ChemInform Abstract: Synthesis of Benzimidazole Derivatives as Potential Antimicrobial Agents.

Abstract

The carboxylic hydrazides (I) are coupled with the isothiocyanates (II) to prepare the corresponding thiosemicarbazides (III). These are cyclized to form the triazolyl (IV) or the thiadiazolyl compounds (V) as outlined in the reaction scheme. Reaction of (III) with the phenacyl bromides (VI) produces the thiazolyl derivatives (VII). Most of the benzimidazoles prepared are active against Staphylococcus aureus, Escherichia coli and Candida albicans.

Synthesis of Some New Quinoxalines and 1,2,4‐Triazolo[4,3‐a]‐quinoxalines for Evaluation of in vitro Antitumor and Antimicrobial Activities

“…As a part of our ongoing research program on quinoxaline derivatives [1 -4], which may serve as leads for designing novel chemotherapeutic agents, we have recently reported the synthesis, anticancer and antimicrobial evaluation of various series of quinoxalines [3,4]. The results obtained from their in vitro screening have shown interesting percent tumor-growth inhibition on various cell lines.…”

A New Type of Synthesis of 1,2,3‐Thiadiazole and 1,2,3‐Diazaphosphole Derivatives Via‐Hurd‐Mori Cyclization

“…A recrystallization from ethyl alcohol was carried out. (11,12,13,14,15) An excess amount of thionyl chloride was stirred at room temperature and the thiosemicarbazones 6 or 7 or 8 or 9 or 10 were added in several portions. The mixtures were stirred at r.t. overnight until no more hydrogen chloride was produced, the product was washed with diethyl ether to give a good yields of the corresponding 1, 2, 3-thiodiazoles as fine powders.…”

“…Preliminary experiments were done using the human tumor cell line to identify the potential toxicity of four chosen selected newly synthesized compounds (11,12,16,17) (Fig. 1) in comparison to the known anticancer drug: doxorubicin by SRB using the method Skehan et al 38  Cells were plated in 96-multiwell plate (10 4 cells/well) for 24 hrs before treatment with compounds to allow attachment of cell to the wall of the plate.…”

“…Derivatives of 1,2,3-thiadiazoles and 1,2,3-diazaphosphole are known to exhibit antiinflammatory [1][2][3] , antiviral 4,5 , analgesic 6,7 , antimicrobial [8][9][10][11][12] , anticonvulsant [13][14][15][16] and antidepressant activity. 17 Among the pharmacological profiles of 1,2,3-thiadiazoles and 1,2,3-diazaphospholes, their antimicrobial, anticonvulsant and antidepressant properties seem to be the best documented.…”

Synthesis, characterization and antibacterial evaluation of some novel derivatives of 2-bromomethyl-benzimidazole

“…Both heteroatoms are nitrogen (N), which are present at non-adjacent position [3]. The benzimidazole moiety is an important heterocyclic ring, a wide variety of benzimidazole derivatives are known for their chemotherapeutic importance and antimicrobial activities [4][5][6][7][8][9], antifungal activity [10][11][12], anti-inflammatory [13] and antioxidant [14][15][16][17][18] in this context. Due to great potential of the moiety, synthesis of benzimidazole derivatives was carried out to evaluate their antimicrobial.…”