66934-10-9

Upstream product

• 1147550-11-5 ammonium thiocyanate 
• 98-88-4 benzoyl chloride 
• 88-74-4 2-nitro-aniline 
• 532-55-8 Benzoyl isothiocyanate 

Downstream Products

• 100856-57-3 N-(4-nitrobenzo[d]thiazol-2-yl)benzamide 
• 85285-75-2 Sm⁽³⁺⁾*C₁₄H₉N₃O₃S^(2-)*Cl^(1-)*H₂O=Sm(C₁₄H₉N₃O₃S)Cl*H₂O 
• 85285-69-4 Nd⁽³⁺⁾*C₁₄H₉N₃O₃S^(2-)*Cl^(1-)*H₂O=Nd(C₁₄H₉N₃O₃S)Cl*H₂O 
• 85285-57-0 La⁽³⁺⁾*C₁₄H₉N₃O₃S^(2-)*Cl^(1-)*H₂O=La(C₁₄H₉N₃O₃S)Cl*H₂O 
• 85285-63-8 Pr⁽³⁺⁾*C₁₄H₉N₃O₃S^(2-)*Cl^(1-)*H₂O=Pr(C₁₄H₉N₃O₃S)Cl*H₂O 
• 80872-18-0 [Cu(C₆H₅CONHCSNHC₆H₄NO₂)2Cl₂] 
• 80872-26-0 [Cu(C₆H₅CONHCSNHC₆H₄NO₂)2(NO₃)2] 
• 80849-56-5 [Cu(C₆H₅CONHCSNHC₆H₄NO₂)2(ClO₄)2] 
• 21578-47-2 1-phenylcarbonyl-3-(2'-aminophenyl)thiourea 
• 1391013-09-4 N-(4-amino-3-(2-nitro-phenyl)-5-phenyl-3H-thiazol-2-ylidine)-benzamide 
• 51039-84-0 N-(2-nitrophenyl)thiourea 
• 85285-75-2 samarium (N-benzoyl-N'-orthonitrophenyl thiocarbamide) chloride hydrate 
• 85285-69-4 neodymium (N-benzoyl-N'-orthonitrophenyl thiocarbamide) chloride hydrate 
• 85285-57-0 lanthanum (N-benzoyl-N'-orthonitrophenyl thiocarbamide) chloride hydrate 

Relevant academic research and scientific papers

Iodine-mediated multi-component reactions: Readily access to tetrazoles and guanidines

Environmentally benign syntheses of One-pot sequential reactions of benzoyl chloride with amines followed by the treatment of molecular I2 reagent under basic conditions provide benzoyl tetrazoles and guanidines in moderate to excellent yields. This one-pot synthesis has several advantages such as mild reaction conditions, short reaction time, convenient workup, high yields, using cheap and readily available reagent molecular Iodine. In addition, functional group tolerance has been explored.

THEORETICAL AND EXPERIMENTAL INVESTIGATION OF THIOUREA DERIVATIVES: SYNTHESIS, CRYSTAL STRUCTURE, IN-SILICO AND IN-VITRO BIOLOGICAL EVALUATION

In this study, five different thiourea derivatives were synthesized from aryl amines according to the reported method. 1-Benzoyl-3-(4-methoxyphenyl)thiourea (2) was confirmed with single crystal XRD analysis while 1-benzoyl-3-phenylthiourea (1), 1-benzoyl

Benzoylthioureas: Design, synthesis and antimycobacterial evaluation

Background: New drugs and strategies to treat tuberculosis (TB) are urgently needed. In this context, thiourea derivatives have a wide range of biological activities, including anti-TB. This fact can be illustrated with the structure of isoxyl, an old anti-TB drug, which has a thiourea as a pharmacophore group. Objective: The aim of this study is to describe the synthesis and the antimycobacterial activity of fifty-nine benzoylthioureas derivatives. Methods: Benzoylthiourea derivatives have been synthesized and evaluated for their activity against Mycobacterium tuberculosis using the MABA assay. After that, a structure-activity relationship study of this series of compounds has been performed. Results and Discussion: Nineteen compounds exhibited antimycobacterial activity between 423.1 and 9.6 μM. In general, we observed that the presence of bromine, chlorine and t-Bu group at the para-position in benzene ring plays an important role in the antitubercular activity of Series A. These substituents were fixed at this position in benzene ring and other groups such as Cl, Br, NO2 and OMe were introduced in the benzoyl ring, leading to the derivatives of Series B. In general, Series B was less cytotoxic than Series A, which indicates that the presence of a substituent at benzoyl ring contributes to an improvement in both antimycobacterial activity and toxicity profiles. Conclusion: Compound 4c could be considered a good prototype to be submitted to further structural modifications in the search for new anti-TB drugs, since it is 1.8 times more active than the first line anti-TB drug ethambutol and 0.65 times less active than isoxyl.

Synthesis and biological evaluation of 3-amino-1,2,4-triazole derivatives as potential anticancer compounds

Two series of compounds carrying 3-amino-1,2,4-triazole scaffold were synthesized and evaluated for their anticancer activity against a panel of cancer cell lines using XTT assay. The 1,2,4-triazole synthesis was revisited for the first series of pyridyl derivatives. The biological results revealed the efficiency of the 3-amino-1,2,4-triazole core that could not be replaced and a clear beneficial effect of a 3-bromophenylamino moiety in position 3 of the triazole for both series (compounds 2.6 and 4.6) on several cell lines tested. Moreover, our results point out an antiangiogenic activity of these compounds. Overall, the 5-aryl-3-phenylamino-1,2,4-triazole structure has promising dual anticancer activity.

