Synthesis, characterization, alkaline phosphatase inhibition assay and molecular modeling studies of 1-benzylidene-2-(4-tert- butylthiazol-2-yl) hydrazines

Synthesis, characterization, alkaline phosphatase inhibition assay and molecular modeling studies of 1-benzylidene-2-(4-tert- butylthiazol-2-yl) hydrazines

alkaline phosphatase is an enzyme that removes phosphate homodimeric proteins of several types of molecules. This catalyzes the hydrolysis of monoesters in phosphoric acid, which in turn catalyzes transfosforilasi. Thiazoles is a special class of heterocyclic compounds that could potentially be an effective phosphatase inhibitors. In this case, this research paper reported the synthesis and characterization smoothly substituted 1-benzylidene-2- (4-tert-butylthiazol-2-yl) hydrazine with excellent results.

Synthesized compounds tested for potency inhibition of alkaline phosphatase. The compound 1- (4-hydroxy, 3-methoxybenzylidene) -2- (4-tert-butylthiazol-2-yl) hydrazine (<b> 5e) </ b> was found to be the most potent inhibitor of human tissue non phosphatase -alkaline in this group of molecules with IC <sub> 50 </ sub> value of 1.09 ± 0.18 pM. The compound 1- (3,4-dimethoxybenzylidene) -2- (4-tert-butylthiazol-2-yl) hydrazine <b> (5d) </ b> exhibited selectivity and the potential for human intestinal alkaline phosphatase with IC <sub> 50 </ sub> value of 0.71 ± 0.02 pM.

In addition, the structure activity relationship and molecular docking studies were performed to evaluate their mode of binding to the target site alkaline phosphatase. Docking analysis revealed that the most active inhibitor showed significant interaction in the binding pocket of human intestinal alkaline phosphatase and alkaline phosphatase non-human tissues and may be responsible for the inhibitory activity of compounds against the enzyme. Therefore, the filtered thiazole derivatives provided a superb platform for the further development of alkaline phosphatase inhibitor.

Alkaline phosphatase assay revealed the compound <b> 5e </ b> (1- (4-hydroxy, 3-methoxybenzylidene) -2- (4-tert-butylthiazol-2-yl) hydrazine) as the most active inhibitor <b> < i> h </ i> -TNAP </ b> IC <sub> 50 </ sub> value of 1.09 ± 0.18 pM. Computing evaluation clearly illustrates the multiple interactions in the binding pocket <b> <i> h </ i> -IAP </ b> and <b> <i> h </ i> -TNAP </ b> and may be responsible for potential inhibitory compounds against the enzyme. Highlights Synthesis of 1- (benzylidene) thiosemicarbazides <b> 3 (a-i) </ b> reacting it with substituted aromatic aldehydes

Thiosemicarbazide <b> 1 (a-i) </ b>. synthesized 1- (benzylidene) thiosemicarbazides was cyclized with 1-chloropinacolone to get each 1-benzylidene-2- (4-tert-butylthiazol-2-yl) hydrazine <b> 5 (a-i) </ b>. synthesized 1-benzylidene-2- (4-tert-butylthiazol-2-yl) hydrazine <b> 5 (a-i) </ b> successfully characterized using elemental analysis, FT-IR and multi nuclear NMR. Alkaline phosphatase assay and computational studies conducted in support of 1-benzylidene-2- (4-tert-butylthiazol-2-yl) hydrazine synthesized <b> 5 (a-i) </ b>.

Reduce background absorption through the double-key strategy for the detection of alkaline phosphatase and α-fetoprotein

Lowering the background signal for analysis is more sensitive than determinands equally important to strengthen the target signal. Oxidase photoinduced of fluorescein have been reported, which can catalyze the oxidation of a common substrate in a few minutes. As a metaphor for the lock and key, we designed a double lock limiting the activity of fluorescein to reduce background uptake during colorimetric detection.

