&lt;i&gt;In-vivo&lt;/i&gt; Anticonvulsant and &lt;i&gt;In-vitro&lt;/i&gt; Antimycobacterial Activities of 6-Aryl Pyridazine-3(&lt;i&gt;2H&lt;/i&gt;)-One Derivatives

Asif, Mohammad; Singh, Anita; Lakshmayya,

doi:10.12691/ajps-2-1-1

Cited by 9 publications

(5 citation statements)

References 13 publications

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“…It was purified by dissolving in 5% w/v sodium bicarbonate solution, followed by extraction with chloroform. The aqueous layer on acidification with dilute hydrochloric acid gave aroyl propionic acid (1a and 1b) and crystallized with aqueous ethanol [18][19][20] .…”

Section: Scheme 1: Synthesis Of 6-(aryl)-2-(substitutedmethyl)-45-dimentioning

confidence: 99%

“…To a solution of compound (1a or 1b) (0.1 mol) in methanol (30 mL), hydrazine hydrate (1 mL) and sodium acetate (0.5 g) were added and the mixture was refluxed for 6 h. The content was poured into cold water. The solid product was separated out and recrystallized with methanol [18][19][20] .…”

Section: Synthesis Of 6-substituted Aryl-45-dihydropyridazin-3-one (mentioning

confidence: 99%

“…Now efforts toward the development of novel anti-TB drugs, which are structurally dissimilar from currently used anti-TB drugs. The current work describes the synthesis of new pyridazinone derivatives with encouraging anti-TB activity [16][17][18][19][20] .…”

Section: Introductionmentioning

confidence: 99%

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2020

IJPSR

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Two series of pyridazinone derivatives, 6-(aryl)-2-(substituted methyl)-4,5-dihydro (2H) pyridazin-3-one derivatives (3a-8a and 3b-8b) were synthesized by reacting 6-phenyl substituted 2,3,4,5-Tetrahydro pyridazin-3-one (2a and 2b) with cyclic secondary amine under Mannich reaction conditions. These final compounds (3a-8a and 3b-8b) were characterized by spectral analysis (IR, 1 HNMR and mass spectroscopy) and evaluated for anti-tubercular activities against Mycobacterium tuberculosis H37Rv strain by Microplate Alamar Blue assay (MABA) method. Most of the compounds were showed significant anti-tubercular activity. Compounds (7a and 7b) were showed maximum antitubercular activity with 6.25 μg/ml minimum inhibitory concentration (MIC) value and compounds (4a, 5a, 8a and 3b, 4b, 6b, 8b) were exhibited 12.5 μg/ml MIC value and other remaining compounds (3a, 6a and 5a) were found less potent (12.5 μg/ml) MIC value than the reference drugs when compared with reference drugs [pyrizinamide (3.125 μg/ml)] and (streptomycin 6.25 μg/ml) MIC values. Among the synthesized pyridazinone derivatives, compound (7a and 7b) emerged as a lead compound with good anti-tubercular activity. These biological activities differences mainly depend on the different type of substitutions on the pyridazinone ring system.

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Section: Scheme 1: Synthesis Of 6-(aryl)-2-(substitutedmethyl)-45-dimentioning

confidence: 99%

Section: Synthesis Of 6-substituted Aryl-45-dihydropyridazin-3-one (mentioning

confidence: 99%

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2020

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“…This variability in the biological response attracted attention of researchers to explore this nucleus to its multiple potential biological activities. Different synthetic methods of pyridazins and pyridazinones depend on reaction of 1,4-disubstituted aromatic hydrocarbons, furanones , diketons, ketoacids or ketoesters with hydrazine or its derivatives [11][12][13][14][15].…”

Section: Pyridazinonesmentioning

confidence: 99%

Pyridazinones and pyrrolones as promising Scaffolds in Medicinal Chemistry

Abdelbaset

Abdel‐Aziz

Abuo‐Rahma

et al. 2018

Journal of advanced Biomedical and Pharmaceutical Sciences

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Pyridazinones and pyrrolones are important building blocks for some important drugs such as the naturally occurring antibacterial pyrrolone, althiomycin; the cardiotonic pyridazinones, pimobendan and levosimendan and the analgesic anti-inflammatory, emorfozan. Therefore, researchers all over the world paid attention to prepare various pyridazinones and pyrroolones derivatives. The variability in the biological response and ease of preparation from the corresponding furanones attracted attention of researchers to explore these two nuclei in the design and synthesis of different analogues. This review article focuses on different biological activities, structure activity relationship and mechanism of action of pyridazinones and pyrrolones derivatives.

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“…[1][2][3] Various pyridazinone and thiopyridazinones derivatives were synthesized and their anti-TB activity was tested. [4][5][6] Hence this feature of the ring system was tapped for the presence of any anti-TB activity. Drug resistance is a major public health problem that threatens progress made in TB care and control worldwide.…”

Section: Introductionmentioning

confidence: 99%

In silico Physicochemical Bioactivities and Toxicities Prediction of 3-chloro-6-arylpyridazines and 6-aryl- 4,5-dihydropyridazine-3(2H)-thiones having Antitubercular Activity

Asif¹,

Acharya²,

Lakshmayya³

et al. 2015

RGUHS J Pharm Sci

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Purpose: In the present study, antitubercular activities and in silico physicochemical toxicities and bioactivity profile of some 3-chloro-6-arylpyridazines (3a-d) and 6-aryl-4,5-dihydropyridazine-3(2H)-thiones (4a-d) are studied. Approach: The compounds (3a-d) and (4a-d) were evaluated as antitubercular agents against Mycobacterium tuberculosis H37Rv by screening through in vitro Microplate Alamar Blue Assay (MABA) method. Findings: In silico physicochemical parameter revealed that the entire compounds follow Lipinski's rule-of-5 to become a "drug like" molecule. ADME (absorption, distribution, metabolism and excretions) profile prediction has shown that all the compounds can be absorbed through human intestine (HIA +), Caco-2 cell (Caco-2 +) and can cross blood brain barrier (BBB +), they all are non-substrate and non-inhibitor of p-glycoprotein. Compounds 4a-d are inhibitor of human microsomal enzyme like CYP 450 1A2, CYP 450 2C19 and CYP 450 3A4. Research limitations/implications: Compounds 4a-4d are better ligand for enzyme inhibition than 3a-d compounds. The MIC of compounds 4a-d and 3a is 6.25 µg/ml. They are potent than compound 3b-d with MIC 12.5 µg/ml. Originality: Toxicity prediction indicated that compounds 3a-3d and 4a-d are non-carcinogenic and non-mutagenic. Bioactivity prediction for compounds 3a-3d and 4a-d indicated better ligand as enzyme inhibitor in comparison to standard.

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<i>In-vivo</i> Anticonvulsant and <i>In-vitro</i> Antimycobacterial Activities of 6-Aryl Pyridazine-3(<i>2H</i>)-One Derivatives

Cited by 9 publications

References 13 publications

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Pyridazinones and pyrrolones as promising Scaffolds in Medicinal Chemistry

In silico Physicochemical Bioactivities and Toxicities Prediction of 3-chloro-6-arylpyridazines and 6-aryl- 4,5-dihydropyridazine-3(2H)-thiones having Antitubercular Activity

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