Synthesis and antibacterial activity of some 5-guanylhydrazone/thiocyanato-6-arylimidazo[2,1-b]-1,3,4-thiadiazole-2-sulfonamide derivatives†

Gadad, Andanappa K.; Mahajanshetti, Chanabasappa S; Nimbalkar, Sudarshan; Raichurkar, Anandkumar

doi:10.1016/s0223-5234(00)00166-5

Cited by 229 publications

(63 citation statements)

References 4 publications

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“…The genotypic plasticity of metabolic networks has very practical implications for these efforts and the long-term success of the drugs that they produce. Multiple existing drugs target the metabolism of pathogens, such as sulfonamides, fosmidomycin, and isoniazid (18)(19)(20)(21). An ideal enzymatic drug target has to fulfill several criteria, among them that the target is essential for the pathogen's survival.…”

mentioning

confidence: 99%

Superessential reactions in metabolic networks

Barve

Rodrigues²,

Wagner³

2012

Proc. Natl. Acad. Sci. U.S.A.

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The metabolic genotype of an organism can change through loss and acquisition of enzyme-coding genes, while preserving its ability to survive and synthesize biomass in specific environments. This evolutionary plasticity allows pathogens to evolve resistance to antimetabolic drugs by acquiring new metabolic pathways that bypass an enzyme blocked by a drug. We here study quantitatively the extent to which individual metabolic reactions and enzymes can be bypassed. To this end, we use a recently developed computational approach to create large metabolic network ensembles that can synthesize all biomass components in a given environment but contain an otherwise random set of known biochemical reactions. Using this approach, we identify a small connected core of 124 reactions that are absolutely superessential (that is, required in all metabolic networks). Many of these reactions have been experimentally confirmed as essential in different organisms. We also report a superessentiality index for thousands of reactions. This index indicates how easily a reaction can be bypassed. We find that it correlates with the number of sequenced genomes that encode an enzyme for the reaction. Superessentiality can help choose an enzyme as a potential drug target, especially because the index is not highly sensitive to the chemical environment that a pathogen requires. Our work also shows how analyses of large network ensembles can help understand the evolution of complex and robust metabolic networks.drug resistance | drug target identification | essential reactions

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mentioning

confidence: 99%

Superessential reactions in metabolic networks

Barve

Rodrigues²,

Wagner³

2012

Proc. Natl. Acad. Sci. U.S.A.

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“…During the present investigation required imidazo [2,1-b] [1,3,4]thiadiazoles were prepared by the reaction of 2-amino-1,3,4-thiadiazole (1) with appropriately substituted α-haloketones (phenacylbromides) in dry ethanol as hydrobromides, which on neutralization with aqueous sodium carbonate solution gave corresponding free bases Animals with serum glucose levels >250 mg/dL were considered diabetic and were used for the study. The animals were divided into two groups of six animals each.…”

Section: Resultsmentioning

confidence: 99%

“…properties such as anticancer [1], antitubercular [2], antibacterial [3], antifungal [4], anticonvulsant, analgesic [5] and antisecretory [6] activities. They have been reported to selectively inhibit several therapeutic receptors and enzymes, extending their applications in modern drug design.…”

Section: Introductionmentioning

confidence: 99%

Synthesis of novel 5-{[2-(4-fluorobenzyl)-6-arylimidazo[2,1-b] [1,3,4]thiadiazol-5-yl]methylene}thiazolidine-2,4-diones as potent Antidiabetic agents

Badiger¹

2015

IJSEA

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“…In an attempt to find novel compounds active against TB, a series of phenylacrylamides designed by molecular hybridization of trans-cinnamic acids and guanylhydrazones were synthesized and antiTB efficacy were evaluated (Scheme 3) (Bairwa et al, 2010). While cinnamic acids are already known for their antituberculosis efficacy, guanylhydrazones have been shown to have antimicrobial activity including an interesting gram-negative bacterial endotoxin lipopolysaccharide (LPS) sequestering activity (Gadad et al 2000;Wu et al 2009). M. tb.…”

Section: Cinnamic Amide Derivativesmentioning

confidence: 99%