Alkaline Phosphatase Activity Fluorometric Assay Kit

GWB-AXR234 500 assays Ask for price

Genorise® Alkaline Phosphatase Activity Fluorometric Assay Kit

GR107016 100 tests
EUR 289

StemTAG Alkaline Phosphatase Activity Assay Kit, Fluorometric

CBA-307 100 assays
EUR 540
Description: Alkaline Phosphatase (AP) is a widely used marker for both mouse and human embryonic stem cells (ES) and embryonic germ cells (EG). Our StemTAG Alkaline Phosphatase kits provide an efficient system for monitoring cell differentiation or undifferentiation using the AP marker. The StemTAG Alkaline Phosphatase Activity Assay Kits provide reagents for quantifying alkaline phosphatase activity in a convenient 96-well plate format, with either colorimetric or fluorescence detection.

StemTAG Alkaline Phosphatase Staining and Activity Assay Kit, Fluorometric

CBA-308 2 x 100 assays
EUR 846
Description: Alkaline Phosphatase (AP) is a widely used marker for both mouse and human embryonic stem cells (ES) and embryonic germ cells (EG). Our StemTAG Alkaline Phosphatase kits provide an efficient system for monitoring cell differentiation or undifferentiation using the AP marker. The StemTAG Alkaline Phosphatase Activity Assay Combo Kits provide reagents for monitoring alkaline phosphatase activity via immunocytochemistry staining as well as in a 96-well plate with either colorimetric or fluorescence detection.

Acid Phosphatase Activity Fluorometric Assay Kit

GWB-AXR233 500 assays Ask for price

Acid Phosphatase Activity Fluorometric Assay Kit

K421-500 each
EUR 418.8

Protein Tyrosine Phosphatase Activity Assay Kit (Fluorometric)

K829-100 each
EUR 639.6

Alkaline Phosphatase Activity Assay Kit

55R-1402 500 assays
EUR 600
Description: Assay Kit for detection of Alkaline Phosphatase in the research laboratory

Alkaline Phosphatase Activity Assay Kit

55R-1406 500 assays
EUR 367
Description: Assay Kit for detection of Alkaline Phosphatase in the research laboratory

HAT Activity Fluorometric Assay Kit

K2034-100 100 assays
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Description: Detects HAT activity, sensitive and non-radioactive.

HAT Activity Fluorometric Assay Kit

K334-100 each
EUR 646.8

HDAC Activity Fluorometric Assay Kit

K2031-100 100 assays
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HDAC Activity Fluorometric Assay Kit

K2031-96 96 tests
EUR 389
Description: Detects HDAC activity, high throughput screening (HTS).

DPP4 Activity Fluorometric Assay Kit

K2178-100 100 assays
EUR 451
Description: Highly Sensitive Assay, HTS

PLTP Activity Fluorometric Assay Kit

K2087-100 100 assays
EUR 682
Description: Detects PLTP activity.

CETP Activity Fluorometric Assay Kit

K2089-100 100 assays
EUR 691
Description: Detects CETP activity.

DPP4 Activity Fluorometric Assay Kit

K779-100 each
EUR 652.8

HDAC Activity Fluorometric Assay Kit

K330-100 each
EUR 588

Phospholipase A2 Activity Assay Kit (Fluorometric)

K400-100 each
EUR 679.2

Renin Activity Fluorometric Assay Kit

K800-100 each
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HDAC3 Activity Fluorometric Assay Kit

K343-100 each
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HDAC8 Activity Fluorometric Assay Kit

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Calpain Activity Fluorometric Assay Kit

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Calpain Activity Fluorometric Assay Kit

K2062-100 100 assays
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Description: Exclusively detects activated calpain

Protease Activity Fluorometric Assay Kit

K781-100 each
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Thrombin Activity Fluorometric Assay Kit

K373-100 each
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Urokinase Activity Fluorometric Assay Kit

K728-100 each
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HAT (H4) Activity Fluorometric Assay Kit

K336-100 each
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Proteasome Activity Fluorometric Assay Kit

K2096-100 100 assays
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Description: Specifically detects proteasome activity

Proteasome Activity Fluorometric Assay Kit

K245-100 each
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MMP-3 Activity Fluorometric Assay Kit

