107634-95-7Relevant academic research and scientific papers
Design and synthesis of novel α(1a) adrenoceptor-selective antagonists. 1. Structure-activity relationship in dihydropyrimidinones
Nagarathnam, Dhanapalan,Miao, Shou Wu,Lagu, Bharat,Chiu, George,Fang, James,Dhar, T. G. Murali,Zhang, Jack,Tyagarajan, Sriram,Marzabadi, Mohammad R.,Zhang, Fengqi,Wong, Wai C.,Sun, Wanying,Tian, Dake,Wetzel, John M.,Forray, Carlos,Chang, Raymond S. L.,Broten, Theodore P.,Ransom, Richard W.,Schorn, Terry W.,Chen, Tsing B.,O'Malley, Stacey,Kling, Paul,Schneck, Kathryn,Bendesky, Robert,Harrell, Charles M.,Vyas, Kamlesh P.,Gluchowski, Charles
, p. 4764 - 4777 (1999)
Dihydropyrimidinones such as compound 12 exhibited high binding affinity and subtype selectivity for the cloned human α(1a) receptor. Systematic modifications of 12 led to identification of highly potent and subtype- selective compounds such as (+)-30 and
5,6,7,8-Tetrahydro-1,6-naphthyridine Derivatives as Potent HIV-1-Integrase-Allosteric-Site Inhibitors
Peese, Kevin M.,Allard, Christopher W.,Connolly, Timothy,Johnson, Barry L.,Li, Chen,Patel, Manoj,Sorensen, Margaret E.,Walker, Michael A.,Meanwell, Nicholas A.,McAuliffe, Brian,Minassian, Beatrice,Krystal, Mark,Parker, Dawn D.,Lewis, Hal A.,Kish, Kevin,Zhang, Ping,Nolte, Robert T.,Simmermacher, Jean,Jenkins, Susan,Cianci, Christopher,Naidu, B. Narasimhulu
supporting information, p. 1348 - 1361 (2019/02/24)
A series of 5,6,7,8-tetrahydro-1,6-naphthyridine derivatives targeting the allosteric lens-epithelium-derived-growth-factor-p75 (LEDGF/p75)-binding site on HIV-1 integrase, an attractive target for antiviral chemotherapy, was prepared and screened for activity against HIV-1 infection in cell culture. Small molecules that bind within the LEDGF/p75-binding site promote aberrant multimerization of the integrase enzyme and are of significant interest as HIV-1-replication inhibitors. Structure-activity-relationship studies and rat pharmacokinetic studies of lead compounds are presented.
