18199-94-5

Upstream product

• 79-04-9 chloroacetyl chloride 
• 28004-62-8 2-amino-5-(4-chlorophenyl)-1,3,4-thiadiazole 
• 64310-32-3 C₈H₈ClN₃OS 
• 104-88-1 4-chlorobenzaldehyde 
• 74-11-3 para-chlorobenzoic acid 
• 64310-32-3 1-(4-chlorobenzoyl)thiosemicarbazide 
• 122-01-0 4-chloro-benzoyl chloride 
• 5706-80-9 4-chlorobenzaldehyde thiosemicarbazone 
• 20038-92-0 C-(4-Chlor-phenylazo)-thioformamid 

Downstream Products

• 89335-19-3 2-[{5-(4-chlorophenyl)-[1,3,4]-thiadiazol-2-yl}imino]-1,3-thiazolidin-4-one 
• 1303531-66-9 C₁₄H₁₅ClN₄O₂S 
• 1303531-65-8 C₁₈H₂₅ClN₄OS 
• 1303531-64-7 C₁₈H₂₅ClN₄OS 
• 89335-29-5 5-benzylidene-2-[{5-(4-chlorophenyl)-[1,3,4]-thiadiazol-2-yl}imino]-1,3-thiazolidin-4-one 
• 1248828-38-7 2-[{5-(4-chlorophenyl)-[1,3,4]-thiadiazol-2-yl}imino]-5-(3,4-dimethoxybenzylidene)-1,3-thiazolidin-4-one 

Relevant academic research and scientific papers

Design of benzothiazole-1,3,4-thiadiazole conjugates: Synthesis and anticonvulsant evaluation

Various 2-[(6-substituted-1,3-benzothiazol-2-yl)amino]-N-[5-substituted- phenyl-1,3,4-thiadiazol-2-yl]acetamides were synthesized with a prospective exploration of "lead hopping", using pharmacophoric elements for in vivo anticonvulsant activity. This yielded three potent candidates (5i, 5t, and 5u) in the preliminary screening employing the maximal electroshock seizure (MES) and the subcutaneous pentylenetetrazole (scPTZ) test, showing minimal neurotoxicity. Their quantitative study indicated an increase of nearly 2-10 times for the MES test and 7- to 67-fold for the scPTZ test in the protective index, the keystone in drug discovery for anticonvulsant activity. Various 2-[(6-substituted-1,3-benzothiazol-2-yl)amino]-N-[5-substituted-phenyl-1,3, 4-thiadiazol-2-yl]acetamides were synthesized with a prospective exploration of "lead hopping", using pharmacophoric elements for in vivo anticonvulsant activity. Three potent candidates (5i, 5t, and 5u) with minimal neurotoxicity were identified in the MES and scPTZ tests.

2-Heteroarylimino-5-arylidene-4-thiazolidinones as a new class of non-nucleoside inhibitors of HCV NS5B polymerase

Hepatitis C virus (HCV) NS5B polymerase is an important and attractive target for the development of anti-HCV drugs. Here we report on the design, synthesis and evaluation of twenty-four novel allosteric inhibitors bearing the 4-thiazolidinone scaffold as

Synthesis, docking, and biological evaluation of thiazolidinone derivatives against hepatitis C virus genotype 4a

Hepatitis C virus (HCV) genotype 4a (GT4a) is prevalent in Egypt. It did not gain the necessary scientific focus despite its high resistance. Since the crystal structure NS5B (RNA-dependent RNA polymerase) of HCV GT4a has not been resolved until now, homology modeling was conducted to build and validate the 3D model of the enzyme. Ligand binding sites including the allosteric thumb II pocket were detected and used in lead optimization. Sixty new 4-thiazolidinone derivatives have been virtually designed and docked into thumb II site of HCV NS5B GT4a using rigid docking approach. Eighteen compounds (7a–r) that show good docking scores were synthesized and tested in vitro against NS5B GT4a. Compounds 7b and 7n showed the best inhibitory activity (IC50 = 0.338 and 0.342 μM, respectively). Compounds 7a, 7b, 7c, 7d, 7k, 7n, 7q, and 7r that have IC50 values less than 2 μM were assessed for cellular anti-HCV GT4a activity using human hepatoma cell line (Huh 7.5). The percentages of viral growth inhibition are between 79.67 and 94.77%. Compound 7b is the most active in the in vitro and cellular assays and could be considered a potential new lead for future anti-HCV studies. [Figure not available: see fulltext.]

