Kalsi R, Pande K, Bhalla T N, Barthwal J P, Gupta G P, Parmar S S
Jawaharlal Nehru Laboratory of Molecular Biology, Department of Pharmacology and Therapeutics, King George's Medical College, Lucknow, India.
J Pharm Sci. 1990 Apr;79(4):317-20. doi: 10.1002/jps.2600790409.
Eight substituted quinazolonoformazans were synthesized and evaluated for anti-inflammatory activity. The degree of protection provided by seven of these compounds, at a dose of 100 mg/kg, po, against carrageenin-induced edema in rat paw ranged from 26 to 57%. The four active substituted quinazolonoformazans (1, 2, 6, 8), on further evaluation for antiwrithmogenic activity, provided 10-80% protection against the aconitine-induced writhing response in mice. The ulcerogenic liabilities of two of the most active compounds were also determined. The doses producing ulcers in 50% of the treated rats (UD50) were 155 and 260 mg/kg, ip, for 2 and 8, respectively. The low toxicities possessed by these substituted quinazolonoformazans were indicated by their LD50 values which ranged from 600 to 1300 mg/kg, ip, in mice.
合成了8种取代喹唑啉并甲臜，并对其抗炎活性进行了评估。这些化合物中的7种，以100mg/kg的口服剂量，对大鼠足跖角叉菜胶诱导的水肿的保护程度在26%至57%之间。对4种活性取代喹唑啉并甲臜（1、2、6、8）进一步评估其抗扭体活性，对小鼠乌头碱诱导的扭体反应提供了10%-80%的保护。还测定了两种活性最高的化合物的致溃疡倾向。在50%的受试大鼠中产生溃疡的剂量（UD50），化合物2和8分别为155和260mg/kg，腹腔注射。这些取代喹唑啉并甲臜的低毒性通过其在小鼠中的LD50值表明，范围为600至1300mg/kg，腹腔注射。
