Eco-friendly Synthesis of Some New Benzylidene-iminothiazolyl-pyrazol-3-ol Derivatives via One-Pot Multicomponent Reaction and Evaluation of Antioxidant Activities

In present work, one-pot multicomponent reaction (MCR) route for the synthesis of benzylideneiminothiazolyl- pyrazol-3-ol derivatives (5a-p) by reacting ethyl cyanoacetate (1), substituted benzaldehyde (2a-c), thiosemicarbazide (3) and substituted phenacyl bromide (4a-g). This reaction proceeds by using bleaching earth clay (BEC) (pH 12.5) in PEG-400 as a green reaction media. All the synthesized compounds were characterized by IR, 1H NMR, 13C NMR and mass spectral data. The pharmacological investigation of the synthesized compounds suggest that most of them showed good antioxidant activity.

Novel Structural Hybrids of Pyrrole and Thiazole Moieties: Synthesis and Evaluation of Antibacterial and Antifungal Activities

One of the best ways to design new biocidal agents is synthesizing hybrid molecules by combining two or more bioactive moieties in a single molecular scaffold. So, new series of pyrroles bearing a thiazole moiety were synthesized using 1-methyl-1H-pyrrole-2-carbaldehyde thiosemicarbazones 1a–c. Cyclization of thiosemicarbazone derivatives 1a–c with ethyl chloroacetate, ethyl 2-chloropropanoate, chloroacetone and phenacyl bromide afforded the corresponding thiazolidin-4-ones 2a–c, 5-methylthiazolidin-4-ones 3a–c, 4-methyl-2,3-dihydrothiazoles 4a–c, and 4-phenyl-2,3-dihydrothiazoles 5a–c, respectively. The antimicrobial activity of the new thiazole derivatives was evaluated.

Synthesis, characterization and photostability study of triazole derivatives

heterocyclic derivative contain triazole ring was synthesized and characterized the product and their structures by infrared spectroscopy, 1H-NMR, 13C-NMR and instrumental techniques. Compound (4) was synthesized by reacting of Schiff base (3) with an three moles of alkyl halide (p-phenyl phenacyl bromide). Final product played an important role in photostabilizer of polymer (PS), and showed the activity as a photostabilizer when exposed to UV light (300 hours).

Synthesis and Anticonvulsant activity of new 5-((1-(2-(4-substituted phenacyl bromide)-2-oxoethyl)-2-phenyl-1H-indol-3yl) methylene) pyrimidine-2, 4, 6(1H, 3H, 5H)-trione Derivatives

In the current scenario we have plant to study to synthesize novel indole derivatives (4a-d) and (5a-b) which have the target activity like anti-convulsion and anti microbial etc. In the primary phase, we synthesized 2-phenyl-1H-indole reacted with Phosphorus oxychloride and N, N’-dimethylformamide by using vilsmeier reagent formylation of a new compound 2-phenylindole-3-carbaldehyde (2). The 2-phenylindole-3-carbaldehyde was reacted with substituted phenacyl bromide, K2CO3 and TBAB (Tetra butyl ammonium bromide) into the presence of N, N’-dimethylformamide to gives [1-(2-(4-substituted phenacyl bromide)-2-oxoethyl)-2-phenylindole-3-carbaldehyde (3a-d). The compound [1-(2-(4- substituted phenacyl bromide)-2-oxo-ethyl)-2-phenylindole-3-carbaldehyde was permitted to mixed with various substituted phenacyl bromide gives corresponding indole derivatives. The indole derivatives (3a-d) were reacted with barbituric acid and thiobarbituric acid dissolved into the methanol at reflux for 4h to gives afforded compounds (4a-d) and (5a-b). The final indole barbituric derivatives (4a-d) and (5a-b) were synthesized from substituted phenacyl bromide by the react with methanol and recrystalized from ethanol. The last compound has been completed on the basis of spectra FT-IR and 1H NMR. All the value of FT-IR, 1H NMR, Solubility and TLC were considered to be prominent. The pharmacological screening through ear electrode induced current 50mA for 0.2 seconds in electro-convulsiometer for anticonvulsant activity. The synthesize compounds were establish to be 4b, 4c, 4d, and 5a. The compound 4c and 5a were established to be the most potent compound through compare to standard drugs phenytoin sodium.

