Alzweiri, Muhammed Alsegiani, Amsha Karaj, Endri Almarghalani, Daniyah Tabaza, Yahia Shah, Zahoor Tillekeratne, Viranga
Published in
Bioorganic & medicinal chemistry letters
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 explain...
Choi, Seoung-Ryoung Narayanasamy, Prabagaran
Published in
Bioorganic & medicinal chemistry letters
Menaquinone (MK) plays essential role in the electron transport chain (ETC), suggesting MK biosynthesis enzymes as potential targets for drug development. Previously, we demonstrated that Methicillin-resistant Staphylococcus aureus (MRSA) is susceptible to naphthol-based compounds which were developed by mimicking demethylmenaquinone, a product of ...
Banerjee, Abhisek Velagaleti, Ranganadh Patil, Sandip Pawar, Mahesh Yadav, Pravin Kadam, Pradip Mohsin Qadri, Mohammad Chakraborti, Samitabh Saini, Jagmohan S Behera, Dayanidhi B
...
Published in
Bioorganic & medicinal chemistry letters
Cathepsin C plays a key role in the activation of several degradative enzymes linked to tissue destruction in chronic inflammatory and autoimmune diseases. Therefore, Cathepsin C inhibitors could potentially be effective therapeutics for the treatment of diseases such as chronic obstructive pulmonary disease (COPD) or acute respiratory distress syn...
Ramya Sucharitha, E Murali Krishna, Thupurani Manchal, Ravinder Ramesh, Gondru Narsimha, Sirassu
Published in
Bioorganic & medicinal chemistry letters
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 anti...
Yao, Dahong Jiang, Jin Zhang, Hualin Huang, Yelan Huang, Jian Wang, Jinhui
Published in
Bioorganic & medicinal chemistry letters
The excessive activation of histone deacetylase (HDAC) and mammalian target of rapamycin (mTOR) signaling promotes tumor growth and progression. We proposed that dual targeting mTOR and HDAC inhibitors is a promising strategy for triple negative breast cancer (TNBC) treatment. In this study, a series of dual mTOR/HDAC6 inhibitors were designed and ...
Hill, Matthew D Fang, Haiquan Tokarski, John Fanslau, Carolynn Haarhoff, Zuzana Huang, Christine Kramer, Melissa Menard, Krista Monereau, Laura Morrison, John
...
Published in
Bioorganic & medicinal chemistry letters
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 p...
Wang, Tianqi Zhang, Rong Liu, Yang Fang, Zhen Zhang, Hailin Fan, Yan Yang, Shengyong Xiang, Rong
Published in
Bioorganic & medicinal chemistry letters
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 co...
Zhu, Long-Qing Fan, Xiao-Hong Li, Jun-Fang Chen, Jin-Hong Liang, Yan Hu, Xiao-Ling Ma, Shu-Meng Hao, Xiang-Yong Shi, Tao Wang, Zhen
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Published in
Bioorganic & medicinal chemistry letters
Inflammation as a host's excessive immune response to stimulation, is involved in the development of numerous diseases. To discover novel anti-inflammatory agents and based on our previous synthetic work on marine natural product Chrysamide B, it and a series of derivatives were synthesized and evaluated for their anti-inflammatory activity on inhi...
Nesaragi, Aravind R Kamble, Ravindra R Dixit, Shruti Kodasi, Barnabas Hoolageri, Swati R Bayannavar, Praveen K Dasappa, Jagadeesh Prasad Vootla, Shyamkumar Joshi, Shrinivas D Kumbar, Vijay M
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Published in
Bioorganic & medicinal chemistry letters
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...
Riley, Andrew T Sanford, Tristan C Woodard, Austin M Clerc, Elliot P Sumita, Minako
Published in
Bioorganic & medicinal chemistry letters
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 ...
