The Current Status of Heterocyclic Combinatorial Libraries

Nefzi, Adel; Ostresh, John M.; Houghten, Richard A.

doi:10.1021/cr960010b

Cited by 599 publications

(259 citation statements)

References 144 publications

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“…From the results of antimicrobial activity evaluation and Structure-activity relationship it could be concluded that that the derivative containing two 1,3-4-thiadiazole rings 6 and the condensed 1,2,4-triazolo [1,3,4]thiadiazole 9 revealed high antimicrobial activity against Bacillus subtilis. Furthermore, the attachment ribose sugar moiety increases the activity than the presence of either the galactose or mannose derivatives.…”

Section: Discussionmentioning

confidence: 99%

“…1,3,4-Thiadiazole ring containing compounds represent an important class of heterocyclic nitrogen compounds and their derivatives are characterized with a broad spectrum of biological activity in both agrochemical and pharmaceutical fields. Many 1,3,4-thiadiazoles derivatives have been used as "privileged" scaffolds to produce substances of interest in numerous therapeutic areas, such as anti-inflammatory, 1,2 antimicrobial, [3][4][5] anticonvulsant, 6-9 and antihypertensive.…”

Section: Introductionmentioning

confidence: 99%

“…Owing to the above facts and as continuation of our program of identification of new active leads that may be valuable in designing new, potent, selective and less toxic antimicrobial agents, [23][24][25] the present work reports the synthesis and antimicrobial activity of new substituted 1,2,4-triazolo [3,4-b] [1,3,4]-thiadiazole derivatives.…”

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confidence: 99%

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Antimicrobial Activity of Newly Synthesized 2,5-Disubstituted 1,3,4-Thiadiaozle Derivatives

Ramiz¹,

Arabia²

2011

Bulletin of the Korean Chemical Society

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A number of new 2,5-disubstituted 1,3,4-thiadiazole and their S-or N-substituted derivatives as well as the corresponding sugar hydrazone derivatives were synthesized and tested for their antimicrobial activity against Bacillus subtilis (Gram-positive), Pseudomonas aeruginosa (Gram-negative), and Streptomyces species (Actinomycetes). The synthesized compounds displayed different degrees of antimicrobial activities or inhibitory actions.

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Section: Discussionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

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Antimicrobial Activity of Newly Synthesized 2,5-Disubstituted 1,3,4-Thiadiaozle Derivatives

Ramiz¹,

Arabia²

2011

Bulletin of the Korean Chemical Society

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“…[20][21][22][23][24][25][26] In a series of studies on the generation of 1,3-dipoles in solution phase, Komatsu and co-wokers discovered that azomethine ylides (11 or 12) can be generated from asilylimines (10) by thermal 1,2-silatropy onto the imino nitrogen or by treatment with a trifluorosilane as a quaternization and desilylation reagent (Scheme 3). 27) In the former method, no additives are required and the reactions can be performed under completely neutral conditions.…”

Section: Generation and Cycloaddition Of Polymer-supported Azomethinementioning

confidence: 99%

“…By applying these 1,3-dipolar cycloaddition reactions to SPOS, they developed a novel solid-phase strategy for the synthesis of pyrrolidine and pyrrole derivatives from polymer-supported a-silylimines (16) by utilizing the characteristics of silicon. 28) Polymer-supported azomethine ylides (21) were generated from the corresponding a-silylimines (20) by thermal 1,2-silatropy or by treatment with a trifluorosilane, and the resulting species were then reacted with dipolarophiles (Scheme 4). A modification of the linker led to a traceless solid-phase synthesis.…”

Section: Generation and Cycloaddition Of Polymer-supported Azomethinementioning

confidence: 99%

Solid-phase organic synthesis of heterocyclic compounds

Izumi

2006

J. Pestic. Sci.

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The establishment of an efficient method of synthesizing heterocycles is required for the development of pharmaceuticals and agrochemicals, since many bioactive compounds have a heterocyclic ring. It is also necessary to prepare libraries of small organic compounds for investigations of function and the discovery of more bioactive compounds in pharmaceutical and agrochemical chemistry. Combinatorial and parallel synthetic methodologies provide the main driving force for the preparation of libraries for applications in the discovery of lead compounds and high-throughput medicinal chemistry within the pharmaceutical industry. [1][2][3] Many different formats of high-throughput chemistry are available and solid-phase organic synthesis (SPOS) plays a pivotal role allowing the convenient handling of large numbers of synthetic intermediates. 4,5) Since the combinatorial chemistry first appeared in the early 1990s, the way drugs are discovered has changed dramatically. The SPOS strategy has been a strong tool for high throughput synthesis and combinatorial chemistry.6-9) Synthetic intermediates are retained on the support and can be, therefore, quickly separated from the reaction mixture without extraction, concentration, and purification. SPOS is thus particularly advantageous for multi-step iterative synthesis. Various solid-phase automated synthesizers have been developed and are now commercially available. Even though several synthesizers for solution synthesis have been developed, automation is essentially easier in solid-phase synthesis than solution synthesis. In particular, the automated synthesis of peptides and oligonucleotides has allowed their facile and rapid preparation and greatly contributed to the elucidation of their functions. However, SPOS is not without its drawbacks since often extended development times are required to optimize new solid-phase chemical reactions. Actually, many laboratories have been engaged in the development of novel solidphase linking strategies and chemical technologies. This paper describes recent findings in, and a useful method for, the synthesis of heterocycle and nitrogen heterocycle compounds. Selenium-based solid-phase chemistry to include nitrogen-containing heterocyclesNicolaou and co-workers have been engaged in the development of novel solid-phase linking strategies and chemical technologies aimed at the construction of discovery-oriented, natural product-like libraries. [10][11][12] Toward this end, several natural product-like templates have been tethered to a solidsupport utilizing an intramolecular, selenium-mediated cycloaddition procedure. Encouraged by their success in developing chemistry and technology to produce natural productlike libraries of oxygen-containing heterocycles and carbocyclic frameworks [13][14][15][16] and due to the potential utility of such libraries in chemical biology investigations, 17,18) they sought to expand the scope of this selenium-based solid-phase chemistry to include nitrogen-containing heterocycles. Recently, they reported t...

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