Synthesis and Biological Evaluation of Oxadiazole Clubbed Thiadiazole Derivatives as Antimicrobial Agents

A series of 1,3,4-oxadiazole clubbed 1,3,4-thiadiazole derivatives were synthesized and assessed in vitro for their activity as antimicrobial agents. The target compounds 2-(5-(substituted aryl)-1, 3, 4-oxadiazol-2-ylthio)-N-(5-(substituted aryl)-1, 3, 4-thiadiazol-2-yl) acetamides (5a-5s) were synthesized using a basic condensation reaction between 5-(substituted aryl)-1,3,4-oxadiazole-2-thiol and 2-chloro-N-(5-(substituted aryl)-1,3,4-thiadiazol-2-yl)acetamide in presence of K2CO3 as a scavenging agent and acetone as reaction solvent. The titled compounds synthesized here, exhibited excellent to moderate antimicrobial activity against a broad panel of antibacterial strains of Gram-positive and Gram-negative bacteria and fungi.

Synthesis and evaluation of novel 1,3,4-thiadiazole–fluoroquinolone hybrids as antibacterial, antituberculosis, and anticancer agents

A series of 5-substituted-1,3,4-thiadiazole-based fluoroquinolone derivatives were designed as potential antibacterial and anticancer agents using a molecular hybridization approach. The target compounds 16–25 were synthesized by reacting the correspondin

COMPOUNDS FOR MODULATING AQUAPORINS

The invention relates to compounds of formula (I) pharmaceutical compositions thereof and methods for modulating aquaporin 9.

Novel 3-nitrotriazole-based amides and carbinols as bifunctional antichagasic agents

3-Nitro-1H-1,2,4-triazole-based amides with a linear, rigid core and 3-nitrotriazole-based fluconazole analogues were synthesized as dual functioning antitrypanosomal agents. Such compounds are excellent substrates for type I nitroreductase (NTR) located in the mitochondrion of trypanosomatids and, at the same time, act as inhibitors of the sterol 14α-demethylase (T. cruzi CYP51) enzyme. Because combination treatments against parasites are often superior to monotherapy, we believe that this emerging class of bifunctional compounds may introduce a new generation of antitrypanosomal drugs. In the present work, the synthesis and in vitro and in vivo evaluation of such compounds is discussed.

Thiadiazole derivatives as potential anticonvulsant agents

A series of thiadiazole derivatives were synthesized with differently substituted benzoic acids which were cyclized to give differently substituted thiazolidin-4-one. Elemental analysis, IR,1HNMR,13C NMR and mass spectral data confir

Synthesis and evaluation of some 2-[(substituted) ethanoyl]amino- 5-aryl-1,3,4-thiadiazoles as diuretic agents

Twelve 2-[(substituted)ethanoyl]amino-5-aryl-1,3,4-thiadiazoles were prepared by the reaction of 2-(chloro ethanoyl)amino-5-aryl-1,3,4- thiadiazoles and various secondary amines. These compounds were screened for diuretic activity. The compounds namely 4a1, 4b2 and 4c2 showed good diuretic activity comparable with the standard drug acetazolamide at a dose level of 100 mg/kg, orally in albino rats.

Synthesis, characterization and antimicrobial activity of new thiadiazole derivatives

A series of thiadiazole derivatives were synthesized with differently substituted benzoic acids which were cyclized to give differently substituted thiazolidin-4-one. Elemental analysis, IR, 1H NMR, 13C NMR and mass spectral data confirmed the