Drug therapy is one of the important means to control hypertension, and the development of small molecular compounds is the core field of antihypertensive drug research.
Chloro-1,3-Dimethyluracil: Drug Design Targeting Adenosine Receptors
Adenosine receptor and hypertension
Adenosine receptors (A1R, A2AR, A2BR and A3R) are important G protein-coupled receptors, which play a key role in the relaxation of vascular smooth muscle, the regulation of heart rate and the sodium reabsorption of renal tubules. A2A receptor, in particular, participates in the regulation of blood pressure by mediating vasodilation.
Effect of 6-chloro -1,3- dimethyluracil
6-chloro-1,3-dimethyluracil is one of the leading compounds of adenosine receptor modulators. A series of adenosine receptor agonists or antagonists can be generated by introducing functional groups (such as aryl or thio) through nucleophilic substitution reaction, which can be used to regulate vascular tension and lower blood pressure.
6-Chloro-1,3-Dimethyluracil: Application of Derivatives in Calcium Channel Blockers
Hypotensive mechanism of calcium channel blockers.
Calcium channel blockers (such as nifedipine and amlodipine) reduce the calcium influx of vascular smooth muscle by blocking L-type calcium channels, thus causing vasodilation and lowering blood pressure.
Advantages of pyrimidine derivatives
6-chloro-1,3-dimethyluracil can be used to design drugs with selective calcium channel blocking effect by introducing specific functional groups. These drugs can not only effectively lower blood pressure, but also have low side effects.
6-Chloro-1,3-Dimethyluracil: Potential Application in Nitric Oxide Donor Drugs
Nitric oxide and lowering blood pressure
Nitric oxide (NO) is an important vascular relaxing factor secreted by endothelial cells. NO donor drugs can directly act on vascular smooth muscle and cause vasodilation by releasing NO.
Development of uracil derivatives
6-chloro-1,3-dimethyluracil reacts with nitro compounds to design derivatives with NO donor function. These derivatives show remarkable efficacy in antihypertensive drugs.
6-Chloro-1,3-Dimethyluracil: Precursor as Raas System Inhibitor
RAAS system and hypertension
Renin-angiotensin-aldosterone system (RAAS) is one of the important mechanisms of hypertension. By inhibiting angiotensin converting enzyme (ACE) or blocking angiotensin II receptor (AT1R), blood pressure can be effectively lowered.
Potential of 6-chloro -1,3- dimethyluracil
Pyrimidine derivatives are widely used in the development of ACE inhibitors or AT1R antagonists because they can target key enzymes or receptors in RAAS system. For example:
6-chloro-1,3-dimethyluracil was derivatized into carboxyl-containing molecules for the design of ACE inhibitors.
By introducing aromatic substituents, high-efficiency angiotensin receptor antagonists were developed.
6-Chloro-1,3-Dimethyluracil: A Precursor for the Development of Diuretics
Diuretics and lowering blood pressure
By inhibiting the reabsorption of sodium ions by renal tubules, diuretics can reduce blood volume, thus lowering blood pressure.
Application of 6-chloro -1,3- dimethyluracil
chloro-1,3-dimethyluracilcan be used as the precursor of pyrimidine diuretics (such as triamterene), and the selectivity and activity of drugs can be improved through molecular modification.
As a pharmaceutical intermediate, it has been used in the development of drugs with various antihypertensive mechanisms, including adenosine receptor modulators, calcium channel blockers, nitric oxide donor drugs and RAAS system inhibitors.