Details

Autor(en) / Beteiligte

• Ismail, Magda M. F.
• El-Sayed, Nehad A. M.
• Rateb, Heba S.
• Ammar, Yousry A.

Titel

New Hybrids of Sulfonamide/Thiourea: Synthesis, In Silico Study and Antihypertensive Evaluation

Ist Teil von

• Polycyclic aromatic compounds, 2022-07, Vol.42 (6), p.3768-3779

Ort / Verlag

Philadelphia: Taylor & Francis

Erscheinungsjahr

2022

Quelle

Taylor & Francis

Beschreibungen/Notizen

• This study describes design and synthesis of new hybrids of N-substituted-N'-(4-(piperidin-1-yl-sulfonyl)phenylthiourea and condensed thiourea derivatives (monocyclic, bicyclic, and tricyclic) via a facile synthetic route. In silico study is performed showing that all hits are bioavailable and comply with Lipiniski rule of five with no side effects. Representative hybrids, 2, 3b, 3c, 6, and 10 were selected for in vivo antihypertensive evaluation using Nifedipine as a reference standard. The target compound, 3c, can be considered comparative/more potent than the reference standard (Nifedipine). Besides, compounds 2, 3b, 6, and 10 showed significant antihypertensive activity. The structures of these derivatives were ascertained using various spectroscopic and analytic techniques.