15816-25-8Relevant academic research and scientific papers
Microwave-assisted synthesis and biological evaluation of some benzimidazole derivatives containing a 1,2,4-Triazol Ring
Mentese, Emre,Karaali, Nesrin,Yimaz, Fatih,Uelker, Serdar,Kahveci, Bahittin
, p. 556 - 561 (2013)
A new series of 2-(4-(trifluoromethyl)phenyl)-1H-benzo[d]imidazole derivatives containing a 1,2,4-triazole ring were synthesized via microwave technique. This efficient procedure provides pure products within a few minutes. The newly synthesized compounds were confirmed by 1H NMR and 13C NMR spectra and they were screened for their lipase inhibition and antioxidant activities. Compounds 4a, 4b, 5a, and 5b showed very good scavenging activity. A series of 2-(4-(trifluoromethyl)phenyl)-1H-benzo[d] imidazole derivatives containing a 1,2,4-triazole ring were synthesized via microwave technique and screened for their lipase inhibition and antioxidant activities. Compounds 4a, 4b, 5a, and 5b showed very good scavenging activity.
DNA-Encoded Libraries: Hydrazide as a Pluripotent Precursor for On-DNA Synthesis of Various Azole Derivatives
Ma, Fei,Li, Jie,Zhang, Shuning,Gu, Yuang,Tan, Tingting,Chen, Wanting,Wang, Shuyue,Ma, Peixiang,Xu, Hongtao,Yang, Guang,Lerner, Richard A.
supporting information, p. 8214 - 8220 (2021/05/03)
DNA-encoded combinatorial chemical library (DEL) technology, an approach that combines the power of genetics and chemistry, has emerged as an invaluable tool in drug discovery. Skeletal diversity plays a fundamental importance in DEL applications, and relies heavily on novel DNA-compatible chemical reactions. We report herein a phylogenic chemical transformation strategy using DNA-conjugated benzoyl hydrazine as a common versatile precursor in azole chemical expansion of DELs. DNA-compatible reactions deriving from the common benzoyl hydrazine precursor showed excellent functional group tolerance with exceptional efficiency in the synthesis of various azoles, including oxadiazoles, thiadiazoles, and triazoles, under mild reaction conditions. The phylogenic chemical transformation strategy provides DELs a facile way to expand into various unique chemical spaces with privileged scaffolds and pharmacophores.
Pd(ii)-catalyzed direct C5-arylation of azole-4-carboxylates through double C-H bond cleavage
Li, Ziyuan,Ma, Ling,Xu, Jinyi,Kong, Lingyi,Wu, Xiaoming,Yao, Hequan
, p. 3763 - 3765 (2012/06/15)
The first palladium-catalyzed direct C5-arylation of azole-4-carboxylates with simple unactivated arenes through double C-H bond cleavage is realized. This protocol provided a straightforward access to diverse 5-arylsubstituted azole-4-carboxylic derivatives with good functional group tolerance. The Royal Society of Chemistry 2012.
AZOLE COMPOUND
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Page/Page column 20; 29, (2011/04/25)
[Problems] A compound which is useful as an active ingredient of a pharmaceutical composition for treating neuropathic pain is provided. [Means for Solution] The present inventors have made extensive studies on compounds having an FAAH inhibitory activity
Microwave-assisted synthesis of novel 2,4-dihydro-5-[4-(trifluoromethyl) phenyl]-3h-1,2,4-triazol-3-ones and potentiometric determination of their pKa in nonaqueous solvents
Oezil, Musa,Islamoglu, Fatih,Mentese, Emre,Kahveci, Bahittin
experimental part, p. 1967 - 1974 (2010/12/25)
The novel 4-amino- or 4-aryl-substituted 2,4-dihydro-5-[(4-trifluoromethyl) phenyl]-3H-1,2,4-triazol-3-ones 3a-3g were synthesized by reaction of N-(ethoxycarbonyl)-4-(trifluoromethyl)benzenehydrazonic acid ethyl ester (2) and primary amines or hydrazine
Reverse-benzamidine antimalarial agents: Design, synthesis, and biological evaluation
Berger, Olivier,Wein, Sharon,Duckert, Jean-Frederic,Maynadier, Marjorie,Fangour, Siham El,Escale, Roger,Durand, Thierry,Vial, Henri,Vo-Hoang, Yen
scheme or table, p. 5815 - 5817 (2010/11/17)
In the frame of the development of bis-cationic choline analogs, the RSA of bis-N-alkylamidines were studied and a new series of reverse-benzamidine derivatives was designed. Contrary to the lipophilicity, the basicity of alkylamidine compounds directly influences their antimalarial potencies.
EPOTHILONE ANALOGUES MODIFIED AT POSITIONS C12-C13 AS ANTICANCER DRUGS
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Page/Page column 32-33, (2008/12/06)
The invention relates to analogues of epothilones of formulae (A), (B), (I) and (II), uses and methods of making the same.
Orally efficacious NR2B-selective NMDA receptor antagonists
Claiborne, Christopher F.,McCauley, John A.,Libby, Brian E.,Curtis, Neil R.,Diggle, Helen J.,Kulagowski, Janusz J.,Michelson, Stuart R.,Anderson, Kenneth D.,Claremon, David A.,Freidinger, Roger M.,Bednar, Rodney A.,Mosser, Scott D.,Gaul, Stanley L.,Connolly, Thomas M.,Condra, Cindra L.,Bednar, Bohumil,Stump, Gary L.,Lynch, Joseph J.,Macaulay, Alison,Wafford, Keith A.,Koblan, Kenneth S.,Liverton, Nigel J.
, p. 697 - 700 (2007/10/03)
A novel series of benzamidines was synthesized and shown to exhibit NR2B-subtype selective NMDA antagonist activity. Compound 31 is orally active in a carrageenan-induced rat hyperalgesia model of pain and shows no motor coordination side effects.
Triazole derivatives
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, (2011/03/17)
The present invention relates to triazole and imidazole derivatives of formula I and to their pharmaceutically acceptable acid addition salts. These compounds are NMDA receptor subtype blockers and are useful for the treatment of diseases related to the NMDA receptor.
