TY - JOUR
T1 - Synthesis, Characterization and Antimycobacterial Activity of Some Substituted Phenylpyridazinone Derivatives
AU - Alghamdi, Saad
AU - Imran, Mohd
AU - Kamal, Mehnaz
AU - Asif, Mohammad
N1 - Publisher Copyright:
© 2022, Springer Science+Business Media, LLC, part of Springer Nature.
PY - 2022/3
Y1 - 2022/3
N2 - Aseries 6-phenyl-2-(substituted methyl)-dihydropyridazinone derivatives (3a–3f) were synthesized using the interaction of 6-phenylpyridazinone with cyclic secondary amine by Mannich reaction and evaluated for antimycobacterial activity against Mycobacterium tuberculosis H37Rv strain by Microplate Alamar Blue Assay (MABA) method. All the synthesized compounds (3a–3f) were characterized by IR, 1H NMR, and mass spectroscopy methods. The results indicated that 6-phenyl-2-(Imidazol-1-ylmethyl)-4,5-dihydro-2H-pyridazin-3-one (3b) and 6-phenyl-2-(1,2-dihydro-phenothiazin-10-ylmethyl)-4,5-dihydro-2H-pyridazin-3-one (3f) exhibited highest antimycobacterial activity. Other compounds (3a, 3c-3e) showed less significant antimycobacterial activity. The most effective compounds (3b and 3f) possessed MIC of 6.25μg/mL that was equal to that of reference drugs Streptomycin and Ciprofloxacin.
AB - Aseries 6-phenyl-2-(substituted methyl)-dihydropyridazinone derivatives (3a–3f) were synthesized using the interaction of 6-phenylpyridazinone with cyclic secondary amine by Mannich reaction and evaluated for antimycobacterial activity against Mycobacterium tuberculosis H37Rv strain by Microplate Alamar Blue Assay (MABA) method. All the synthesized compounds (3a–3f) were characterized by IR, 1H NMR, and mass spectroscopy methods. The results indicated that 6-phenyl-2-(Imidazol-1-ylmethyl)-4,5-dihydro-2H-pyridazin-3-one (3b) and 6-phenyl-2-(1,2-dihydro-phenothiazin-10-ylmethyl)-4,5-dihydro-2H-pyridazin-3-one (3f) exhibited highest antimycobacterial activity. Other compounds (3a, 3c-3e) showed less significant antimycobacterial activity. The most effective compounds (3b and 3f) possessed MIC of 6.25μg/mL that was equal to that of reference drugs Streptomycin and Ciprofloxacin.
KW - antitubercular activity
KW - microplate alamar blue assay
KW - Mycobacterium tuberculosis H37Rv
KW - pyridazinone
UR - http://www.scopus.com/inward/record.url?scp=85125640481&partnerID=8YFLogxK
U2 - 10.1007/s11094-022-02583-5
DO - 10.1007/s11094-022-02583-5
M3 - Article
AN - SCOPUS:85125640481
SN - 0091-150X
VL - 55
SP - 1367
EP - 1371
JO - Pharmaceutical Chemistry Journal
JF - Pharmaceutical Chemistry Journal
IS - 12
ER -
