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Page 1
Design and synthesis of novel alpha(1)(a) adrenoceptor-selective antagonists. 1. Structure-activity relationship in dihydropyrimidinones.
Nagarathnam D, Miao SW, Lagu B, Chiu G, Fang J, Murali Dhar TG, Zhang J, Tyagarajan S, Marzabadi MR, Zhang F, Wong WC, Sun W, Tian D, Wetzel JM, Forray C, Chang RS, Broten TP, Ransom RW, Schorn TW, Chen TB, O'Malley S, Kling P, Schneck K, Bendesky R, Harrell CM, et al. Nagarathnam D, et al. Among authors: tyagarajan s. J Med Chem. 1999 Nov 18;42(23):4764-77. doi: 10.1021/jm990200p. J Med Chem. 1999. PMID: 10579840
Design and synthesis of novel alpha(1)(a) adrenoceptor-selective antagonists. 2. Approaches to eliminate opioid agonist metabolites via modification of linker and 4-methoxycarbonyl-4-phenylpiperidine moiety.
Murali Dhar TG, Nagarathnam D, Marzabadi MR, Lagu B, Wong WC, Chiu G, Tyagarajan S, Miao SW, Zhang F, Sun W, Tian D, Shen Q, Zhang J, Wetzel JM, Forray C, Chang RS, Broten TP, Schorn TW, Chen TB, O'Malley S, Ransom R, Schneck K, Bendesky R, Harrell CM, Vyas KP, et al. Murali Dhar TG, et al. Among authors: tyagarajan s. J Med Chem. 1999 Nov 18;42(23):4778-93. doi: 10.1021/jm990201h. J Med Chem. 1999. PMID: 10579841
In vitro studies on L-771,688 (SNAP 6383), a new potent and selective alpha1A-adrenoceptor antagonist.
Chang RS, Chen TB, O'Malley SS, Pettibone DJ, DiSalvo J, Francis B, Bock MG, Freidinger R, Nagarathnam D, Miao SW, Shen Q, Lagu B, Murali Dhar TG, Tyagarajan S, Marzabadi MR, Wong WC, Gluchowski C, Forray C. Chang RS, et al. Among authors: tyagarajan s. Eur J Pharmacol. 2000 Dec 15;409(3):301-12. doi: 10.1016/s0014-2999(00)00854-2. Eur J Pharmacol. 2000. PMID: 11108825
Invention of MK-8262, a Cholesteryl Ester Transfer Protein (CETP) Inhibitor Backup to Anacetrapib with Best-in-Class Properties.
Vachal P, Duffy JL, Campeau LC, Amin RP, Mitra K, Murphy BA, Shao PP, Sinclair PJ, Ye F, Katipally R, Lu Z, Ondeyka D, Chen YH, Zhao K, Sun W, Tyagarajan S, Bao J, Wang SP, Cote J, Lipardi C, Metzger D, Leung D, Hartmann G, Wollenberg GK, Liu J, Tan L, Xu Y, Chen Q, Liu G, Blaustein RO, Johns DG. Vachal P, et al. Among authors: tyagarajan s. J Med Chem. 2021 Sep 23;64(18):13215-13258. doi: 10.1021/acs.jmedchem.1c00959. Epub 2021 Aug 10. J Med Chem. 2021. PMID: 34375108
Rapid Affinity and Microsomal Stability Ranking of Crude Mixture Libraries of Histone Deacetylase Inhibitors.
Tyagarajan S, Andrews CL, Beshore DC, Buevich AV, Curran PJ, Dandliker P, Greshock TJ, Hoar J, Kim A, Karnachi P, Knemeyer I, Kozlowski J, Liu J, Maletic M, Myers R, Rada V, Sha D, Sauvagnat B, Vachal P, Wolkenberg S, Yu W, Yu Y, Krska SW. Tyagarajan S, et al. ACS Med Chem Lett. 2024 Sep 12;15(10):1787-1794. doi: 10.1021/acsmedchemlett.4c00345. eCollection 2024 Oct 10. ACS Med Chem Lett. 2024. PMID: 39411537
Nodulisporic acid side-chain modifications: access to the 2", 3", 4", and 6" registers.
Chakravarty PK, Shih TL, Colletti SL, Ayer MB, Snedden C, Kuo H, Tyagarajan S, Gregory L, Zakson-Aiken M, Shoop WL, Schmatz DM, Wyvratt M, Fisher MH, Meinke PT. Chakravarty PK, et al. Among authors: tyagarajan s. Bioorg Med Chem Lett. 2003 Jan 6;13(1):147-50. doi: 10.1016/s0960-894x(02)00826-0. Bioorg Med Chem Lett. 2003. PMID: 12467636
Discovery of a novel class of biphenyl pyrazole sodium channel blockers for treatment of neuropathic pain.
Tyagarajan S, Chakravarty PK, Zhou B, Taylor B, Eid R, Fisher MH, Parsons WH, Wyvratt MJ, Lyons KA, Klatt T, Li X, Kumar S, Williams B, Felix J, Priest BT, Brochu RM, Warren V, Smith M, Garcia M, Kaczorowski GJ, Martin WJ, Abbadie C, McGowan E, Jochnowitz N, Weber A, Duffy JL. Tyagarajan S, et al. Bioorg Med Chem Lett. 2010 Dec 15;20(24):7479-82. doi: 10.1016/j.bmcl.2010.10.017. Epub 2010 Oct 14. Bioorg Med Chem Lett. 2010. PMID: 21106456
Potent, non-covalent reversible BTK inhibitors with 8-amino-imidazo[1,5-a]pyrazine core featuring 3-position bicyclic ring substitutes.
Liu J, Guiadeen D, Krikorian A, Gao X, Wang J, Babu Boga S, Alhassan AB, Yu W, Selyutin O, Yu Y, Anand R, Xu J, Kelly J, Duffy JL, Liu S, Yang C, Wu H, Cai J, Bennett C, Maloney KM, Tyagarajan S, Gao YD, Fischmann TO, Presland J, Mansueto M, Xu Z, Leccese E, Zhang-Hoover J, Knemeyer I, Garlisi CG, Stivers P, Brandish PE, Hicks A, Kim R, Kozlowski JA. Liu J, et al. Among authors: tyagarajan s. Bioorg Med Chem Lett. 2020 Sep 1;30(17):127390. doi: 10.1016/j.bmcl.2020.127390. Epub 2020 Jul 11. Bioorg Med Chem Lett. 2020. PMID: 32738973
A potent and selective indole N-type calcium channel (Ca(v)2.2) blocker for the treatment of pain.
Tyagarajan S, Chakravarty PK, Park M, Zhou B, Herrington JB, Ratliff K, Bugianesi RM, Williams B, Haedo RJ, Swensen AM, Warren VA, Smith M, Garcia M, Kaczorowski GJ, McManus OB, Lyons KA, Li X, Madeira M, Karanam B, Green M, Forrest MJ, Abbadie C, McGowan E, Mistry S, Jochnowitz N, Duffy JL. Tyagarajan S, et al. Bioorg Med Chem Lett. 2011 Jan 15;21(2):869-73. doi: 10.1016/j.bmcl.2010.11.067. Epub 2010 Nov 21. Bioorg Med Chem Lett. 2011. PMID: 21195616
72 results