Nitrofuryl heterocycles. IX. Some derivatives and analogs of 6,7-dihydro-3-(5-nitro-2-furyl)-5H-imidazo[2,1-b]thiazolium chloride

Synthesis of Thiazolium-Labeled 1,3,4-Oxadiazole Thioethers as Prospective Antimicrobials: In Vitro and in Vivo Bioactivity and Mechanism of Action

“…In drug design programs, one of the most efficient and promising approaches to explore securely bioactive structures is based on existing pharmacological skeletons from naturally occurring products, which have been verified to have a variety of advantages, including inartificial structural features, well-balanced physicochemical property, good biocompatibility, permissible environment friendliness, low cytotoxicity toward mammalian cells, and unique modes of action. − Among these native structural fragments, the thiazolium scaffold has been elaborately explored and highlighted because it is a crucially active component of thiamine (vitamin B 1 ) and thiamin pyrophosphate (ThDP) and serves as a cofactor of certain enzymes or multienzyme complexes, including pyruvate decarboxylase, α-ketoglutarate dehydrogenase, and transketolase, catalyzing several biochemical reactions in all living organisms; in addition, this favorable building block offers diverse capabilities in various aspects, such as improving the balance of the physicochemical and amphiphilic properties of target molecules, allowing decoration with functional groups, and reforming molecular pharmacological activities. − Thus, comprehensive investigations into this flexible motif are still being conducted, resulting in an array of thiazolium-tailored compounds with excellent potential applications (Figure ). For instance, furazolium chloride containing a thiazolium moiety was discovered and developed as a powerful antimicrobial agent against Proteus vulgaris, Pseudomonas aeruginosa, Salmonella typhosa, and Staphylococcus aureus . Meanwhile, Kim et al evaluated the antibacterial effects of a type of cephalosporin derivative carrying a thiazolium motif and found that these designed molecules exhibited potent bioactivities against Gram-positive and Gram-negative microorganisms except P.…”

“…For instance, furazolium chloride containing a thiazolium moiety was discovered and developed as a powerful antimicrobial agent against Proteus vulgaris, Pseudomonas aeruginosa, Salmonella typhosa, and Staphylococcus aureus. 21 Meanwhile, Kim et al 22 evaluated the antibacterial effects of a type of cephalosporin derivative carrying a thiazolium motif and found that these designed molecules exhibited potent bioactivities against Gram-positive and Gram-negative micro- 23−25 Inspired by these results, the integration of a thiazolium motif in a target molecule may lead to improved biological activities for its versatile functions of this valuable moiety.…”

Synthesis and Tautomeric Structure of 2-arylazo-4H-imidazo[2,1-b][1,3,4]thiadiazines

“…Considerable effort has been made therefore during the past three decades to study their synthesis and reactions. [1][2][3][4][5] Furthermore, a literature search revealed that although several imidazo [2,1-b] [1,3,4]thiadiazine derivatives have been prepared by the action of α-halocarbonyl compounds upon either 2-amino-1,3,4-thiadiazines [6][7][8] or 1-amino-2imidazolinethione derivatives, [7][8][9] the 2-arylazo derivatives of this fused-ring system have not been reported previously. 5 In continuation of our recent studies on the reactions of hydrazonoyl halides with heterocyclic thiones, [10][11][12][13][14][15][16][17] we now describe a new one-pot method for the preparation of 3substituted 2-arylazo-7-phenyl-4H-imidazo [2,1-b] [1,3,4]thiadiazines 4.…”

Determination of Untreated Whole-Milk Effects on In Vitro Antibacterial Activity

“…RESULTS AND DISCUSSION In addition to the antibiotics listed earlier, several antibacterials prepared in our laboratories were used for selected comparisons or gave results of special interest referred to below. The chemical name of each compound is given in Table 1, and specific details of their synthesis and activity may be found in reports by Burch (1, 2), Gever (G. Gever, U.S. Patent 2,802,002, 1957), Snyder and Benjamin (13,14), and Thomsen (15).…”