Design, synthesis and algicides activities of thiourea derivatives as the novel scaffold aldolase inhibitors

By using a new Fragment-Based Virtual Screen strategy, two series of novel FBA-II inhibitors (thiourea derivatives) were de novo discovered based on the active site of fructose-1, 6-bisphosphate aldolase from Cyanobacterial (CyFBA). In comparison, most of the N-(2-benzoylhydrazine-1-carbonothioyl) benzamide derivatives (L14～L22) exhibit higher CyFBA-II inhibitory activities compared to N-(phenylcarbamothioyl) benzamide derivatives (L1～L13). Especially, compound L14 not only shows higher CyFBA-II activity (Ki = 0.65 μM), but also exhibits most potent in vivo activity against Synechocystis sp. PCC 6803 (EC50 = 0.09 ppm), higher (7-fold) than that of our previous inhibitor (EC50 = 0.6 ppm). The binding modes of compound L14 and CyFBA-II were further elucidated by jointly using DOX computational protocol, MM-PBSA and site-directed mutagenesis assays. The positive results suggest that strategy adopted in this study was promising to rapidly discovery the potent inhibitors with novel scaffolds. The satisfactory algicide activities suggest that the thiourea derivatives is very likely to be a promising lead for the development of novel specific algicides to solve Cyanobacterial harmful algal blooms (CHABs).

Synthesis and antitumor evaluation of 5-(benzo[: D] [1,3]dioxol-5-ylmethyl)-4-(tert -butyl)- N -arylthiazol-2-amines

A series of novel N-aryl-5-(benzo[d][1,3]dioxol-5-ylmethyl)-4-(tert-butyl)thiazol-2-amines (C1-C31) were synthesized and evaluated for their antitumor activities against HeLa, A549 and MCF-7 cell lines. Some tested compounds showed potent growth inhibition properties with IC50 values generally below 5 μM against the three human cancer cells lines. Compound C27 showed potent activities against HeLa and A549 cell lines with IC50 values of 2.07 ± 0.88 μM and 3.52 ± 0.49 μM, respectively. Compound C7 (IC50 = 2.06 ± 0.09 μM) was the most active compound against A549 cell line, while compound C16 (IC50 = 2.55 ± 0.34 μM) showed the best inhibitory activity against the MCF-7 cell line. The preliminary mechanism of the inhibitory effect was investigated via further experiments, such as morphological analysis by dual AO/EB staining and Hoechst 33342 staining, and cell apoptosis and cycle assessment by FACS analysis. The results illustrated that compound C27 could induce apoptosis and cause both S-phase and G2/M-phase arrests in HeLa cell line. Therefore, compound C27 could be developed as a potential antitumor agent.

Design, syntheses and evaluation of benzoylthioureas as urease inhibitors of agricultural interest

Urea is one of the most used nitrogen fertilizers worldwide. However, occurrence of urea hydrolysis to ammonia and carbon dioxide on soil surface, catalyzed by soil ureases, considerably reduces nitrogen availability to crops. In this study, we describe the design, synthesis and screening of sixty five benzoylthioureas (BTUs) for their ability to inhibit purified jack bean and soil ureases. BTUs were readily obtained in one pot, two steps synthesis with no need of cumbersome procedures for product purification. In vitro assays revealed BTUs 11, 12, 14, 19-22 and 37 as the most active jack bean urease inhibitors. Such BTUs were found to be able to bind to both catalytic and allosteric sites of urease, acting therefore as mixed-type inhibitors. Out of 28 compounds that effectively inhibited soil ureases activity, BTUs 3, 6, 10, 12, 16, 19 and 22 were determined to be more potent than the reference inhibitor N-(butyl) thiophosphoric triamide (NBPT; 40%). The other 22 BTUs were as potent as NBPT on soil ureases. The temperature-tolerance of BTUs, along with their ability to inhibit soil ureases, makes of this class of compounds potential additive for urea-based fertilizers.

Synthesis and Cytotoxicity in Vitro of N-Aryl-4-(Tert-butyl)-5-(1H-1,2,4-triazol-1-yl)thiazol-2-amine

A series of novel N-aryl-4-(tert-butyl)-5-(1H-1,2,4-triazol-1-yl)thiazol-2-amines were synthesized in a green way. H2O2-NaBr Brominating circulatory system was used in the synthesis of the key intermediate in a mild condition. All of the target compounds were confirmed by1H NMR and elemental analysis and tested for their cytotoxicity against two different human cancer cell lines. The cytotoxicity assay revealed that some of the title compounds showed moderate to strong cytotoxic activities. Compound 2i was the most potent compound with the IC50 values of 9 μMagainst Hela cells and 15 μMagainst Bel-7402 cells, respectively.

Microwave Promoted Efficient Synthesis of N-Aryl-N′-aroyl Thioureas under Solvent-Free and Phase Transfer Catalysis Conditions

A simple, rapid and efficient method for the synthesis of N-aryl-N′-aroyl thioureas under phase transfer catalysis, microwave irradiation and solvent-free conditions is reported.

A mild and efficient synthesis of N-aryl-N′-aroyl thioureas under phase transfer catalysis and solvent-free conditions

A series of N-aryl-N′-aroyl thioureas 3a-m were synthesized in high yields (80.0-98.1%) by an environmentally benign, simple and efficient method under phase transfer catalysis and solvent-free conditions.