IN VITRO INHIBITION OF PURIFIED HUMAN CARBONIC ANHYDRASE I AND II BY NOVEL FLUORENE DERIVATIVES

被引：0
|
作者：
Demirhan, Hulya [1 ]
Arslan, Mustafa [2 ]
Kaya, Mustafa Oguzhan [3 ]
Kaya, Yesim [4 ]
Gencer, Nahit [4 ]
Arslan, Oktay [4 ]
机构：
[1] Sakarya Univ, Pamukova Vocat High Sch, Dept Chem Proc, Sakarya, Turkey
[2] Sakarya Univ, Sci & Art Fac, Dept Chem, Sakarya, Turkey
[3] Siirt Univ, Fac Arts & Sci, Dept Chem, TR-56100 Siirt, Turkey
[4] Balikesir Univ, Sci & Art Fac, Dept Chem, Balikesir, Turkey
来源：
MACEDONIAN JOURNAL OF CHEMISTRY AND CHEMICAL ENGINEERING | 2014年 / 33卷 / 02期
关键词：
9-benzylidene-9H-fluorene; urea; thiourea; carbonic anhydrase; inhibition; THERAPEUTIC APPLICATIONS; REGIOSELECTIVITY; PURIFICATION; ERYTHROCYTE; TARGET; UREASE; ADDUCT;
D O I：
暂无
中图分类号：
O6 [化学];
学科分类号：
0703 ;
摘要：
In this study, 9-benzylidene-9H-fluorene-substituted urea (5a-p) and thiourea derivatives (5q-v) were synthesized and their inhibitory effects on the activity of human carbonic anhydrase (hCA) I and II were evaluated. hCA I and II were purified from human erythrocytes using a Sepharose 4B-L-tyrosine-sulphanilamide affinity column. All the synthesized compounds inhibited the activity of the hCA I and II isoenzymes. Among the synthesized compounds, 5f was found to be the most active (IC50 = 21.4 mu M) for inhibition of hCA I and 5s was the most active (IC50 = 25.3 mu M) for inhibition of hCA II.
引用
收藏
页数：9
相关论文
共 50 条
  • [31] New Thiazole Derivatives: Carbonic Anhydrase I-II and Cholinesterase Inhibition Profiles, Molecular Docking Studies
    Karakaya, Abdullatif
    Ercetin, Tugba
    Yildirim, Suheda
    Kocyigit, Umit M.
    Rudrapal, Mithun
    Rakshit, Gourav
    Cevik, Ulviye Acar
    Ozkay, Yusuf
    [J]. CHEMISTRYSELECT, 2024, 9 (28):
  • [32] Influence of Chirality of Benzimidazole Amine Hybrids on Inhibition of Human Erythrocytes Carbonic Anhydrase I, II and Acetylcholinesterase
    Tunc, Turgay
    Abdurrahmanoglu, Suzan
    Gunel, Aslihan
    Alim, Zuhal
    Demirel, Nadir
    [J]. CHEMISTRY & BIODIVERSITY, 2023, 20 (06)
  • [33] Synthesis of two phloroglucinol derivatives with cinnamyl moieties as inhibitors of the carbonic anhydrase isozymes I and II: an in vitro study
    Burmaoglu, Serdar
    Dilek, Esra
    Yilmaz, Ali Osman
    Supuran, Claudiu T.
    [J]. JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY, 2016, 31 : 208 - 212
  • [34] Inhibition of human carbonic anhydrase isozymes I, II and VI with a series of bisphenol, methoxy and bromophenol compounds
    Balaydin, Halis Turker
    Durdagi, Serdar
    Ekinci, Deniz
    Senturk, Murat
    Goksu, Suleyman
    Menzek, Abdullah
    [J]. JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY, 2012, 27 (04) : 467 - 475
  • [35] Carbonic anhydrase inhibitors. Inhibition of human erythrocyte isozymes I and II with a series of antioxidant phenols
    Senturk, Murat
    Gulcin, Ilhami
    Dastan, Arif
    Kufrevioglu, O. Irfan
    Supuran, Claudiu T.
    [J]. BIOORGANIC & MEDICINAL CHEMISTRY, 2009, 17 (08) : 3207 - 3211
  • [36] Carbonic anhydrase inhibitors: Inhibition of the human isozymes I, II, VA, and IX with a library of substituted difluoromethanesulfonamides
    Cecchi, A
    Taylor, SD
    Liu, Y
    Hill, B
    Vullo, D
    Scozzafava, A
    Supuran, CT
    [J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2005, 15 (23) : 5192 - 5196
  • [37] Some drugs inhibit in vitro hydratase and esterase activities of human carbonic anhydrase-I and II
    Ekinci, Deniz
    Beydemir, Sukru
    Alim, Zuhal
    [J]. PHARMACOLOGICAL REPORTS, 2007, 59 (05) : 580 - 587
  • [38] In vitro and in silico interactions of antiulcer, glucocorticoids and urological drugs on human carbonic anhydrase I and II isozymes
    Guller, Ugur
    Beydemir, Sukru
    Kufrevioglu, Omer Irfan
    [J]. BIOPHARMACEUTICS & DRUG DISPOSITION, 2022, 43 (02) : 47 - 56
  • [39] Carbonic anhydrase inhibitors .50. Interaction of isozymes I and II of carbonic anhydrase with Ge(IV) and Sb(III) derivatives
    RiviereBaudet, M
    Supuran, CT
    Scozzafava, A
    Briganti, F
    ElBaz, F
    BenMaarouf, Z
    Riviere, P
    [J]. MAIN GROUP METAL CHEMISTRY, 1997, 20 (10) : 641 - 647
  • [40] Carbonic anhydrase inhibitors: Synthesis, molecular docking, cytotoxic and inhibition of the human carbonic anhydrase isoforms I, II, IX, XII with novel benzenesulfonamides incorporating pyrrole, pyrrolopyrimidine and fused pyrrolopyrimidine moieties
    Ghorab, Mostafa M.
    Alsaid, Mansour S.
    Ceruso, Mariangela
    Nissan, Yassin M.
    Supuran, Claudiu T.
    [J]. BIOORGANIC & MEDICINAL CHEMISTRY, 2014, 22 (14) : 3684 - 3695
12345