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NATASHA RIX SERIES

Synthesis and Antibacterial Activity of New Chiral Aminoalcohol and Benzimidazole Hybrids. İlknur Çiçek, Turgay Tunç, Hatice Ogutcu, Suzan Abdurrahmanoglu, Aslıhan Günel, Nadir Demirel.Inducible nitric oxide synthase inhibitors: A comprehensive update. Richa Minhas, Yogita Bansal, Gulshan Bansal.Bicyclic 5–6 Systems: Other Four Heteroatoms 2:2. European Journal of Medicinal Chemistry 2021, 213, 113174. Discovery and development of novel pyrimidine and pyrazolo/thieno-fused pyrimidine derivatives as potent and orally active inducible nitric oxide synthase dimerization inhibitor with efficacy for arthritis. Liu Zeng Chen, Hai Yang Shu, Jing Wu, Yun Long Yu, Duo Ma, Xin Huang, Ming Ming Liu, Xin Hua Liu, Jing Bo Shi.Organic & Biomolecular Chemistry 2021, 19 indoles through a cyclobutenylation/deprotection cascade. Bioorganic & Medicinal Chemistry Letters 2021, 44, 128106. Discovery of a novel inhibitor of nitric oxide production with potential therapeutic effect on acute inflammation. Long-Qing Zhu, Xiao-Hong Fan, Jun-Fang Li, Jin-Hong Chen, Yan Liang, Xiao-Ling Hu, Shu-Meng Ma, Xiang-Yong Hao, Tao Shi, Zhen Wang.Direct Alkylation of Heteroaryls Using Potassium Alkyl- and Alkoxymethyltrifluoroborates. Molander, Virginie Colombel, and Valerie A. 1,2,3,4-Tetrahydroquinoline-Based Selective Human Neuronal Nitric Oxide Synthase (nNOS) Inhibitors: Lead Optimization Studies Resulting in the Identification of N-(1-(2-(Methylamino)ethyl)-1,2,3,4-tetrahydroquinolin-6-yl)thiophene-2-carboximidamide as a Preclinical Development Candidate. Maddaford, Salvatore Zinghini, Suman Rakhit, John Andrews, David K. Annedi, Joanne Speed, Sarah Silverman, Gabriela Mladenova, Shawn P. Jailall Ramnauth, Paul Renton, Peter Dove, Subhash C.Target- and Mechanism-Based Therapeutics for Neurodegenerative Diseases: Strength in Numbers. Trippier, Kristin Jansen Labby, Dustin D. Novel Pyrazolopyrimidine as Potent and Orally Active Inducible Nitric Oxide Synthase (iNOS) Dimerization Inhibitor with Efficacy in Rheumatoid Arthritis Mouse Model. Jing Bo Shi, Liu Zeng Chen, Bao Shi Wang, Xin Huang, Ming Ming Jiao, Ming Ming Liu, Wen Jian Tang, Xin Hua Liu.The Journal of Organic Chemistry 2020, 85 Palladium-Catalyzed Direct Arylation of Alkylpyridine via Activated N-Methylpyridinium Salts.

Xue Chen, Wen-jing Li, Shun Li, Juan Tang, Xi Du, Xue-li Zheng, Mao-lin Yuan, Hai-yan Fu, Rui-xiang Li, Hua Chen.

Journal of the American Chemical Society 2021, 143 Synthesis of N-CF3 Alkynamides and Derivatives Enabled by Ni-Catalyzed Alkynylation of N-CF3 Carbamoyl Fluorides. This article is cited by 46 publications. Further 42 did not affect motor coordination up to doses of 1000 mg/kg, demonstrating a wide therapeutic margin. 2009, 52, 3047−3062) was confirmed as an iNOS dimerization inhibitor and was efficacious in the mouse formalin model of nociception and Chung model of neuropathic pain, without showing tolerance after repeat dosing. Compounds were triaged utilizing an LPS challenge assay coupled with mouse and rhesus pharmacokinetics and led to the identification of 4,7-imidazopyrazine 42 as the lead compound.

NATASHA RIX SERIES

By conformationally restricting the amide of this progenitor series, we describe the identification of a novel series of benzimidazole-quinolinone dual iNOS/nNOS inhibitors with low clearance and sustained exposure in vivo. Previously, we described the identification of a series of amide-quinolinone iNOS dimerization inhibitors that although potent, suffered from high clearance and limited exposure in vivo.

Inappropriate or excessive NO produced by iNOS and/or nNOS is associated with inflammatory and neuropathic pain. Three isoforms of nitric oxide synthase (NOS), dimeric enzymes that catalyze the formation of nitric oxide (NO) from arginine, have been identified.