202865-64-3Relevant academic research and scientific papers
Discovery of Natural Product-Based Fungicides (II): Semisynthesis and Biological Activity of Sarisan Attached 3-Phenylisoxazolines as Antifungal Agents
Liu, Zhiyan,Cao, Jiangping,Yan, Xiaoting,Cheng, Wanqing,Wang, Xiaoguang,Yang, Ruige,Guo, Yong
, (2020/12/09)
Many phytopathogenic fungi cause severe damage to crop yields. In continuation of our research aimed at the discovery and development of natural products-based fungicides, a series of thirty-one sarisan attached 3-phenylisoxazolines were synthesized and evaluated for their antifungal activities against five phytopathogenic fungi (B. cinerea, C. lagenarium, A. solani, F. solani, and F. graminearum). Among all title sarisan derivatives, compounds IV2, IV14 and IV23 showed potent antifungal activity against some phytopathogenic fungi. In particular, compound IV2 exhibited a broad-spectrum and more potent antifungal activity against A. solani, F. solani, and F. graminearum than the commercial fungicide Hymexazol. In addition, compounds IV2, IV14 and IV23 also displayed relative low toxicity on normal NRK-52E cells. This work will give some insights into the development of sarisan derivatives as new fungicide candidates in plant protection.
Synthesis and antiproliferative properties of isoxazole analogs containing dibenzosuberane moiety
Moger, Manjunath,Pradhan, Ashok,Singh, Apoorva,Govindaraju, Darshan Raj Chenna,Hindupur, Rama Mohan,Pati, Hari N.
, p. 449 - 455 (2016/02/19)
A series of twelve novel isoxazole analogs containing dibenzosuberane moiety were synthesized using convergent synthesis approach. Newly synthesized compounds were well characterized by mass spectroscopy, IR and NMR spectroscopy. All the compounds were screened for their antiproliferative property against HepG2 and HeLa cell lines. Among them, compounds 7a, 7b, 7c, 7g and 7h were found active against both HepG2 and HeLa cell lines. Graphical Abstract: Twelve analogs of isoxazole containing dibenzosuberane moiety (7a-l) were synthesized, characterized and evaluated for their antiproliferative activity. [Figure not available: see fulltext.]
GLUCOSYLCERAMIDE SYNTHASE INHIBITORS FOR THE TREATMENT OF DISEASES
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Paragraph 0001023, (2015/04/15)
Described herein are compounds of Formula I, methods of making such compounds, pharmaceutical compositions and medicaments containing such compounds, and methods of using such compounds to treat or prevent diseases or conditions associated with the enzyme glucosylceramide synthase (GCS).
ISOXAZOLINE HYDROXAMIC ACID DERIVATIVES AS LPXC INHIBITORS
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Page/Page column 82-83, (2015/11/10)
This invention pertains generally to compounds of Formula I and compositions containing such compounds, as well as methods of using such compounds to treat bacterial infections. In certain aspects, the invention pertains to methods and compositions for tr
Fragment-based discovery of JAK-2 inhibitors
Antonysamy, Stephen,Hirst, Gavin,Park, Frances,Sprengeler, Paul,Stappenbeck, Frank,Steensma, Ruo,Wilson, Mark,Wong, Melissa
scheme or table, p. 279 - 282 (2009/04/16)
Fragment-based hit identification coupled with crystallographically enabled structure-based drug design was used to design potent inhibitors of JAK-2. After two iterations from fragment 1, we were able to increase potency by greater than 500-fold to provide sulfonamide 13, a 78-nM JAK-2 inhibitor.
OXAZOLIDINONE DERIVATIVES AS ANTIMICROBIALS
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Page/Page column 69-70; 72; 74; 95, (2010/10/20)
The present invention relates to certain substituted phenyl oxazolidinones and to processes for the synthesis of the same. This invention also relates to pharmaceutical compositions containing the compounds of the present invention as antimicrobials. The compounds are useful antimicrobial agents, effective against a number of human and veterinary pathogens, including gram-positive aerobic bacteria, for example, multiple-resistant staphylococci, streptococci and enterococci as well as anaerobic organisms, for example, Bacterioides spp. and Clostridia spp. species, and acid fast organisms, for example, Mycobacterium tuberculosis, Mycobacterium avium and Mycobacterium spp.
ANTIBACTERIAL COMPOUNDS
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Page 60, (2008/06/13)
A compound of the formula (I), or a pharmaceutically-acceptable salt, or in-vivo hydrolysable ester thereof wherein in (I) C is for example formula (D), (E), (H) wherein A and B are independently selected from formulae (i) and (ii) and R2b and R6b, R2b and R6a, R3a and R5a, are for example selected from H, F, OMe and Me; R2b’ and R6b’, R2a’ and R6a’, R3a’, R5a’ are for example selected from H, OMe and Me; R1a and R1b are for example selected from hydroxy, -OSi(tri-(1-6C)alkyl), NR5C(=W) R4, formla (a), formula (b) wherein HET-1 is for example isoxazolyl and HET-2 is for example triazolyl or tetrazolyl. Methods for making compounds of the formula (I), compositions containing them and their use as antibacterial agents are also described.
FUSED HETEROARYL DERIVATIVES FOR USE AS P38 KINASE INHIBITORS IN THE TREATMENT OF I.A. RHEUMATOID ARTHRISTIS
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Page/Page column 47, (2010/11/30)
Compounds of formula (I): wherein A is a 5-membered heteroaryl ring are inhibitors of p38 kinase and are useful in the treatment of conditions or disease states mediated by p38 kinase activity or mediated by cytokines produced by the activity of p38, such as rheumatoid arthritis.
Compounds and method for inhibiting MRP1
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Page column 49, (2010/02/05)
The present invention relates to a compound of formula (I), which is useful for inhibiting resistant neoplasms where the resistance is conferred in part or in total by MRP1.
