13) anti-in ammatory, 14) antimicrobial, 15) herbicidal, 16) fungicidal 17) and insecticidal 18) activities. In addition, hydrazones are very useful starting materials in many reactions in the synthesis of various bioactive molecules. 19) It is well-known that tricyclazole, a triazolo [3,4-b]benzothiazole derivative, is applied mainly as a commercial fungicide to control Pyricularia oryzae. 13) In line with our continuous e orts to synthesize bioactive lead compounds for crop protection, the title compounds were designed by introducing a hydrazone pharmacophore into the benzothiazole sca old. Our original strategy is depicted in Fig. 1. Materials and Methods InstrumentsMelting points were determined using an X-4 apparatus without calibration. 1 H NMR spectra were measured on a Bruker ADVANCE III instrument (500 MHz) using TMS as an internal standard and deuterochloroform as a solvent. FT-IR spectra were recorded on a NICOLET 6700 instrument. Mass spectra were recorded on a ermo Scienti c ITQ 1100TM and erm LCQ TM Deca XP plus instrument. Elemental analyses were performed on a Vario EL elemental analyzer. Synthesis of compoundsAll starting materials were used as purchased or of analytic grade purity. Analytical TLC was performed on silica gel GF254. e title compounds were synthesized according to the route shown in Fig. 2. 2-Hydrazino-4-methylbenzo [d]thiazole was prepared according to the reference. 20) o-Toluidine (0.2 mol) was added to water and warmed with dilute hydrochloric acid (10 mL) until a clear solution was obtained. Ammonium thiocyanate (0.22 mol) dissolved in water (50 mL), then added this solution gradually. e reaction mixture boiled at 100-110°C for 8 hr and evaporated to less than half the volume. It was then cooled to get the precipitate of compound 2, which was ltered, washed wit...

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“…The structures of diazines are prepared by replacing two carbon atoms to two nitrogen atoms in the benzene ring at their respective positions. Diazines and its derivatives are noteworthy for their physiological and biological importance [12][13][14]. Recently diazine derivatives have been a subject of intensive research owing to their wide spectrum of pharmacological activities.…”

Section: Introductionmentioning

confidence: 99%

Recent Efforts for the Development of Antitubercular Drug Containing Diazine Ring

Asif¹

2012

Med chem

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There has been considerable interest in the development of new molecule with antibacterial activities particularly against tuberclosis because mycobacterium species have developed resistant against currently used drugs, their toxic effect and long duration of therapy. The diazine (pyridazine, pyrimidine and piperazine) derivatives possess an important class of compound for new drugs research and development. Therefore, many researchers have synthesized these compounds as target structures and evaluated their antitubercular activity. These observations have been guiding for the development of new molecules that possess potent antitubercular activity with minimum side effects or effective against MDR, XDR mycobacterium strains, and also in patient co-infected with HIV/AIDS.

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Synthesis and analgesic and anti-inflammatory activities 6-substituted-3(2H)-pyridazinone-2-acetyl-2-(p-substituted/nonsubstituted benzal)hydrazone derivatives

Cited by 116 publications

References 19 publications

Synthesis and Biological Evaluation of New Heteroaryl Carboxylic Acid Derivatives as Anti-inflammatory-Analgesic Agents

Synthesis and Biological Evaluation of New Heteroaryl Carboxylic Acid Derivatives as Anti-inflammatory-Analgesic Agents

Synthesis and fungicidal activity of hydrazones containing 4-methylbenzo[d]thiazole moiety

Recent Efforts for the Development of Antitubercular Drug Containing Diazine Ring

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