Quinazolinones, 13.Comm. Synthesis of 3‐[2‐(2,3‐Dihydro‐5‐phenyl‐4‐substituted‐3H‐1,2,4‐triazole‐3‐thione‐2‐yl)‐acetylamino]‐2‐methyl‐4(3H)‐quinazolinones and their pharmacological activities

Abstract

Some 2-methyl-3-triazole-substituted-4(3H)-quinazolinones 3a-f were prepared and tested for their H1- and H2-antihistaminic activities. In addition these compounds are central nervous system depressants and anticonvulsants. 3e shows highly significant decrease of locomotor activity.

Synthesis of 1-Substituted-4-(Pyridin-4-yl) [1,2,4] Triazolo [4,3-a] Quinazolin-5(4H)-ones as a New Class of H1- Antihistaminic Agents

“…loratadine, azelastine and flazelastine] that does not possess the above mentioned pharmacophore for H 1 -antihistamines gave way for the discovery of many novel antihistamines temelastine and mangostin [6,7]. Quinazolinones are associated with a wide range of biological and pharmacological activities such as analgesic [8], anti-inflammatory [9], antifungal [10,11], antiviral [12] and antihistaminic activities [13,14].…”

Quinazolinone Analogs as Potential Therapeutic Agents

“…loratadine, azelastine and flazelastine) that do not possess the above mentioned pharmacophore for H 1 -antihistamines, gave way for the discovery of many novel antihistamines such as temelastine and mangostin [150]. Literature provides a variety of reports on excellent antihistaminic activity in quinazolines [151][152].…”

Synthesis of 2,3-Disubstituted Quinazolinone Derivatives Using Silver Triflate as a Efficient Catalyst at Room Temperature

“…Literature survey revealed the versatile biological activities of quinazolinone derivatives (Büyüktimkin, 1985;Büyüktimkin et al, 1989). It has been established that quinazolinones possess antiviral (Mukherji et al, 1980), antifungal (Peet et al, 1986), antiallergic (Chaurasia, Sharma, 1982), antitumor (Li et al, 2012), antidiabetic activities (Chiou et al, 1996), coronary vasodilatory (Nagase et al, 2008, histamine receptor type-3 inverse agonism (Pandey, Lohani, 1979), anti cancer (Murugan et al, 2003;Shankar et al, 1984), anti-inflammatory (Shankar et al, 1985Abdel-Aim's et al, 1994;Mohd, Shalini, 1998;Saravanan et al, 1998;Bhat et al, 2000) antituberculosis (Kumar et al, 1970), CNS depressant activity (Tiwari, Pandey, 1975), anti-parkinsonism (Tiwardi, Rastogi, 1978Srivastava et al, 1986) and bronchodilator activity (Rao, Bahekar, 1999).…”