- A sustainable approach towards the three-component synthesis of unsubstituted 1H-imidazoles in the water at ambient conditions
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A green protocol for the synthesis of unsubstituted imidazoles has been demonstrated herein. The reaction is realized using commercially available lipase enzyme, porcine pancreas lipase (PPL) in water. The reaction conditions are selective and mild which helped to tolerate a wide variety of functional groups to give the desired products in good chemical yields. (Figure presented.).
- Kapale, Suraj S.,Chaudhari, Hemchandra K.,Mali, Suraj N.,Takale, Balaram S.,Pawar, Hitesh
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p. 712 - 716
(2020/05/22)
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- Rh-Catalyzed Annulation of ortho-C?H Bonds of 2-Arylimidazoles with 1,4,2-Dioxazol-5-ones toward 5-Arylimidazo[1,2-c]quinazolines
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A Rh-catalyzed unique and direct approach for constructing a series of 5-arylimidazo[1,2-c]quinazolines in moderate to excellent yields from simple and readily available 2-arylimidazoles and 3-phenyl-1,4,2-dioxazol-5-ones was described. This procedure pro
- Wu, Xiaopeng,Sun, Song,Xu, Shengbo,Cheng, Jiang
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supporting information
p. 1111 - 1115
(2018/01/27)
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- PPAR AGONISTS, COMPOUNDS, PHARMACEUTICAL COMPOSITIONS, AND METHODS OF USE THEREOF
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Provided herein are compounds and compositions useful in increasing PPARδ activity. The compounds and compositions provided herein are useful for the treatment of PPARδ related diseases (e.g., muscular diseases, vascular disease, demyelinating disease, and metabolic diseases).
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Page/Page column 31; 72
(2017/11/10)
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- PPAR AGONISTS, COMPOUNDS, PHARMACEUTICAL COMPOSITIONS, AND METHODS OF USE THEREOF
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Provided herein are compounds of Formula (I) and compositions useful in increasing PPARS activity. The compounds and compositions provided herein are useful for the treatment of PPARS related diseases (e.g., muscular diseases, vascular disease, demyelinat
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Page/Page column 70; 71
(2016/05/02)
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- As opioid receptor antagonists or inverse agonists of the novel compounds
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Novel compounds which are antagonists or inverse agonists at one or more of the opioid receptors, pharmaceutical compositions containing them, to processes for their preparation.
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Paragraph 0396; 0397; 0397-0400
(2016/10/08)
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- Fe3O4/SiO2/(CH2)3N+Me3Br3- core-shell nanoparticles: A novel catalyst for the solvent-free synthesis of five- and six-membered heterocycles
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Functionalized magnetic core-shell nanoparticles [Fe3O4/SiO2/(CH2)3N+Me3Br3-] are prepared by co-precipitation method, characterized by transmission electron microscopy, FT-IR, X-ray diffraction, and vibrating sample magnetometer. The catalytic activity of these nanoparticles was tested in the syntheses of imidazole, benzothiazole, and perimidine derivatives, under solvent-free conditions. The catalyst was readily recycled by the use of an external magnetic field and could be reused five times without significant loss of activity or mass.
- Farrokhi, Azita,Ghodrati, Keivan,Yavari, Issa
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- COMPOUNDS FOR TREATMENT OF CANCER
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The present invention relates to pharmaceutical compositions for treating cancer comprising BRAF inhibitors, (e.g. vemurafenib) and/or MEK inhibitor, (e.g. trametinib, RO5068760), in combination with anti-tubulin compounds of the invention or other known tubulin inhibitors, and using such compositions for treating cancer such as melanoma, drug-resistant cancer, and cancer metastasis.
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-
Paragraph 00236; 00246
(2014/09/29)
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- An efficient and convenient synthesis of imidazolines and benzimidazoles via oxidation of carbon-nitrogen bond in water media
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The metal coordination complex K4[Fe(CN)6] is an efficient and environmentally benign catalyst for the synthesis of imidazolines and benzimidazoles from various aldehydes and 1,2-diamines in aqueous medium at room temperature. This protocol gives excellent yield of product with desired purity. Copyright
- Shaikh, Kabeer A.,Patil, Vishal A.,Shaikh, Parveen A.
