Benzamide derivatives and their constrained analogs as histamine Hb>3 b> receptor antagonists
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- 作者：Ramakrishna Nirogi ; nvsrk@suven.com" class="auth_mail" title="E-mail the corresponding author ; Anil Shinde ; Vinaykumar Tiriveedhi ; Laxman Kota ; Sangram Keshari Saraf ; Rajesh Kumar Badange ; Abdul Rasheed Mohammed ; Ramkumar Subramanian ; Nageshwararao Muddana ; Gopinadh Bhyrapuneni ; Renny Abraham
- 关键词：Histamine H3 receptor ; SAR ; Pharmacokinetic profile ; Receptor occupancy
- 刊名：European Journal of Medicinal Chemistry
- 出版年：2016
- 出版时间：27 January 2016
- 年：2016
- 卷：108
- 期：Complete
- 页码：655-662
- 全文大小：610 K
文摘
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About twenty novel Benzamide derivatives were synthesized and evaluated for their affinity at H
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Most of the compounds showed good in vitro potency.
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Selected compounds showed acceptable ADME properties.
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Compound ass="boldFont">3d showed good exposures, adequate brain penetration and target engagement.
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Compound ass="boldFont">3d showed minimal hERG liability and reduced drug–drug interaction potential.