Search Results - "Mandal, Mihirbaran"

Design and Validation of Bicyclic Iminopyrimidinones As Beta Amyloid Cleaving Enzyme‑1 (BACE1) Inhibitors: Conformational Constraint to Favor a Bioactive Conformation by Mandal, Mihirbaran, Zhu, Zhaoning, Cumming, Jared N, Liu, Xiaoxiang, Strickland, Corey, Mazzola, Robert D, Caldwell, John P, Leach, Prescott, Grzelak, Michael, Hyde, Lynn, Zhang, Qi, Terracina, Giuseppe, Zhang, Lili, Chen, Xia, Kuvelkar, Reshma, Kennedy, Matthew E, Favreau, Leonard, Cox, Kathleen, Orth, Peter, Buevich, Alexei, Voigt, Johannes, Wang, Hongwu, Kazakevich, Irina, McKittrick, Brian A, Greenlee, William, Parker, Eric M, Stamford, Andrew W

“…On the basis of our observation that the biaryl substituent of iminopyrimidinone 7 must be in a pseudoaxial conformation to occupy the contiguous S1–S3…”
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In Pursuit of Carbohydrate-Based HIV Vaccines, Part 2: The Total Synthesis of High-Mannose-Type gp120 Fragments-Evaluation of Strategies Directed to Maximal Convergence by Geng, Xudong, Dudkin, Vadim Y., Mandal, Mihirbaran, Danishefsky, Samuel J.

“…A “layered approach” and a “block approach” were used to assemble the high‐mannose glycan of gp120 glycopeptide fragments (e.g. high‐mannose‐type conjugates…”
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Stereoselective Nucleophilic Trifluoromethylation of N-(tert-Butylsulfinyl)imines by Using Trimethyl(trifluoromethyl)silane by Prakash, G. K. Surya, Mandal, Mihirbaran, Olah, George A.

“…A very general reaction is presented to achieve the nucleophilic transfer of “CF3” to chiral N‐(tert‐butylsulfinyl)imines in high yield and high…”
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In Pursuit of Carbohydrate-Based HIV Vaccines, Part 1: The Total Synthesis of Hybrid-Type gp120 Fragments by Mandal, Mihirbaran, Dudkin, Vadim Y., Geng, Xudong, Danishefsky, Samuel J.

“…Key features in the successful synthesis of hybrid‐type gp‐120 fragments (see picture) include β‐mannosylations to construct the core trisaccharide and a…”
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Facile Synthesis of TMS-Protected Trifluoromethylated Alcohols Using Trifluoromethyltrimethylsilane (TMSCF3) and Various Nucleophilic Catalysts in DMF by Prakash, G. K. Surya, Panja, Chiradeep, Vaghoo, Habiba, Surampudi, Vijayalakshmi, Kultyshev, Roman, Mandal, Mihirbaran, Rasul, Golam, Mathew, Thomas, Olah, George A

“…Organofluorine compounds are becoming increasingly important in different fields, such as material science, agro chemistry, and the pharmaceutical industry…”
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Total Synthesis of Guanacastepene A: A Route to Enantiomeric Control by Mandal, Mihirbaran, Yun, Heedong, Dudley, Gregory B, Lin, Songnian, Tan, Derek S, Danishefsky, Samuel J

“…The goal of the total synthesis of guanacastepene A served as a focus to bring together several chemical inquiries. One involved the synthesis of fused…”
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Preparation of TMS protected trifluoromethylated alcohols using trimethylamine N-oxide and trifluoromethyltrimethylsilane (TMSCF3) by Prakash, G.K.Surya, Mandal, Mihirbaran, Panja, Chiradeep, Mathew, Thomas, Olah, George A.

“…Graphic A catalytic trifluoromethylation of aldehydes using trimethylamine N-oxide and trifluoromethyltrimethylsilane (TMSCF3) is described. Aromatic,…”
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Aroylation of aromatics with aryl carboxylic acids over Nafion-H (polymeric perfluoroalkanesulfonic acid), an environmentally friendly solid acid catalyst by Prakash, G. K. Surya, Mathew, Thomas, Mandal, Mihirbaran, Farnia, Morteza, Olah, George A.