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experimental part
p. 924 - 928
(2012/05/21)
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- Synthesis and antiproliferative activity of novel 2-aryl-4-benzoyl- imidazole derivatives targeting tubulin polymerization
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We previously reported the discovery of 2-aryl-4-benzoyl-imidazoles (ABI-I) as potent antiproliferative agents for melanoma. To further understand the structural requirements for the potency of ABI analogs, gain insight in the structure-activity relationships (SAR), and investigate metabolic stability for these compounds, we report extensive SAR studies on the ABI-I scaffold. Compared with the previous set of ABI-I analogs, the newly synthesized ABI-II analogs have lower potency in general, but some of the new analogs have comparable potency to the most active compounds in the previous set when tested in two melanoma and four prostate cancer cell lines. These SAR studies indicated that the antiproliferative activity was very sensitive to subtle changes in the ligand. Tested compounds 3ab and 8a are equally active against highly paclitaxel resistant cancer cell lines and their parental cell lines, indicating that drugs developed based on ABI-I analogs may have therapeutic advantages over paclitaxel in treating resistant tumors. Metabolic stability studies of compound 3ab revealed that N-methyl imidazole failed to extend stability as literature reported because de-methylation was found as the major metabolic pathway in rat and mouse liver microsomes. However, this sheds light on the possibility for many modifications on imidazole ring for further lead optimization since the modification on imidazole, such as compound 3ab, did not impact the potency.
- Chen, Jianjun,Li, Chien-Ming,Wang, Jin,Ahn, Sunjoo,Wang, Zhao,Lu, Yan,Dalton, James T.,Miller, Duane D.,Li, Wei
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experimental part
p. 4782 - 4795
(2011/09/20)
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- COMPOUNDS FOR TREATMENT OF CANCER
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The present invention relates to novel compounds having anti-cancer activity, methods of making these compounds, and their use for treating cancer and drug-resistant tumors, e.g. melanoma, metastatic melanoma, drug resistant melanoma, prostate cancer and drug resistant prostate cancer.
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Paragraph 0043; 00373
(2011/10/03)
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- SUBSTITUTED PYRAZOLO[1,5-a]PYRIMIDINE COMPOUNDS AS mTOR INHIBITORS
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Compounds of Formula I: and salts thereof in which R1, R2, R2a, R3, n, X and ring B have the meanings given in the specification, are inhibitors of mTOR and are useful in the treatment of diseases which are sensitive to inhibition of mTOR, such as cancers.
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Page/Page column 43
(2011/04/14)
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- NOVEL COMPOUNDS AS ANTAGONISTS OR INVERSE AGONISTS AT OPIOID RECEPTORS
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Novel compounds which are antagonists or inverse agonists at one or more of the opioid receptors, pharmaceutical compositions containing them, to processes for their preparation.
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- Synthesis, antimicrobial and antimycobacterial evaluation of [2-(substituted phenyl)-imidazol-1-yl]-pyridin-3-yl-methanones
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A series of [2-(substituted phenyl)-imidazol-1-yl]-pyridin-3-yl-methanones (111) were synthesized and screened for their antimicrobial and antimycobacterial activities. Further, a series of [2-(substituted phenyl)-benzimidazol-1-yl]-pyridin-3-yl-methanones (1220) reported in our earlier study was also screened for their antimycobacterial activity. The antimycobacterial activity results indicated that [2-(4-Nitro-phenyl)-imidazol- 1-yl]-pyridin-3-yl-methanone (8, minimum inhibitory concentration [MIC]=3.13 g) was equipotent as standard drug ciprofloxacin and [2-(4-Nitro-phenyl)- benzimidazol-1-yl]-pyridin-3-yl-methanone (16, MIC=1.56 g) was equipotent as standard drug ethambutol. The results of antimicrobial screening demonstrated that 2-[1-(Pyridine-3-carbonyl)-1H-imidazol-2-yl]-benzoic acid (compound 11, MIC=0.002 g) was two times more effective than standard drug ciprofloxacin (MIC=0.004 g) against tested bacterial strains and [2-(2,5-Dimethyl-phenyl)- imidazol-1-yl]-pyridin-3-yl-methanone (compound 3, MIC=0.005 g) was equipotent to the reference compound, fluconazole against tested fungal strains.
