111556-82-2Relevant academic research and scientific papers
Microwave Oriented Solid Support Synthesis of Novel 5,6-Disubstituted-1,2,4-Triazolopyrimidines as Antifungal Agents
Bala, Anju,Gumber, Khushbu,Sidhu, Anjali,Sidhu, Navjot Kaur
, p. 39 - 46 (2021/06/12)
Microwave oriented, basic solid support assisted, two-step reaction of aryl aldehyde, active methylene compounds, and 3-amino-1,2,4-triazole yielded 5,6-disubstituted-1,2,4-triazolopyrimidines in excellent yield without side products, in short reaction time. The preliminary in vitro antifungal evaluation of the compounds indicated the promising antifungal potential of the synthesized compounds against most of the test fungi using standard fungicides as a positive control. The in silico analysis of the synthesized molecules favors the results of in vitro analysis.
Design and synthesis of orally bioavailable 4-methyl heteroaryldihydropyrimidine based hepatitis B virus (HBV) capsid inhibitors
Qiu, Zongxing,Lin, Xianfeng,Zhou, Mingwei,Liu, Yongfu,Zhu, Wei,Chen, Wenming,Zhang, Weixing,Guo, Lei,Liu, Haixia,Wu, Guolong,Huang, Mengwei,Jiang, Min,Xu, Zhiheng,Zhou, Zheng,Qin, Ning,Ren, Shuang,Qiu, Hongxia,Zhong, Sheng,Zhang, Yuxia,Zhang, Yi,Wu, Xiaoyue,Shi, Liping,Shen, Fang,Mao, Yi,Zhou, Xue,Yang, Wengang,Wu, Jim Z.,Yang, Guang,Mayweg, Alexander V.,Shen, Hong C.,Tang, Guozhi
, p. 7651 - 7666 (2016/09/04)
Targeting the capsid protein of hepatitis B virus (HBV) and thus interrupting normal capsid formation have been an attractive approach to block the replication of HBV viruses. We carried out multidimensional structural optimizations based on the heteroaryldihydropyrimidine (HAP) analogue Bay41-4109 (1) and identified a novel series of HBV capsid inhibitors that demonstrated promising cellular selectivity indexes, metabolic stabilities, and in vitro safety profiles. Herein we disclose the design, synthesis, structureactivity relationship (SAR), cocrystal structure in complex with HBV capsid proteins and in vivo pharmacological study of the 4-methyl HAP analogues. In particular, the (2S,4S)-4,4-difluoroproline substituted analogue 34a demonstrated high oral bioavailability and liver exposure and achieved over 2 log viral load reduction in a hydrodynamic injected (HDI) HBV mouse model.
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 (2007/10/03)
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
Crystal Structures and Pharmacologic Activities of 1,4-Dihydropyridine Calcium Channel Antagonists of the Isobutyl Methyl 2,6-Dimethyl-4-(substituted phenyl)-1,4-dihydropyridine-3,5-dicarboxylate (Nisoldipine) Series
Fossheim, R.,Joslyn, A.,Solo, A. J.,Luchowski, E.,Rutledge, A.,Triggle, D. J.
, p. 301 - 305 (2007/10/02)
A series of isobutyl methyl 2,6-dimethyl-4-(X-substituted phenyl)-1,4-dihydropyridine-3,5-dicarboxylates (X= H, 2-NO2, 3-NO2, 3-CN, 3-MeO, 4-F, 2-CF3, 3-CF3, and 4-Cl) related to and including nisoldipine (X= 2-NO2) has been synthesized, their solid-state