K783-100 each
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PLTP Activity Fluorometric Assay Kit II

K593-100 each
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CETP Activity Fluorometric Assay Kit II

K595-100 each
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Alkaline Phosphatase -ALP- Activity Assay Kit

E-BC-K091-M-500Assays 500 Assays
EUR 380
Description: Enzyme Activity

Alkaline Phosphatase -ALP- Activity Assay Kit

E-BC-K091-M-96T 96T
EUR 15
Description: Enzyme Activity

Alkaline Phosphatase -ALP- Activity Assay Kit

E-BC-K091-M-each each Ask for price
Description: Enzyme Activity

Alkaline Phosphatase -ALP- Activity Assay Kit

E-BC-K091-S-100Assays 100Assays
EUR 15
Description: Enzyme Activity

Alkaline Phosphatase -ALP- Activity Assay Kit

E-BC-K091-S-500Assays 500 Assays
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Description: Enzyme Activity

Alkaline Phosphatase -ALP- Activity Assay Kit

E-BC-K091-S-each each Ask for price
Description: Enzyme Activity

Factor Xa Activity Fluorometric Assay Kit

Kit-0337 100 tests
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Description: -20°C

Rat Renin Activity Fluorometric Assay Kit

K806-100 each
EUR 777.6

Factor Xa Activity Fluorometric Assay Kit

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Total Phosphodiesterase Activity Assay Kit (Fluorometric)

K927-100 each
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Neuraminidase Activity Fluorometric Assay Kit

K2230-100 100 assays
EUR 571
Description: Detects neuraminidase (NA) activity, sensitive.

Neuraminidase Activity Fluorometric Assay Kit

K732-100 each
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Lipase Activity Fluorometric Assay Kit III

K2095-100 100 assays
EUR 480
Description: Detects lipase activity, highly sensitive, high throughput screening (HTS).

Lipase Activity Fluorometric Assay Kit III

K724-100 each
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Caspae-9 Activity Fluorometric Assay Kit

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GST Fluorometric Activity Assay Kit

K2105-100 100 assays
EUR 600
Description: Highly sensitive in vitro assay

GST Fluorometric Activity Assay Kit

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GST Fluorometric Activity Assay Kit

K260-100 each
EUR 561.6

Granzyme B Activity Fluorometric Assay Kit

K168-100 each
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Granzyme B Activity Fluorometric Assay Kit

K2001-100 100 assays
EUR 571
Description: Detects Apoptosis & Necrosis within 10 min

InSitu HDAC Activity Fluorometric Assay Kit

K339-100 each
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Cathepsin S Activity Fluorometric Assay Kit

K144-100 each
EUR 614.4

Cathepsin H Activity Fluorometric Assay Kit

K145-100 each
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Cathepsin L Activity Fluorometric Assay Kit

K142-100 each
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Cathepsin D Activity Fluorometric Assay Kit

K143-100 each
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Cathepsin B Activity Fluorometric Assay Kit

K140-100 each
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Cathepsin K Activity Fluorometric Assay Kit

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Cathepsin B Activity Fluorometric Assay Kit

K2151-100 100 assays
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Description: Detects cathepsin B activity, sensitive.

Cathepsin K Activity Fluorometric Assay Kit

K2152-100 100 assays
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Description: Detects cathepsin K activity, sensitive.

Cathepsin L Activity Fluorometric Assay Kit

K2153-100 100 assays
EUR 643
Description: Detects cathepsin L activity, sensitive.

Cathepsin D Activity Fluorometric Assay Kit

K2154-100 100 assays
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Description: Detects cathepsin D activity, sensitive.

Cathepsin S Activity Fluorometric Assay Kit

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Description: Detects cathepsin S activity, sensitive.

