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Page 1
Lead Optimization to Advance Protease-Activated Receptor-1 Antagonists in Early Discovery.
Mandal M, Madeira M, Amin RP, Buevich AV, Cheng A, Labroli M, Liu X, Acton J, Pio B, Basso A, Chobanian H, Dong G, Dropinski J, Guo Y, Guo Z, Kurowski S, Korfmacher W, Lee S, Meng D, Ondeyka D, Yang Z, Zhang R, Wei H, Wu Z, Zhang F, Wollenberg G, Biftu T, Greenlee WJ, Chintala M, Maletic M, Zhu Z. Mandal M, et al. Among authors: madeira m. J Med Chem. 2022 Apr 14;65(7):5575-5592. doi: 10.1021/acs.jmedchem.1c02048. Epub 2022 Mar 29. J Med Chem. 2022. PMID: 35349275
Discovery of MK-7725, A Potent, Selective Bombesin Receptor Subtype-3 Agonist for the Treatment of Obesity.
Chobanian HR, Guo Y, Liu P, Chioda M, Lanza TJ Jr, Chang L, Kelly TM, Kan Y, Palyha O, Guan XM, Marsh DJ, Metzger JM, Gorski JN, Raustad K, Wang SP, Strack AM, Miller R, Pang J, Madeira M, Lyons K, Dragovic J, Reitman ML, Nargund RP, Lin LS. Chobanian HR, et al. Among authors: madeira m. ACS Med Chem Lett. 2012 Jan 21;3(3):252-6. doi: 10.1021/ml200304j. eCollection 2012 Mar 8. ACS Med Chem Lett. 2012. PMID: 24900461 Free PMC article.
Discovery of MK-3168: A PET Tracer for Imaging Brain Fatty Acid Amide Hydrolase.
Liu P, Hamill TG, Chioda M, Chobanian H, Fung S, Guo Y, Chang L, Bakshi R, Hong Q, Dellureficio J, Lin LS, Abbadie C, Alexander J, Jin H, Mandala S, Shiao LL, Li W, Sanabria S, Williams D, Zeng Z, Hajdu R, Jochnowitz N, Rosenbach M, Karanam B, Madeira M, Salituro G, Powell J, Xu L, Terebetski JL, Leone JF, Miller P, Cook J, Holahan M, Joshi A, O'Malley S, Purcell M, Posavec D, Chen TB, Riffel K, Williams M, Hargreaves R, Sullivan KA, Nargund RP, DeVita RJ. Liu P, et al. Among authors: madeira m. ACS Med Chem Lett. 2013 Apr 20;4(6):509-13. doi: 10.1021/ml4000996. eCollection 2013 Jun 13. ACS Med Chem Lett. 2013. PMID: 24900701 Free PMC article.
Discovery of MK-4409, a Novel Oxazole FAAH Inhibitor for the Treatment of Inflammatory and Neuropathic Pain.
Chobanian HR, Guo Y, Liu P, Chioda MD, Fung S, Lanza TJ, Chang L, Bakshi RK, Dellureficio JP, Hong Q, McLaughlin M, Belyk KM, Krska SW, Makarewicz AK, Martel EJ, Leone JF, Frey L, Karanam B, Madeira M, Alvaro R, Shuman J, Salituro G, Terebetski JL, Jochnowitz N, Mistry S, McGowan E, Hajdu R, Rosenbach M, Abbadie C, Alexander JP, Shiao LL, Sullivan KM, Nargund RP, Wyvratt MJ, Lin LS, DeVita RJ. Chobanian HR, et al. Among authors: madeira m. ACS Med Chem Lett. 2014 Apr 10;5(6):717-21. doi: 10.1021/ml5001239. eCollection 2014 Jun 12. ACS Med Chem Lett. 2014. PMID: 24944750 Free PMC article.
Improved Stability of Proline-Derived Direct Thrombin Inhibitors through Hydroxyl to Heterocycle Replacement.
Chobanian HR, Pio B, Guo Y, Shen H, Huffman MA, Madeira M, Salituro G, Terebetski JL, Ormes J, Jochnowitz N, Hoos L, Zhou Y, Lewis D, Hawes B, Mitnaul L, O'Neill K, Ellsworth K, Wang L, Biftu T, Duffy JL. Chobanian HR, et al. Among authors: madeira m. ACS Med Chem Lett. 2015 Mar 13;6(5):553-7. doi: 10.1021/acsmedchemlett.5b00047. eCollection 2015 May 14. ACS Med Chem Lett. 2015. PMID: 26005532 Free PMC article.
