Citation
Vats, Lalit, et al. "Synthesis of Novel 4-functionalized 1,5-diaryl-1,2,3-triazoles Containing Benzenesulfonamide Moiety as Carbonic Anhydrase I, II, IV and IX Inhibitors." European Journal of Medicinal Chemistry, vol. 150, 2018, pp. 678-686.
Vats L, Sharma V, Angeli A, et al. Synthesis of novel 4-functionalized 1,5-diaryl-1,2,3-triazoles containing benzenesulfonamide moiety as carbonic anhydrase I, II, IV and IX inhibitors. Eur J Med Chem. 2018;150:678-686.
Vats, L., Sharma, V., Angeli, A., Kumar, R., Supuran, C. T., & Sharma, P. K. (2018). Synthesis of novel 4-functionalized 1,5-diaryl-1,2,3-triazoles containing benzenesulfonamide moiety as carbonic anhydrase I, II, IV and IX inhibitors. European Journal of Medicinal Chemistry, 150, 678-686. https://doi.org/10.1016/j.ejmech.2018.03.030
Vats L, et al. Synthesis of Novel 4-functionalized 1,5-diaryl-1,2,3-triazoles Containing Benzenesulfonamide Moiety as Carbonic Anhydrase I, II, IV and IX Inhibitors. Eur J Med Chem. 2018 Apr 25;150:678-686. PubMed PMID: 29571155.
TY - JOUR
T1 - Synthesis of novel 4-functionalized 1,5-diaryl-1,2,3-triazoles containing benzenesulfonamide moiety as carbonic anhydrase I, II, IV and IX inhibitors.
AU - Vats,Lalit,
AU - Sharma,Vikas,
AU - Angeli,Andrea,
AU - Kumar,Rajiv,
AU - Supuran,Claudiu T,
AU - Sharma,Pawan K,
Y1 - 2018/03/14/
PY - 2018/01/17/received
PY - 2018/03/09/revised
PY - 2018/03/09/accepted
PY - 2018/3/24/pubmed
PY - 2018/4/27/medline
PY - 2018/3/24/entrez
KW - 1,2,3-Triazole
KW - Benzenesulfonamide
KW - Carbonic anhydrase inhibitors
KW - Isoforms I, II, IV, IX
SP - 678
EP - 686
JF - European journal of medicinal chemistry
JO - Eur J Med Chem
VL - 150
N2 - The design, synthesis and biological evaluation of a library of 1,2,3-triazole carboxylates incorporating carboxylic acid, hydroxymethyl, carboxylic acid hydrazide, carboxamide and benzenesulfonamide moieties is disclosed. All the novel compounds were investigated for their inhibition potential against carbonic anhydrase (CA, EC 4.2.1.1) human (h) isoforms hCA I, II, IV and IX, well established drug targets. The cytosolic isoform hCA I was inhibited with Ki's ranging between 53.2 nM and 7.616 μM whereas the glaucoma associated cytosolic isoform hCA II was inhibited with Ki's in the range 21.8 nM-0.807 μM. The membrane bound isoform hCA IV, involved in glaucoma and retinitis pigmentosa among others, was effectively inhibited by some of these compounds with Ki < 60 nM, better than the reference drug acetazolamide (AAZ). The tumor associated isoform hCA IX, a recently validated antitumor/antimetastatic drug target, was also effectively inhibited by some of the new sulfonamides, which possess thus the potential to be used as tools for exploring in more details the selective inhibition of hCAs involved in various pathologies.
SN - 1768-3254
UR - https://www.unboundmedicine.com/medline/citation/29571155/Synthesis_of_novel_4_functionalized_15_diaryl_123_triazoles_containing_benzenesulfonamide_moiety_as_carbonic_anhydrase_I_II_IV_and_IX_inhibitors_
L2 - https://linkinghub.elsevier.com/retrieve/pii/S0223-5234(18)30273-3
DB - PRIME
DP - Unbound Medicine
ER -