Anticonvulsant and Antitubercular Activities of 6-Phenyl/Biphenyl-4-yl-2- [2-(pyridin-2-ylamino)-ethyl]- and 6-(Biphenyl-4yl)-2-(2N-subtituted amin- 1-yl)-ethyl derivatives of 4,5-dihydropyridazin-3(2H)-one

Asif, Mohammad; Singh, Anita; Lakshmayya,; Husain, Asif; Anees, Anees A.

doi:10.2174/1570180811310070013

Cited by 10 publications

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“…Pyridazinone derivatives hold considerable interest in all types of biological activities. Various structural modifications were carried out in pyridazinone ring system and these structural changes cause some fruitful biological activities [20][21][22] . From the above findings wed developed some pyridazinone compounds as antitubercular agents.…”

Section: Structure Feature Of Pyridazinone Derivativesmentioning

confidence: 99%

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2020

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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: Structure Feature Of Pyridazinone Derivativesmentioning

confidence: 99%

“…Blue color in the well was interpreted as no bacterial growth, and pink color was scored as growth. The minimum inhibitory concentration (MIC) was defined as lowest drug concentration which prevented the color change from blue to pink21,22 .…”

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2020

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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.…”

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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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