Search Results - "Gotchev, Dimitar"

Preclinical Antiviral and Safety Profiling of the HBV RNA Destabilizer AB-161 by Lam, Angela M, Dugyala, Ravi R, Sheraz, Muhammed, Liu, Fei, Thi, Emily P, Graves, Ingrid E, Cuconati, Andrea, Steuer, Holly Micolochick, Ardzinski, Andrzej, Overholt, Nathan, Mason, Jeremy D, Gotchev, Dimitar, Cole, Andrew G, Harasym, Troy O, Sofia, Michael J

“…HBV RNA destabilizers are a class of small-molecule compounds that target the noncanonical poly(A) RNA polymerases PAPD5 and PAPD7, resulting in HBV RNA…”
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Spongipyran synthetic studies. Evolution of a scalable total synthesis of (+)-spongistatin 1 by Smith, Amos B., Sfouggatakis, Chris, Risatti, Christina A., Sperry, Jeffrey B., Zhu, Wenyu, Doughty, Victoria A., Tomioka, Takashi, Gotchev, Dimitar B., Bennett, Clay S., Sakamoto, Satoshi, Atasoylu, Onur, Shirakami, Shohei, Bauer, David, Takeuchi, Makoto, Koyanagi, Jyunichi, Sakamoto, Yasuharu

“…Three syntheses of the architecturally complex, cytotoxic marine macrolide (+)-spongistatin 1 ( 1) are reported. Highlights of the first-generation synthesis…”
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Synthetic Studies Toward (−)-FR901483 Using a Conjugate Allylation To Install the C-1 Quaternary Carbon by Gotchev, Dimitar B, Comins, Daniel L

“…Two approaches to the aza-tricyclo dodecane skeleton of (−)-FR901483 are reported. Both routes utilized a Grignard addition to an N-acylpyridinium salt to…”
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Spongistatin Synthetic Studies. Evolution of a Scalable Synthesis for the EF Fragment of (+)-Spongistatin 1 Exploiting a Petasis−Ferrier Union/Rearrangement Tactic by Smith, Amos B, Sfouggatakis, Chris, Gotchev, Dimitar B, Shirakami, Shohei, Bauer, David, Zhu, Wenyu, Doughty, Victoria A

“…An efficient, stereocontrolled, and scalable second-generation synthesis of (+)-3, an advanced EF subtarget for the total synthesis of (+)-spongistatin 1, has…”
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Structure–Activity Relationships and Discovery of a G Protein Biased μ Opioid Receptor Ligand, [(3-Methoxythiophen-2-yl)methyl]({2-[(9R)‑9-(pyridin-2-yl)-6-oxaspiro-[4.5]decan-9-yl]ethyl})amine (TRV130), for the Treatment of Acute Severe Pain by Chen, Xiao-Tao, Pitis, Philip, Liu, Guodong, Yuan, Catherine, Gotchev, Dimitar, Cowan, Conrad L, Rominger, David H, Koblish, Michael, DeWire, Scott M, Crombie, Aimee L, Violin, Jonathan D, Yamashita, Dennis S

“…The concept of “ligand bias” at G protein coupled receptors has been introduced to describe ligands which preferentially stimulate one intracellular signaling…”
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Structure-Activity Relationships and Discovery of (S)-6-Isopropyl-2-methoxy-3-(3-methoxypropoxy)-10-oxo-5,10-dihydro-6H-pyrido1,2-h1,7naphthyridine-9-carboxylic Acid (AB-452), a Novel Orally Available HBV RNA Destabilizer by Gotchev, Dimitar, Dorsey, Bruce D, Nguyen, Duyan, Kakarla, Ramesh, Dugan, Benjamin, Chen, Shuai, Gao, Min, Bailey, Laurèn, Liu, Fei, Harasym, Troy, Chiu, Tim, Tang, Sunny, Lee, Amy C-H, Cole, Andrew G, Sofia, Michael J

“…Approved therapies for hepatitis B virus (HBV) treatment include nucleos(t)ides and interferon alpha (IFN-α) which effectively suppress viral replication, but…”
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Structure–Activity Relationships and Discovery of ( S )-5-( tert -Butyl)-11-(difluoromethoxy)-9-methoxy-2-oxo-1,2,5,6-tetrahydropyrido[2′,1′:2,3]imidazo[4,5- h ]quinoline-3-carboxylic Acid (AB-161), a Novel Orally Available and Liver-Centric HBV RNA Destabilizer by Gotchev, Dimitar, Chen, Shuai, Dugan, Benjamin, Dorsey, Bruce D., Wang, Xu, Sheraz, Muhammad, Kowalski, Rose, Liu, Fei, Tang, Sunny, Chiu, Tim, Harasym, Troy, Graves, Ingrid E., Thi, Emily P., Mason, Jeremy D., Overholt, Nathan, Dugyala, Ravi, Lam, Angela M., Cole, Andrew G., Sofia, Michael J.