Synthesis of Imidazo [1, 2-a] Pyridine Derivatives Using Copper Silicate as an Efficient and Reusable Catalyst

Synthesis of imidazo [1, 2-a] pyridines derivatives were reported from 2-aminopyridine and various substituted phenacyl bromide using copper silicate as an efficient, eco-friendly, and reusable catalyst. The present protocol offers various advantages, such as the use of less hazardous solvent, high yield, and operationally simple procedure.

Synthesis and spectral characterization of some new thiazolopyrimidine derivatives

Thiazolopyrimidnes are considered one of the most interesting classes in heterocyclic chemistry due to their pharmaceutical importance. Herein, we report the synthesis of some new heterocyclic compounds containing thiazolopyrimidine starting from compound (1) which was previously prepared in literature. The starting compound was allowed to react with different alkylating agents such as chloroacetone, chloroacetyl chloride, and phenacyl bromide to afford derivatives (2-4). Compound (5), benzylidene derivative, was obtained by the reaction of compound (2) with benzaldehyde while amino-dicarbonitrile compound (6) can be obtained by the reaction of compound (5) and malononitrile. Acetylation of amino group in compound (6) with chloroacetyl chloride led to formation of compound (7). Nucleophilic substitution of chlorine in compound (7) by aniline gave compound (8) which further subjected the Munich reaction to form compound (9). All new synthesized compounds were characterized using different elemental and spectral analysis.

Synthesis, Biological Profile, and Molecular Docking of Some New BisImidazole Fused Templates and Investigation of Their Cytotoxic Potential as Anti-tubercular and/or Anticancer Prototypes

Background: There is a great need to discover more drugs with antimycobacterial activities to fight lung cancer and tuberculosis (two of the deadliest diseases world-wide). To our knowledge, the present study is the first to report antimycobacterial activity of imidazole-fused heterocycles. Objective: Construction of some bis-imidazole fused heterocycles with potential anti-tubercular and/or potent antitumor activities. Method: A series of bis-imidazole fused derivatives 6-8 and 13-16 was constructed using bis-phenacyl bromide derivative 2 as a synthetic platform. Compound 2 was also used to access bis-quinoxaline 20, bis-benzothiazine derivatives 23, and bisthiazolopyrimidine derivatives 26. The new bis-imidazole derivatives were evaluated for their anticancer activity against lung carcinoma cell line (A-549) using Cisplatin as a reference drug. The new compounds were also screened for their antitubercular activity against M. tuberculosis (ATCC 25177) using Isoniazid as a reference drug. Result: Among the new bis-imidazole derivatives, three examples showed remarkable antitumor activities while five other compounds showed high antimycobacterial activity. Conclusion: A novel series of bis-imidazole fused heterocycles was developed. Multiple prototypes of this new series showed remarkable anti-tubercular and/or potent antitumor activities.

Synthesis and Biological Evaluation of Novel Thiazole Hydrazines as Antimicrobial and Antimalarial Agents

Synthesis of some novel thiazole hydrazine derivatives from thiosemicarbazones of salicylaldehyde and 5-chlorosalicylaldehyde with phenacyl bromide in ethanol under reflux condition is reported. The synthesized compounds were characterized by spectral analysis and further screened against - S. aureus, E. coli, P. aeruginosa, S. pyogenus bacteria, and against C. albicans, A. clavatus, and A. niger fungal strains. Most of the compounds were active against E. coli and C. albicans. Antimalarial screening against Plasmodium falciparum showed moderate to the good activity of the synthesized compounds but less than the standard quinine. One of the synthesized compounds (4c) exhibited promising antimalarial activity against Plasmodium falciparum with IC50 close to the standard quinine.