Discovery of Broad-Spectrum Herpes Antiviral Oxazolidinone Amide Derivatives and Their Structure-Activity Relationships.
Plotkin MA, Labroli M, Schubert J, Shaw A, Schlegel KS, Berger R, Cooke AJ, Hayes RP, Armacost KA, Kinek K, Krosky P, Burlein C, Meng S, DiNunzio E, Murray EM, Agrawal S, Madeira M, Flattery A, Yao H, Leithead A, Rose WA 2nd, Cox C, Tellers DM, McKenna PM, Raheem I. Plotkin MA, et al. Among authors: madeira m. ACS Med Chem Lett. 2024 Jul 9;15(8):1232-1241. doi: 10.1021/acsmedchemlett.4c00117. eCollection 2024 Aug 8. ACS Med Chem Lett. 2024. PMID: 39140041
Discovery of a Potent and Selective DGAT1 Inhibitor with a Piperidinyl-oxy-cyclohexanecarboxylic Acid Moiety.
He S, Hong Q, Lai Z, Yang DX, Ting PC, Kuethe JT, Cernak TA, Dykstra KD, Sperbeck DM, Wu Z, Yu Y, Yang GX, Jian T, Liu J, Guiadeen D, Krikorian AD, Sonatore LM, Wiltsie J, Liu J, Gorski JN, Chung CC, Gibson JT, Lisnock J, Xiao J, Wolff M, Tong SX, Madeira M, Karanam BV, Shen DM, Balkovec JM, Pinto S, Nargund RP, DeVita RJ. He S, et al. Among authors: madeira m. ACS Med Chem Lett. 2014 Sep 8;5(10):1082-7. doi: 10.1021/ml5003426. eCollection 2014 Oct 9. ACS Med Chem Lett. 2014. PMID: 25349648 Free PMC article.
Microscale High-Throughput Experimentation as an Enabling Technology in Drug Discovery: Application in the Discovery of (Piperidinyl)pyridinyl-1H-benzimidazole Diacylglycerol Acyltransferase 1 Inhibitors.
Cernak T, Gesmundo NJ, Dykstra K, Yu Y, Wu Z, Shi ZC, Vachal P, Sperbeck D, He S, Murphy BA, Sonatore L, Williams S, Madeira M, Verras A, Reiter M, Lee CH, Cuff J, Sherer EC, Kuethe J, Goble S, Perrotto N, Pinto S, Shen DM, Nargund R, Balkovec J, DeVita RJ, Dreher SD. Cernak T, et al. Among authors: madeira m. J Med Chem. 2017 May 11;60(9):3594-3605. doi: 10.1021/acs.jmedchem.6b01543. Epub 2017 Mar 2. J Med Chem. 2017. PMID: 28252959
Discovery of Chromane Propionic Acid Analogues as Selective Agonists of GPR120 with in Vivo Activity in Rodents.
Adams GL, Velazquez F, Jayne C, Shah U, Miao S, Ashley ER, Madeira M, Akiyama TE, Di Salvo J, Suzuki T, Wang N, Truong Q, Gilbert E, Zhou D, Verras A, Kirkland M, Pachanski M, Powles M, Yin W, Ujjainwalla F, Venkatraman S, Edmondson SD. Adams GL, et al. Among authors: madeira m. ACS Med Chem Lett. 2016 Dec 6;8(1):96-101. doi: 10.1021/acsmedchemlett.6b00394. eCollection 2017 Jan 12. ACS Med Chem Lett. 2016. PMID: 28105282 Free PMC article.
Accelerating the discovery of DGAT1 inhibitors through the application of parallel medicinal chemistry (PMC).
Yu Y, Wu Z, Shi ZC, He S, Lai Z, Cernak TA, Vachal P, Liu M, Liu J, Hong Q, Jian T, Guiadeen D, Krikorian A, Sperbeck DM, Verras A, Sonatore LM, Murphy BA, Wiltsie J, Chung CC, Gorski JN, Liu J, Xiao J, Wolff M, Tong SX, Madeira M, Karanam BV, Shen DM, Balkovec JM, De Vita RJ, Pinto S, Nargund RP. Yu Y, et al. Among authors: madeira m. Bioorg Med Chem Lett. 2019 Jun 1;29(11):1380-1385. doi: 10.1016/j.bmcl.2019.03.039. Epub 2019 Mar 27. Bioorg Med Chem Lett. 2019. PMID: 30952592
549 results