Hexahydroquinoline Featuring Amide Functionality: A Promising Scaffold With Calcium Channel Blocking Activity
 
Yazarlar (14)
Arş. Gör. Ebru Koçak Aslan Hacettepe Üniversitesi, Türkiye
Kevin Lam Freie Universität Berlin, Almanya
Sun Huang Alberta Children’S Hospital Research Institute, Kanada
Doç. Dr. Göknil Pelin Coşkun Acıbadem Mehmet Ali Aydınlar Üniversitesi, Türkiye
Arş. Gör. Ayşe Karagüzel Hacettepe Üniversitesi, Türkiye
Katrin Denzinger Freie Universität Berlin, Almanya
Kaan Birgül
Bahçeşehir Üniversitesi, Türkiye
Prof. Dr. Mert Ülgen Acıbadem Mehmet Ali Aydınlar Üniversitesi, Türkiye
Jordan W. Nafie
Biotools, Inc., Amerika Birleşik Devletleri
Prof. Dr. Onur ŞAHİN Sinop Üniversitesi, Türkiye
Daniel W. Armstrong
The University Of Texas At Arlington, Amerika Birleşik Devletleri
Gerald W. Zamponi Alberta Children’S Hospital Research Institute, Kanada
Gerhard Wolber Freie Universität Berlin, Almanya
Prof. Dr. Miyase Gözde Gündüz Hacettepe Üniversitesi, Türkiye
Makale Türü Açık Erişim Özgün Makale (SSCI, AHCI, SCI, SCI-Exp dergilerinde yayınlanan tam makale)
Dergi Adı Drug Development Research (Q1)
Dergi ISSN 0272-4391 Dergi Bilgileri (2026)
Dergi Tarandığı Indeksler SCI-Expanded
Makale Dili İngilizce Basım Tarihi 01-2026
Cilt / Sayı / Sayfa 87 / 2 / 70261– DOI 10.1002/ddr.70261
UAK Araştırma Alanları
Yoğun Madde Fiziği
Özet
Hexahydroquinoline (HHQ) is a widely recognized scaffold that has garnered considerable attention owing to its diverse pharmacological properties. The structure of HHQ includes a 1,4‐dihydropyridine (DHP) ring, which serves as the pharmacophore for the predominant class of drugs known as calcium channel blockers. DHPs are frequently utilized in the management of cardiovascular diseases and also show potential for pain management. Since all DHPs on the market possess ester functionality, we aimed to employ bioisosteric replacement to observe if their amide‐containing counterparts would still block calcium channels. Therefore, we synthesized new HHQs with ester or amide functionality (EM1‐EM15) and investigated their effects on L‐(Cav1.2) and T‐(Cav3.2)‐type calcium channels using the whole‐cell patch clamp technique. Although the amide derivatives were somewhat less effective than their …
Anahtar Kelimeler
"dihydropyridine" | "enantioseparation" | "Hantzsch synthesis" | "metabolic stability" | "molecular modeling" | "patch clamp"