Bioorganic & Medicinal Chemistry Letters
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#1Rammohan R. Yadav Bheemanaboina (SWU: Southwest University)H-Index: 13
#2Juan Wang (SWU: Southwest University)H-Index: 3
Last. Cheng-He Zhou (SWU: Southwest University)H-Index: 41
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Abstract null null A novel type of sulfonyl-hybridized imidazolyl ethanols as potential DNA-targeting antibacterial agents was constructed via the unique ring-opened reaction of oxiranes by imidazoles for the first time. Some developed target hybrids showed potential antimicrobial potency against the tested microbes. Especially, imidazole derivative 5f could strongly suppressed the growth of MRSA (MIC = 4 μg/mL), which was 2-fold and 16-fold more potent than the positive control sulfathiazole an...
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In this paper, we report an efficient one-pot three-component reaction sequences comprising Cu(I)-catalyzed 1,3-dipolar cycloaddition (CuAAC) followed by Cu-catalyzed arylation of resulting 1,2,3-triazole in the presence of ionic liquid [Emim]BF4 under microwave conditions involving. The newly synthesized derivatives were screened for in vitro antibacterial inhibition potency against both gram+ve and gram-ve strains. Among the tested compounds, 4f exhibited significant inhibition activity with M...
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#1Muhammed Alzweiri (UJ: University of Jordan)H-Index: 6
#2Amsha A. Alsegiani (UT: University of Toledo)
Last. L. M. Viranga Tillekeratne (UT: University of Toledo)H-Index: 12
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Alzheimer's disease (AD) is a neurodegenerative disorder, projected to be the second leading cause of mortality by 2040. AD is characterized by a progressive impairment of memory leading to dementia and loss of ability to carry out daily functions. In addition to the deficiency of acetylcholine release in synapse, there are other mechanisms explaining the etiology of the disease. The most disputing ones are associated with the accumulation of damaged proteins β-amyloid Aβ and hyperphosphorylated...
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#1Cong-Truong Nguyen (SNU: Seoul National University)H-Index: 2
#2Minh Thanh La (SNU: Seoul National University)
Last. Jeewoo Lee (SNU: Seoul National University)H-Index: 31
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A series of O-substituted analogs of the C-ring-truncated scaffold of deguelin designed as heat shock protein 90 (HSP90) C-terminal inhibitors were investigated as novel antitumor agents against human epidermal growth factor receptor 2 (HER2)-positive breast cancer. Among the synthesized compounds, compound 37 displayed significant inhibition in both trastuzumab-sensitive and trastuzumab-resistant breast cancer cells with little cytotoxicity to normal cells. Mechanistic studies of compound 37 ca...
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#1Andrew T. Riley (SIUE: Southern Illinois University Edwardsville)
#2Tristan C. Sanford (SIUE: Southern Illinois University Edwardsville)
Last. Minako Sumita (SIUE: Southern Illinois University Edwardsville)H-Index: 1
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Abstract Modifications of RNA molecules have a significant effect on their structure and function. One of the most common modifications is the isomerization from uridine to pseudouridine. Despite its prevalence in natural RNA sequences, organic synthesis of pseudouridine has been challenging because of the stereochemistry requirement and the sensitivity of reaction steps to moisture. Herein, a semi-enzymatic synthetic route is developed for the synthesis of pseudouridine using adenosine 5’-monop...
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#1Matthew D. Hill (BMS: Bristol-Myers Squibb)H-Index: 10
#2Haiquan Fang (BMS: Bristol-Myers Squibb)H-Index: 7
Last. Andrew P. Degnan (BMS: Bristol-Myers Squibb)H-Index: 10
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Abstract We describe our efforts to identify structurally diverse leads in the triazole-containing N1-carboline series of bromodomain and extra-terminal inhibitors. Replacement of the N5 “cap” phenyl moiety with various heteroaryls, coupled with additional modifications to the carboline core, provided analogs with similar potency, improved pharmacokinetic properties, and increased solubility compared to our backup lead, BMS-986225 (2). Rapid SAR exploration was enabled by a convergent, synthetic...
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#1Alexander O. Pritchard (UM: University of Manitoba)H-Index: 2
#2Dion B. Nemez (UM: University of Manitoba)H-Index: 3
Last. John L. Sorensen (UM: University of Manitoba)H-Index: 12
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Abstract Forskolin (1) is a diterpene found in the Coleus forskohlii plant that has been examined for its medical properties resulting from adenylyl cyclase activation. This article describes a straightforward purification method of 1 from commercially available weight loss capsules. In addition, there has been some ambiguity with respect to the use of the name ‘forskolin’ to describe 1 and related diterpenes, which this report serves to eliminate. Herein we detail the complete spectroscopic cha...
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#1Tianqi Wang (NKU: Nankai University)H-Index: 7
#2Rong Zhang (Sichuan University)H-Index: 1
Last. Rong Xiang (NKU: Nankai University)H-Index: 66
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JmjC domain-containing protein 6 (JMJD6) has been thought as a potential target for various diseases particularly cancer. However, few selective JMJD6 inhibitors have been reported. In this investigation, molecular docking and biological activity evaluation were performed to retrieve new JMJD6 inhibitors, which led to the identification of a hit compound, J2. Further structural optimization and structure-activity relationship (SAR) analysis towards J2 were carried out, which gave a new potent JM...
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#1C.B. Pradeep Kumar (Malnad College of Engineering)H-Index: 3
#2Madihalli S. Raghu (New Horizon College of Engineering)H-Index: 9
Last. Fahad A. Alharthi (KSU: King Saud University)H-Index: 8
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A Ta2O5-anchored-piperidine-4-carboxylic acid (PPCA) nanoparticle has been synthesized and characterized. It was then used as a highly effective nanocatalyst for the synthesis of quinolin-2(1H)-one derivatives through C-O bond functionalization. The special advantage of this heterogeneous solid catalyst is the reusability of the catalyst for up to five cycles without any noticeable reduction in product yields. In comparison, healthy reaction profiles, wide substrate scope, excellent yields and e...
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#1Aravind R. Nesaragi (Karnatak University)H-Index: 2
#2Ravindra R. Kamble (Karnatak University)H-Index: 14
Last. Vijay M. KumbarH-Index: 3
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A modest, competent and green synthetic procedure for novel coumarinyl-1,3,4-oxadiazolyl-2-mercaptobenzoxazoles 8i-t has been reported. Analysis of the docked (PDB ID: 5IKR; A-Chain) poses of the compounds illustrated that they adopt identical conformations to the extremely selective COX-2 inhibitor. The biological outcomes as well as computational study suggested that the compounds originated to have elevated resemblance towards COX-2 enzyme than COX-1. The compounds 8i, 8l, 8q, 8r, 8s and 8t e...
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