Lamani, Manjunath Malamas, Michael S Farah, Shrouq I Shukla, Vidyanand G Almeida, Michael F Weerts, Catherine M Anderson, Joseph Wood, JodiAnne T Farizatto, Karen L G Bahr, Ben A
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Published in
Bioorganic & medicinal chemistry
FAAH inhibitors offer safety advantages by augmenting the anandamide levels "on demand" to promote neuroprotective mechanisms without the adverse psychotropic effects usually seen with direct and chronic activation of the CB1 receptor. FAAH is an enzyme implicated in the hydrolysis of the endocannabinoid N-arachidonoylethanolamine (AEA), which is a...
Singh, Sylvia Wang, Minghui Gao, Ruixuan Teng, Peng Odom, Timothy Zhang, En Xu, Hai Cai, Jianfeng
Published in
Bioorganic & medicinal chemistry
Though antibiotics have been used for decades to treat bacterial infections, there is a great need for new treatment methods. Bacteria are becoming resistant to conventional antibiotics, as is the case with Methicillin resistant Staphylococcus aureus (MRSA). Herein we report the design of a series of lipidated α/Sulfono-α-AA heterogeneous peptides ...
Sutherland, Hamish S Tong, Amy S T Choi, Peter J Blaser, Adrian Franzblau, Scott G Cooper, Christopher B Upton, Anna M Lotlikar, Manisha Denny, William A Palmer, Brian D
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Published in
Bioorganic & medicinal chemistry
Analogues of the anti-tuberculosis drug bedaquiline, bearing a 3,5-dimethoxy-4-pyridyl C-unit, retain high anti-bacterial potency yet exert less inhibition of the hERG potassium channel, in vitro, than the parent compound. Two of these analogues (TBAJ-587 and TBAJ-876) are now in preclinical development. The present study further explores structure...
Dinh, Huyen Nakata, Eiji Lin, Peng Saimura, Masayuki Ashida, Hiroki Morii, Takashi
Published in
Bioorganic & medicinal chemistry
Ribulose-1,5-biphosphate carboxylase/oxygenase (RuBisCO), an enzyme in the Calvin-Benson-Bassham cycle of photosynthesis, catalyzes the first step of CO2 fixation in plants, algae, and photosynthetic bacteria. Despite of the important function in the global carbon cycle, RuBisCO suffers from a slow reaction rate and a competing reaction with O2 whi...
Suaifan, Ghadeer A R Y Mohammed, Aya A M
Published in
Bioorganic & medicinal chemistry
Kuskovsky, Rostislav Lloyd, Dina Arora, Kriti Plotkin, Balbina J Green, Jacalyn M Boshoff, Helena I Barry, Clifton 3rd Deschamps, Jeffrey Konaklieva, Monika I
Published in
Bioorganic & medicinal chemistry
C4-phenylthio β-lactams are a new family of antibacterial agents that have activity against two phylogenetically distant bacteria - Mycobacterium tuberculosis (Mtb) and Moraxella catarrhalis (M. cat). These compounds are effective against β-lactamase producing Mtb and M. cat unlike the clinically relevant β-lactam antibiotics. The structure-activit...
Yang, Zhikun Wang, Jine Tian, Hao He, Yan Duan, Hongxia Duan, Liusheng Tan, Weiming
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Bioorganic & medicinal chemistry
Computer-aided drug design has advanced by leaps and bounds, and has been widely used in various fields, and especially in the field of drug discovery. Although the crystal structure of the gibberellin (GA) receptor GID1A had been reported in previous studies, there is still a lack of designs of gibberellin functional analogue based GID1A. In the p...
Leechaisit, Ronnakorn Pingaew, Ratchanok Prachayasittikul, Veda Worachartcheewan, Apilak Prachayasittikul, Supaluk Ruchirawat, Somsak Prachayasittikul, Virapong
Published in
Bioorganic & medicinal chemistry
A library of bis-sulfonamides (9-26) were synthesized and tested for their aromatase inhibitory activities. Interestingly, all bis-sulfonamide derivatives inhibited the aromatase with IC50 range of 0.05-11.6 μM except for compound 23. The analogs 15 and 16 bearing hydrophobic chloro and bromo groups exhibited the potent aromatase inhibitory activit...
Zeng, Anqi Hua, Hua Liu, Li Zhao, Junning
Published in
Bioorganic & medicinal chemistry
Othman, Dina I A Selim, Khalid B El-Sayed, Magda A-A Tantawy, Atif S Amen, Yhiya Shimizu, Kuniyoshi Okauchi, Tatsuo Kitamura, Mitsuru
Published in
Bioorganic & medicinal chemistry
A series of new isoxazolyl, triazolyl and phenyl based 3-thiophen-2-yl-quinoline derivatives were synthesized adopting click chemistry approach. In addition, the synthesis of new useful synthon, (2-chloroquinolin-3-yl) (thiophen-2-yl) methanol, is reported. The obtained compounds were characterized by spectral data analysis and evaluated for their ...
