TY - JOUR
T1 - Antimycobacterial Activity of Some New Pyridinylpyridazine Derivatives
AU - Almehmadi, Mazen M.
AU - Halawi, Mustafa
AU - Kamal, Mehnaz
AU - Yusuf, Mohd
AU - Chawla, Udeep
AU - Asif, Mohammad
N1 - Publisher Copyright:
© 2022, Colegio de Farmaceuticos de la Provincia de Buenos Aires. All rights reserved.
PY - 2022
Y1 - 2022
N2 - SUMMARY. Some new pyridazine compounds were synthesized, characterized, and evaluated for their in vitro antimycobacterial activity against Mycobacterium tuberculosis by the microplate Alamar blue dye assay (MABA) method. Isonicotinohydrazide was condensed with appropriate heterocyclic aldehydes to form compounds N-(heteroaryl-2-yl-methylidene)-isonicotinohydrazides. Intramolecular cyclization of compound N-(heteroaryl-2-yl-methylidene)-isonicotinohydrazideto formed 4-(pyridine-4-yl)furo[2,3-d]pyr-idazine,4-(pyridine-4-yl)-1H-pyrrolo[2,3-d]pyridazineand4-(pyridin-4-yl) thieno [2,3-d]pyridazine, respec-tively. All the title compounds were characterized byusing IR, NMR, and mass spectral data. Docking study, optimized geometries, electrical and optical parameters were also studied in a solvent phase of synthesized pyridazine derivatives. Compound 4-(pyridin-4-yl) thieno[2,3-d]pyridazinewas found to have the most sig-nificant antimycobacterial activity (12.5 μg/mL) when compared to reference drugs streptomycin (6.25 μg/ mL) and pyrazinamide (3.125 μg/mL).
AB - SUMMARY. Some new pyridazine compounds were synthesized, characterized, and evaluated for their in vitro antimycobacterial activity against Mycobacterium tuberculosis by the microplate Alamar blue dye assay (MABA) method. Isonicotinohydrazide was condensed with appropriate heterocyclic aldehydes to form compounds N-(heteroaryl-2-yl-methylidene)-isonicotinohydrazides. Intramolecular cyclization of compound N-(heteroaryl-2-yl-methylidene)-isonicotinohydrazideto formed 4-(pyridine-4-yl)furo[2,3-d]pyr-idazine,4-(pyridine-4-yl)-1H-pyrrolo[2,3-d]pyridazineand4-(pyridin-4-yl) thieno [2,3-d]pyridazine, respec-tively. All the title compounds were characterized byusing IR, NMR, and mass spectral data. Docking study, optimized geometries, electrical and optical parameters were also studied in a solvent phase of synthesized pyridazine derivatives. Compound 4-(pyridin-4-yl) thieno[2,3-d]pyridazinewas found to have the most sig-nificant antimycobacterial activity (12.5 μg/mL) when compared to reference drugs streptomycin (6.25 μg/ mL) and pyrazinamide (3.125 μg/mL).
KW - antimycobacterial activity
KW - pyridazine derivative
KW - spectral characterization
KW - synthesis
KW - tuberculosis
UR - http://www.scopus.com/inward/record.url?scp=85133872922&partnerID=8YFLogxK
M3 - Article
AN - SCOPUS:85133872922
SN - 0326-2383
VL - 41
SP - 1428
EP - 1432
JO - Latin American Journal of Pharmacy
JF - Latin American Journal of Pharmacy
IS - 7
ER -