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Generation of Leads for γ‑Secretase Modulation by Mandal, Mihirbaran, Buevich, Alexei, Caldwell, John P, Hyde, Lynn, Huang, Xianhai, Liu, Xiaoxiang, McKittrick, Brian, Mazzola, Robert D, Pissarnitski, Dmitri, Palani, Anandan, Zhang, Lili, Parker, Eric, Xiao, Li, Rindgen, Diane, Zhu, Zhaoning

“…Herein, we disclose three structurally differentiated γ-secretase modulators (GSMs) based on an oxadiazine scaffold. The analogues from series I potently…”
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Unprecedented Reversal of Regioselectivity during Methanolysis and an Interception of Curtius Rearrangement by Mandal, Mihirbaran, Buevich, Alexei V., Wang, Hongwu, Brunskill, Andrew, Orth, Peter, Caldwell, John P., Liu, Xiaoxiang, Mazzola, Robert, Cumming, Jared, McKittrick, Brian, Zhu, Zhaoning, Stamford, Andrew

“…Unprecedented reversal in regioselectivity during methanolysis of anhydrides due to the change in substitution pattern of fluorine in the phenyl moiety, and…”
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Rapid Evolution of a Fragment-like Molecule to Pan-Metallo-Beta-Lactamase Inhibitors: Initial Leads toward Clinical Candidates by Mandal, Mihirbaran, Xiao, Li, Pan, Weidong, Scapin, Giovanna, Li, Guoqing, Tang, Haiqun, Yang, Shu-Wei, Pan, Jianping, Root, Yuriko, de Jesus, Reynalda Keh, Yang, Christine, Prosise, Winnie, Dayananth, Priya, Mirza, Asra, Therien, Alex G., Young, Katherine, Flattery, Amy, Garlisi, Charles, Zhang, Rumin, Chu, Donald, Sheth, Payal, Chu, Inhou, Wu, Jin, Markgraf, Carrie, Kim, Hai-Young, Painter, Ronald, Mayhood, Todd W., DiNunzio, Edward, Wyss, Daniel F., Buevich, Alexei V., Fischmann, Thierry, Pasternak, Alexander, Dong, Shuzhi, Hicks, Jacqueline D., Villafania, Artjohn, Liang, Lianzhu, Murgolo, Nicholas, Black, Todd, Hagmann, William K., Tata, Jim, Parmee, Emma R., Weber, Ann E., Su, Jing, Tang, Haifeng

“…With the emergence and rapid spreading of NDM-1 and existence of clinically relevant VIM-1 and IMP-1, discovery of pan inhibitors targeting…”
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Structure Guided Discovery of Novel Pan Metallo-β-Lactamase Inhibitors with Improved Gram-Negative Bacterial Cell Penetration by Dong, Shuzhi, Zhao, Zhiqiang, Tang, Haiqun, Li, Guoqing, Pan, Jianping, Gu, Xin, Jiang, Jinlong, Xiao, Li, Scapin, Giovanna, Hunter, David N., Yang, Dexi, Huang, Yuhua, Bennett, Frank, Yang, Shu-Wei, Mandal, Mihirbaran, Tang, Haifeng, Su, Jing, Tudge, Clare, deJesus, Reynalda Keh, Ding, Fa-Xiang, Lombardo, Matthew, Hicks, Jacqueline D., Fischmann, Thierry, Mirza, Asra, Dayananth, Priya, Painter, Ronald E., Villafania, Artjohn, Garlisi, Charles G., Zhang, Rumin, Mayhood, Todd W., Si, Qian, Li, Nianyu, Amin, Rupesh P., Bhatt, Bhavana, Chen, Feifei, Regan, Christopher P., Regan, Hillary, Lin, Xinjie, Wu, Jin, Leithead, Andrew, Pollack, Scott R., Scott, Jack D., Nargund, Ravi P., Therien, Alex G., Black, Todd, Young, Katherine, Pasternak, Alexander

“…The use of β-lactam (BL) and β-lactamase inhibitor combination to overcome BL antibiotic resistance has been validated through clinically approved drug…”
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Lead Optimization to Advance Protease-Activated Receptor‑1 Antagonists in Early Discovery by Mandal, Mihirbaran, Madeira, Maria, Amin, Rupesh P, Buevich, Alexei V, Cheng, Alan, Labroli, Marc, Liu, Xiaoxiang, Acton, John, Pio, Barbara, Basso, Andrea, Chobanian, Harry, Dong, Grace, Dropinski, Jamie, Guo, Yan, Guo, Zhuyan, Kurowski, Stan, Korfmacher, Walter, Lee, Sandra, Meng, Dongfang, Ondeyka, Debra, Yang, Zhiqiang, Zhang, Rumin, Wei, Huijun, Wu, Zhicai, Zhang, Fengqi, Wollenberg, Gordon, Biftu, Tesfaye, Greenlee, William J, Chintala, Madhu, Maletic, Milana, Zhu, Zhaoning

