Synthesis, Polymorphism, and Insecticidal Activity of Methyl 4‐(4‐chlorophenyl)‐8‐iodo‐2‐methyl‐6‐oxo‐1,6‐dihydro‐4H‐pyrimido[2,1‐b]quinazoline‐3‐Carboxylate Against Anopheles arabiensis Mosquito

Abstract

Mosquitoes are the major vectors of pathogens and parasites including those causing malaria, the most deadly vector-borne disease. The negative environmental effects of most synthetic compounds combined with widespread development of insecticide resistance encourage an interest in finding and developing alternative products against mosquitoes. In this study, pyrimido[2,1-b]quinazoline derivative DHPM3 has been synthesized by three-step chemical reaction and screened for larvicide, adulticide, and repellent properties against Anopheles arabiensis, one of the dominant vectors of malaria in Africa. The title compound emerged as potential larvicide agent for further research and development, because it exerted 100% mortality, while adulticide activity was considered moderate.

Synthesis of Fused Indolo‐Pyrazoles and Their Antimicrobial and Insecticidal Activities against Anopheles arabiensis Mosquito

“…It is concluded that FIPs displayed a major feature of insect poisoning through paralysis to death. Furthermore, it showed insect immobilization that is comparable with drugs already reported such as halogenated coumarin [21], 2‐chloro‐ N ‐(benzothiazol‐2‐yl)acetamine, polymorphic form DHPM3b and DEET . Therefore, the FIPS merit further study of their repellent properties and molecular docking should be used to understand their mechanism of action.…”

Larvicidal study of tetrahydropyrimidine scaffolds against Anopheles arabiensis and structural insight by single crystal X‐ray studies

“…HPM molecules are generally synthesized by multicomponent reaction, which was discovered by Italian chemist Pietro Biginelli in 1893, known as Biginelli reaction, which is a simple combination of equal molar ratio of alkyl/aryl aldehyde, β‐keto ester, and urea or thiourea in the presence of acid as a catalyst in ethanol medium . Owing to hetero atom present on HPM scaffolds, these multicomponent products have shown various pharmacological properties such as antimicrobial, topoisomerase inhibitors, antimalarial, antitubercular, antimosquito, cardiovascular treatment as they act as potent calcium channel blockers, anti‐inflammatory, and pancreatic neuroendocrine neoplasm therapy . Copper complexes of HPM molecules are reported for the activity of human breast cancer cells .…”

“…Anopheles arabiensis belongs to the Anopheles gambiae species complex and is one of the most important vectors of malaria. HPM is a versatile pharmacophore that has exhibited larvicidal activity against Anopheles arabiensis , Aedesaegypti , and Culex quinquefasciatus . In view of such versatile pharmacological properties of HPM molecules and in continuation of our effort in search of novel heterocyclic larvicidal agents, a new series of methyl/ethyl 4‐(substitutedphenyl/pyridyl)‐6‐methyl‐2‐oxo/thioxo‐1,2,3,4‐tetrahydropyrimidine‐5‐carboxylate derivatives 4a–g have been designed in Scheme 1.…”

Synthesis, Spectroscopic Characterization, and Time‐Dependent DFT Calculations of 1‐Methyl‐5‐phenyl‐5H‐pyrido[1,2‐a]quinazoline‐3,6‐dione and Its Starting Precursor in Different Solvents

“…[3] Many of them showanalgesic, [4] antifungal, antibacterial, [5][6][7] anticancer, and anti-inflammatory activities. [8] As pesticides, they are used as insecticidal [9,10] and antiviral agents. [11] Earlier reports showed that the presence of alkyl/aryl/heteroaryl groups at the 2-and 3-positions of the quinazolinone ring was benefi-cial to anti-inflammatory and antimicrobial activity.I nt his regard, it was planned to synthesize some new derivatives of quinazolin-4-one.…”