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Structure-Activity Relationships and Discovery of (S)-5-(tert-Butyl)-11-(difluoromethoxy)-9-methoxy-2-oxo-1,2,5,6-tetrahydropyrido2',1':2,3imidazo4,5-hquinoline-3-carboxylic Acid (AB-161), a Novel Orally Available and Liver-Centric HBV RNA Destabilizer by Gotchev, Dimitar, Chen, Shuai, Dugan, Benjamin, Dorsey, Bruce D, Wang, Xu, Sheraz, Muhammad, Kowalski, Rose, Liu, Fei, Tang, Sunny, Chiu, Tim, Harasym, Troy, Graves, Ingrid E, Thi, Emily P, Mason, Jeremy D, Overholt, Nathan, Dugyala, Ravi, Lam, Angela M, Cole, Andrew G, Sofia, Michael J

“…Lowering hepatitis B surface antigen (HBsAg) levels from covalently closed circular DNA (cccDNA) and the integrated genome could reduce the persistence of…”
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Structure–Activity Relationships and Discovery of (S)‑6-Isopropyl-2-methoxy-3-(3-methoxypropoxy)-10-oxo-5,10-dihydro‑6H‑pyrido[1,2‑h][1,7]naphthyridine-9-carboxylic Acid (AB-452), a Novel Orally Available HBV RNA Destabilizer by Gotchev, Dimitar, Dorsey, Bruce D., Nguyen, Duyan, Kakarla, Ramesh, Dugan, Benjamin, Chen, Shuai, Gao, Min, Bailey, Laurèn, Liu, Fei, Harasym, Troy, Chiu, Tim, Tang, Sunny, Lee, Amy C.-H., Cole, Andrew G., Sofia, Michael J.

“…Approved therapies for hepatitis B virus (HBV) treatment include nucleos­(t)­ides and interferon alpha (IFN-α) which effectively suppress viral replication,…”
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Structure-Activity Relationships and Discovery of ( S )-6-Isopropyl-2-methoxy-3-(3-methoxypropoxy)-10-oxo-5,10-dihydro-6 H -pyrido[1,2- h ][1,7]naphthyridine-9-carboxylic Acid (AB-452), a Novel Orally Available HBV RNA Destabilizer by Gotchev, Dimitar, Dorsey, Bruce D, Nguyen, Duyan, Kakarla, Ramesh, Dugan, Benjamin, Chen, Shuai, Gao, Min, Bailey, Laurèn, Liu, Fei, Harasym, Troy, Chiu, Tim, Tang, Sunny, Lee, Amy C-H, Cole, Andrew G, Sofia, Michael J

“…Approved therapies for hepatitis B virus (HBV) treatment include nucleos(t)ides and interferon alpha (IFN-α) which effectively suppress viral replication, but…”
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Rational Design of Macrocyclic Noncovalent Inhibitors of SARS-CoV-2 M pro from a DNA-Encoded Chemical Library Screening Hit That Demonstrate Potent Inhibition against Pan-Coronavirus Homologues and Nirmatrelvir-Resistant Variants by Wang, Xu, Gotchev, Dimitar, Fan, Kristi Yi, Vega, Marvin M, Mani, Nagraj, McGovern-Gooch, Kayleigh, Cuconati, Andrea, Tercero, Breanna, Wang, Xiaohe, Carpino, Philip, Maskos, Klaus, Centrella, Paolo A, Schmitt, Andreas, Preuss, Franziska, Prasad, Archna, Chen, Chia-Yi, Clark, Matthew A, Guilinger, John P, Johnstone, Shawn, von König, Konstanze, Keefe, Anthony D, Liu, Jenny, Turcotte, Stéphane, Zhang, Ying, Konz Makino, Debora L, Lam, Angela M, Cole, Andrew G, Sofia, Michael J

“…The recent global COVID-19 pandemic has highlighted treatments for coronavirus infection as an unmet medical need. The main protease (M ) has been an important…”
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Rational Design of Macrocyclic Noncovalent Inhibitors of SARS-CoV‑2 Mpro from a DNA-Encoded Chemical Library Screening Hit That Demonstrate Potent Inhibition against Pan-Coronavirus Homologues and Nirmatrelvir-Resistant Variants by Wang, Xu, Gotchev, Dimitar, Fan, Kristi Yi, Vega, Marvin M., Mani, Nagraj, McGovern-Gooch, Kayleigh, Cuconati, Andrea, Tercero, Breanna, Wang, Xiaohe, Carpino, Philip, Maskos, Klaus, Centrella, Paolo A., Schmitt, Andreas, Preuss, Franziska, Prasad, Archna, Chen, Chia-yi, Clark, Matthew A., Guilinger, John P., Johnstone, Shawn, von König, Konstanze, Keefe, Anthony D., Liu, Jenny, Turcotte, Stéphane, Zhang, Ying, Konz Makino, Debora L., Lam, Angela M., Cole, Andrew G., Sofia, Michael J.