“…Vorapaxar is an approved drug for the reduction of thrombotic cardiovascular events in patients with a history of myocardial infarction or with peripheral…”
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Structure-Based Design of an Iminoheterocyclic β‑Site Amyloid Precursor Protein Cleaving Enzyme (BACE) Inhibitor that Lowers Central Aβ in Nonhuman Primates by Mandal, Mihirbaran, Wu, Yusheng, Misiaszek, Jeffrey, Li, Guoqing, Buevich, Alexei, Caldwell, John P, Liu, Xiaoxiang, Mazzola, Robert D, Orth, Peter, Strickland, Corey, Voigt, Johannes, Wang, Hongwu, Zhu, Zhaoning, Chen, Xia, Grzelak, Michael, Hyde, Lynn A, Kuvelkar, Reshma, Leach, Prescott T, Terracina, Giuseppe, Zhang, Lili, Zhang, Qi, Michener, Maria S, Smith, Brad, Cox, Kathleen, Grotz, Diane, Favreau, Leonard, Mitra, Kaushik, Kazakevich, Irina, McKittrick, Brian A, Greenlee, William, Kennedy, Matthew E, Parker, Eric M, Cumming, Jared N, Stamford, Andrew W

“…We describe successful efforts to optimize the in vivo profile and address off-target liabilities of a series of BACE1 inhibitors represented by 6 that…”
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In Pursuit of Carbohydrate-Based HIV Vaccines, Part 1: The Total Synthesis of Hybrid-Type gp120 Fragments by Mandal, Mihirbaran, Dudkin, Vadim Y., Geng, Xudong, Danishefsky, Samuel J.

“…Schlüsselschritte in der erfolgreichen Synthese von hybriden gp120‐Fragmenten (siehe Bild) umfassen β‐Mannosylierungen zum Aufbau des Trisaccharidkerns und…”
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Overcoming Time-Dependent Inhibition (TDI) of Cytochrome P450 3A4 (CYP3A4) Resulting from Bioactivation of a Fluoropyrimidine Moiety by Mandal, Mihirbaran, Mitra, Kaushik, Grotz, Diane, Lin, Xinjie, Palamanda, Jairam, Kumari, Pramila, Buevich, Alexei, Caldwell, John P, Chen, Xia, Cox, Kathleen, Favreau, Leonard, Hyde, Lynn, Kennedy, Matthew E, Kuvelkar, Reshma, Liu, Xiaoxiang, Mazzola, Robert D, Parker, Eric, Rindgen, Diane, Sherer, Edward, Wang, Hongwu, Zhu, Zhaoning, Stamford, Andrew W, Cumming, Jared N

“…Herein we describe structure–activity relationship (SAR) and metabolite identification (Met-ID) studies that provided insight into the origin of time-dependent…”
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Nucleophilic trifluoromethylation tamed by Prakash, G.K.Surya, Mandal, Mihirbaran

“…The paper reviews our recent findings on the trifluoromethylation of organic compounds using TMSCF 3. Direct preparation of trifluoromethylated ketones from…”
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Diverted Total Synthesis Leads to the Generation of Promising Cell-Migration Inhibitors for Treatment of Tumor Metastasis: In vivo and Mechanistic Studies on the Migrastatin Core Ether Analog by Oskarsson, Thordur, Nagorny, Pavel, Krauss, Isaac J, Perez, Lucy, Mandal, Mihirbaran, Yang, Guangli, Ouerfelli, Ouathek, Xiao, Danhua, Moore, Malcolm A. S, Massagué, Joan, Danishefsky, Samuel J

“…A significantly simpler analog of the natural product migrastatin, termed migrastatin ether (ME), has been prepared and evaluated. Both in vivo and in vitro…”
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Can We Make Small Molecules Lean? Optimization of a Highly Lipophilic TarO Inhibitor by Mandal, Mihirbaran, Tan, Zheng, Madsen-Duggan, Christina, Buevich, Alexei V, Caldwell, John P, Dejesus, Reynalda, Flattery, Amy, Garlisi, Charles G, Gill, Charles, Ha, Sookhee Nicole, Ho, Ginny, Koseoglu, Sandra, Labroli, Marc, Basu, Kallol, Lee, Sang Ho, Liang, Lianzhu, Liu, Jenny, Mayhood, Todd, McGuinness, Debra, McLaren, David G, Wen, Xiujuan, Parmee, Emma, Rindgen, Diane, Roemer, Terry, Sheth, Payal, Tawa, Paul, Tata, James, Yang, Christine, Yang, Shu-Wei, Xiao, Li, Wang, Hao, Tan, Christopher, Tang, Haifeng, Walsh, Paul, Walsh, Erika, Wu, Jin, Su, Jing

“…We describe our optimization efforts to improve the physicochemical properties, solubility, and off-target profile of 1, an inhibitor of TarO, an early stage…”
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Stereoselective Synthesis of Trifluoromethylated Vicinal Ethylenediamines with α-Amino N-tert-Butanesulfinimines and TMSCF3 by Prakash, G. K. Surya, Mandal, Mihirbaran

“…Isolable α-amino N-tert-butanesulfinimines were prepared through the condensation of Reetz's α-amino aldehydes (prepared from α-amino acids) with Ellman's…”
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