- Narasimhan, Balasubramanian,Sharma, Deepika,Kumar, Pradeep,Yogeeswari, Perumal,Sriram, Dharmarajan
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experimental part
p. 720 - 727
(2012/04/04)
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- METHOD OF TREATMENT USING NOVEL ANTAGONISTS OR INVERSE AGONISTS AT OPIOID RECEPTORS
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A method of treatment using pharmaceutical compositions containing novel antagonists or inverse agonists at opioid receptors for the treatment of binge eating disorder, anorexia nervosa, bulimia nervosa, excess drug or alcohol use, or eating disorder not otherwise specified.
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- Synthesis, antimicrobial and antiviral evaluation of substituted imidazole derivatives
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In the present study, we have synthesized 2-(substituted phenyl)-1H-imidazole (1-12) and (substituted phenyl)-[2-(substituted phenyl)-imidazol-1-yl]-methanone (13-26) analogues and screened them for their antimicrobial activity against Gram positive, Gram negative and fungal species. The results of antibacterial study indicated that compounds 15, 17 and 24 showed appreciable antibacterial activity and compound 26 emerged as the most potential antifungal agent. The results of SAR studies indicated that the presence of electron withdrawing groups is necessary for the antimicrobial activity of the synthesized compounds. The results of the present study indicated that compounds 15, 17 and 24 might be of interest for the identification of new antimicrobial molecules as their antibacterial activity is equivalent to the standard drug norfloxacin. Further, the antiviral screening of (substituted phenyl)-[2-(substituted phenyl)-imidazol-1-yl]-methanones (13-26) against a panel of viral strains indicated that compounds 16 and 19 can be selected as lead compounds for the development of novel antiviral agents.
- Sharma, Deepika,Narasimhan, Balasubramanian,Kumar, Pradeep,Judge, Vikramjeet,Narang, Rakesh,De Clercq, Erik,Balzarini, Jan
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experimental part
p. 2347 - 2353
(2009/12/03)
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- Direct Oxidative Conversion of Benzoyl Chlorides to 2-Imidazoles Using Heteropolyacids
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The reaction of benzoyl chlorides with ethylenediamine in the presence of catalytic amounts of Keggin-type heteropolyacids led to oxidative conversion of benzoyl chlorides to the corresponding 2-imidazoles in good yields.
- Sadjadi, Samaheh,Heravi, Majid M.,Poormohammad, Nargess,Oskooie, Hossein A.,Beheshtiha, Yahya. Sh.,Bamoharram, Fatemeh F.
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experimental part
p. 3119 - 3125
(2009/12/01)
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- An efficient synthesis of 2-arylimidazoles by oxidation of 2-arylimidazolines using activated carbon-O2 system and its application to palladium-catalyzed Mizoroki-Heck reaction
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Oxidative conversion of 2-substituted imidazoline (dihydroimidazole) to the corresponding imidazole was achieved by an activated carbon-O2 system. Also, the 2-arylimidazolines and 2-arylimidazoles have been found to work as simple ligands in the palladium-catalyzed Mizoroki-Heck reaction.
- Haneda, Satoshi,Okui, Ayaka,Ueba, Chigusa,Hayashi, Masahiko
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p. 2414 - 2417
(2007/10/03)
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- An efficient preparation of 2-imidazolines and imidazoles from aldehydes with molecular iodine and (diacetoxyiodo)benzene
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2-Imidazolines were easily prepared in quite good yields from the reaction of aldehydes and ethylenediamine with molecular iodine in the presence of potassium carbonate. Moreover, 2-imidazolines obtained were smoothly oxidized to the corresponding imidazoles in good yields using (diacetoxyiodo)benzene at room temperature. Georg Thieme Verlag Stuttgart.
- Ishihara, Midori,Togo, Hideo
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p. 227 - 230
(2007/10/03)
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