“…The recent global COVID-19 pandemic has highlighted treatments for coronavirus infection as an unmet medical need. The main protease (Mpro) has been an…”
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HBsAg mRNA degradation induced by a dihydroquinolizinone compound depends on the HBV posttranscriptional regulatory element by Zhou, Tianlun, Block, Timothy, Liu, Fei, Kondratowicz, Andrew S., Sun, Liren, Rawat, Siddhartha, Branson, Jeffrey, Guo, Fang, Steuer, Holly Micolochick, Liang, Hongyan, Bailey, Lauren, Moore, Chris, Wang, Xiaohe, Cuconatti, Andy, Gao, Min, Lee, Amy C.H., Harasym, Troy, Chiu, Tim, Gotchev, Dimitar, Dorsey, Bruce, Rijnbrand, Rene, Sofia, Michael J.

“…In pursuit of novel therapeutics targeting the hepatitis B virus (HBV) infection, we evaluated a dihydroquinolizinone compound (DHQ-1) that in the nanomolar…”
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Host Poly(A) Polymerases PAPD5 and PAPD7 Provide Two Layers of Protection That Ensure the Integrity and Stability of Hepatitis B Virus RNA by Liu, Fei, Lee, Amy C. H, Guo, Fang, Kondratowicz, Andrew S, Micolochick Steuer, Holly M, Miller, Angela, Bailey, Lauren D, Wang, Xiaohe, Chen, Shuai, Kultgen, Steven G, Cuconati, Andrea, Cole, Andrew G, Gotchev, Dimitar, Dorsey, Bruce D, Rijnbrand, Rene, Lam, Angela M, Sofia, Michael J, Gao, Min

“…Noncanonical poly(A) polymerases PAPD5 and PAPD7 (PAPD5/7) stabilize hepatitis B virus (HBV) RNA via the interaction with the viral posttranscriptional…”
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A G protein-biased ligand at the μ-opioid receptor is potently analgesic with reduced gastrointestinal and respiratory dysfunction compared with morphine by DeWire, Scott M, Yamashita, Dennis S, Rominger, David H, Liu, Guodong, Cowan, Conrad L, Graczyk, Thomas M, Chen, Xiao-Tao, Pitis, Philip M, Gotchev, Dimitar, Yuan, Catherine, Koblish, Michael, Lark, Michael W, Violin, Jonathan D

“…The concept of ligand bias at G protein-coupled receptors broadens the possibilities for agonist activities and provides the opportunity to develop safer, more…”
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Novel heterocyclic systems. Synthesis of 2,7-dimethyl-10-oxa-1,8-diaza-anthracen-9-one and derivatives by Gotchev, Dimitar B., Comins, Daniel L.

“…Synthesis of novel heterocycles, which contain the unique 10-oxa-1,8-diazaanthracen-9-one tricyclic core, is reported. The core structure was assembled via a…”
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Spongipyran synthetic studies. Evolution of a scalable total synthesis of (+)-spongistatin 1: 2008 Tetrahedron Prize for Creativity in Organic Chemistry. The Art of Synthesis: Methods, Strategies and Applications by SMITH, Amos B, SFOUGGATAKIS, Chris, ATASOYLU, Onur, SHIRAKAMI, Shohei, BAUER, David, TAKEUCHI, Makoto, KOYANAGI, Jyunichi, SAKAMOTO, Yasuharu, RISATTI, Christina A, SPERRY, Jeffrey B, WENYU ZHU, DOUGHTY, Victoria A, TOMIOKA, Takashi, GOTCHEV, Dimitar B, BENNETT, Clay S, SAKAMOTO, Satoshi

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Alkaloid synthesis using N-acylpyridinium salts as building blocks: Progress towards the total synthesis of (-)-FR901483 and synthesis of novel polyheterocyclic compounds by Gotchev, Dimitar Borissov

“…A study directed toward the total synthesis of the potent immunosuppressant (−)FR901483 was examined. Three approaches to the tricyclic core of the targeted…”
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Alkaloid synthesis using N-acylpyridinium salts as building blocks: Progress towards the total synthesis of (−)-FR901483 and synthesis of novel polyheterocyclic compounds by Gotchev, Dimitar Borissov

“…A study directed toward the total synthesis of the potent immunosuppressant (−)FR901483 was examined. Three approaches to the tricyclic core of the targeted…”
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