Catalase -CAT- Activity Fluorometric Assay Kit

E-BC-F006-500Assays 500 Assays
EUR 960
Description: Enzyme Activity

Catalase -CAT- Activity Fluorometric Assay Kit

E-BC-F006-96T 96T
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Description: Enzyme Activity

Catalase -CAT- Activity Fluorometric Assay Kit

E-BC-F006-each each Ask for price
Description: Enzyme Activity

Catalase (CAT) Activity Fluorometric Assay Kit

MBS2567662-500Tests 500Tests
EUR 830

Catalase (CAT) Activity Fluorometric Assay Kit

MBS2567662-5x100Tests 5x100Tests
EUR 3830

Catalase (CAT) Activity Fluorometric Assay Kit

MBS2567662-5x96Test 5x96Test
EUR 1615

Catalase (CAT) Activity Fluorometric Assay Kit

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EUR 355

Catalase (CAT) Activity Fluorometric Assay Kit

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HDAC Fluorometric Activity Assay Kit

GWB-AXR199 100 assays Ask for price

Sphingomyelinase Activity Fluorometric Assay Kit

K574-100 each
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Proteasome Activity Fluorometric Assay Kit I

RP10220K 1Kit
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Proteasome Activity Fluorometric Assay Kit II

RP10221K 1Kit
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HDAC6 Activity Assay Kit (Fluorometric)

K466-100 each
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Alkaline Phosphatase Activity Colorimetric Assay Kit

K2075-500 500 assays
EUR 557
Description: Detects alkaline phosphatase activity, highly sensitive, high throughput screening (HTS).

Alkaline Phosphatase Activity Colorimetric Assay Kit

GWB-AXR230 500 assays Ask for price

Alkaline Phosphatase Activity Colorimetric Assay Kit

K412-500 each
EUR 646.8

GST Fluorometric Activity Assay

KT-205 100 tests
EUR 510

Sirtuin Activity Assay Kit (Fluorometric)

K324-100 each
EUR 686.4

Plasmin Activity Assay Kit (Fluorometric)

K381-100 each
EUR 548.4

Uricase Activity Assay Kit (Fluorometric)

K734-100 each
EUR 614.4

Beta-Secretase Activity Fluorometric Assay Kit

K2043-100 100 assays
EUR 749
Description: Detects β-secretase activity, highly sensitive.

Beta-Secretase Activity Fluorometric Assay Kit

K360-100 each
EUR 744

Caspase-8, 10 Activity Fluorometric Assay Kit

RP10238K 1kit
EUR 552.5

Caspase-3, 7 Activity Fluorometric Assay Kit

RP10240K 1kit
EUR 552.5

Lysozyme Activity Assay Kit (Fluorometric)

K236-100 each
EUR 588

Lipoprotein Lipase Activity Fluorometric Assay Kit

K721-100 each
EUR 646.8

PPDK (Pyruvate, phosphate dikinase) Activity Assay Kit (Fluorometric/Colorimetric)

K456-100 each
EUR 574.8

?-Xylosidase Activity Assay Kit (Fluorometric)

K981-100 each
EUR 705.6

Neprilysin Activity Assay Kit (Fluorometric)

K487-100 each
EUR 732

Purine Nucleoside Phosphorylase Activity Assay Kit (Fluorometric)

K767-100 each
EUR 914.4

DNAse I Activity Assay Kit (Fluorometric)

K429-100 each
EUR 836.4

Lipoxygenase Activity Assay Kit (Fluorometric)

K978-100 each
EUR 783.6

Chymotrypsin Activity Assay Kit (Fluorometric)

K352-100 each
EUR 588

Factor IXa Activity Assay Kit (Fluorometric)

K364-100 each
EUR 588

?-Glucuronidase Activity Assay Kit (Fluorometric)

K514-100 each
EUR 744

Xanthine Oxidase -XOD- Activity Fluorometric Assay Kit

E-BC-F019-500Assays 500 Assays
EUR 960
Description: Enzyme Activity

Xanthine Oxidase -XOD- Activity Fluorometric Assay Kit

E-BC-F019-96T 96T
EUR 32
Description: Enzyme Activity

Xanthine Oxidase -XOD- Activity Fluorometric Assay Kit

E-BC-F019-each each Ask for price
Description: Enzyme Activity

Xanthine Oxidase (XOD) Activity Fluorometric Assay Kit

MBS2567665-500Tests 500Tests
EUR 880

Xanthine Oxidase (XOD) Activity Fluorometric Assay Kit

MBS2567665-5x100Tests 5x100Tests
EUR 4055

Xanthine Oxidase (XOD) Activity Fluorometric Assay Kit

MBS2567665-5x96Test 5x96Test
EUR 1665

Xanthine Oxidase (XOD) Activity Fluorometric Assay Kit

MBS2567665-96Test 96Test
EUR 365

Xanthine Oxidase (XOD) Activity Fluorometric Assay Kit

MBS2567665-96Tests 96Tests
EUR 365

Deubiquitinase Activity Assay Kit (Fluorometric)

