Synthesis and Docking Study of Pyrimidine Derivatives Scaffold for Anti‐Hypertension Application

Abstract

The present work introduces four new macromolecules pyrrolo[2,3‐d]pyrimidine scaffolds substituted with various benzene‐sulfonamide moieties; those were picked up via cyclization of 2‐amino‐3‐cyanopyrroles with phenyl isothiocyanate. The newly prepared pyrrolopyrimidine derivatives have been elucidated by spectroscopic techniques (FT‐IR, 1HNMR, 13CNMR and MS) and elemental analyses. The antihypertensive activity of the synthesized pyrrolopyrimidine derivatives based on sulfonamide moiety was evaluated. All pyrrolopyrimidine derivatives were showed a potent antihypertensive activity than Prazosin that utilized as standard drug. The structure activity relationship (SAR) was studied to correlate the influence of sulfonamide group with the aminopyrimidine moiety. Molecular docking for the synthesized derivatives and theoretical statistics were carried out to expect their antihypertensive efficacy.

Synthesis, Docking and Antihypertensive Activity of Pyridone Derivatives

“…Furthermore, from the previous literature, the SO 2 bridge in the sulfonamide moiety played a vital role in α1 A receptor blocking activity. [27] Finally, the synthesized analogues have a mutual framework in their structures; the noticed structural activity relationship is principally owing to the dissimilarity of other functionalities on this scaffold. While the difference in the structures on the chief scaffold at C3 is liable for dissimilarity in effectiveness potential while all structures are captivating portion in the action.…”

Synthesis of novel calcium channel blockers with ACE2 inhibition and dual antihypertensive/anti-inflammatory effects: A possible therapeutic tool for COVID-19

“…Pyrimidines and DHPMs, the important lead compounds for treatment of hypertension [32] , have been developed as for SQ 32926, SQ 32,547 and some pyrimidines analogues ( Fig. 2 & Fig.…”

Pyrimidine: An elite heterocyclic leitmotif in drug discovery‐synthesis and biological activity

“…9 | ANTIHYPERTENSIVE ACTIVITY Katouah and Gaffer synthesized four pyrrolo [2,pyrimidine analogues (Scheme 30) possessing benzene sulfonamide component. 61d exhibited a potent activity by effectively decreasing the mean systolic blood pressure (SBP) of hypertensive rats using prazosin as the reference standard (Katouah & Gaffer, 2019).…”