K485-100 each
EUR 639.6

Cathepsin E Activity Assay Kit (Fluorometric)

K165-100 each
EUR 764.4

TEV Protease Activity Assay Kit (Fluorometric)

K842-100 each
EUR 601.2

Factor VIIIa Activity Assay Kit (Fluorometric)

K358-100 each
EUR 646.8

Chitotriosidase Activity Assay Kit (Fluorometric)

K512-100 each
EUR 744

StemTAG Alkaline Phosphatase Activity Assay Kit, Colorimetric

MBS168350-100Assays 100Assays
EUR 490

StemTAG Alkaline Phosphatase Activity Assay Kit, Colorimetric

MBS168350-5x100Assays 5x100Assays
EUR 2235

Lysyl Oxidase Activity Assay Kit (Fluorometric)

K928-100 each
EUR 639.6

Enolase Activity Colorimetric/Fluorometric Assay Kit

K691-100 each
EUR 952.8

Alkaline Phosphatase -ALP- Activity Assay Kit -PNPP method-

E-BC-K009-M-500Assays 500 Assays
EUR 400
Description: Enzyme Activity

Alkaline Phosphatase -ALP- Activity Assay Kit -PNPP method-

E-BC-K009-M-96T 96T
EUR 15
Description: Enzyme Activity

Alkaline Phosphatase -ALP- Activity Assay Kit -PNPP method-

E-BC-K009-M-each each Ask for price
Description: Enzyme Activity

Alkaline Phosphatase (ALP) Activity Assay Kit (PNPP method)

MBS2567975-500Assays 500Assays
EUR 435

Alkaline Phosphatase (ALP) Activity Assay Kit (PNPP method)

MBS2567975-500Tests 500Tests
EUR 435

Alkaline Phosphatase (ALP) Activity Assay Kit (PNPP method)

MBS2567975-5x100Tests 5x100Tests
EUR 1975

Alkaline Phosphatase (ALP) Activity Assay Kit (PNPP method)

MBS2567975-96Test 96Test
EUR 250

Alkaline Phosphatase (ALP) Activity Assay Kit (PNPP method)

MBS2567975-96Tests 96Tests
EUR 250

Fluorometric Proteasome 20S Activity Assay Kit

K2242-100 100T
EUR 444
Description: Cell Biology|Enzyme Activity Detection

?-L-Fucosidase Activity Assay Kit (Fluorometric)

K542-100 each
EUR 627.6

Methyltransferase Activity Assay Kit (Fluorometric)

K521-100 each
EUR 679.2

Adenosylhomocysteinase (AHCY) Activity Fluorometric Assay Kit

K807-100 each
EUR 1038

Enteropeptidase/Enterokinase Activity Fluorometric Assay Kit

K758-100 each
EUR 732

Catalase Activity Colorimetric/Fluorometric Assay Kit

K2177-100 100 assays
EUR 427
Description: Highly Sensitive Assay, HTS

Catalase Activity Colorimetric/Fluorometric Assay Kit

K773-100 each
EUR 502.8

Diamine Oxidase Activity Assay Kit (Fluorometric)

K496-100 each
EUR 679.2

?-Secretase (BACE1) Activity Assay Kit (Fluorometric)

K388-100 each
EUR 724.8

The first key inhibit the main activity of fluorescein by phosphate. The second key is almost completely disable fluorescein by forming nanoparticles coordination (CNPS) through self-assembly of cerium chloride and fluorescein diphosphate (FDP).