药物结构的作用（The role of drug structure）.docVIP

药物结构的作用（The role of drug structure） The role of drug structure The difference in the chemical structure between a female and a male is that the male has 19 methyl, and the female does not The introduction of estradiol 17 alpha into acetylene group, the main consideration of its design is to prevent the 17 bit metabolism, can be taken orally Without structural modification, the direct drug steroid is progesterone In the structural modification of hydrocortisone, 1 - bit introduction of double bonds can enhance the anti-inflammatory effect Tamoxifen citrate cis isomers activity of estradiol is 3 with hydroxy steroid hormone In the synthesis of steroid drugs, the reaction of microorganism is often used, including the aromatization and dehydrogenation of A ring in the synthesis of estrone, and the 11 oxidation in the synthesis of prednisolone acetate 16 introduction the purpose of methyl glucocorticoid is 17 increase in side chain stability, reduce the effect of sodium retention, increased glucocorticoid activity from double to dilute synthetic route of progesterone, by oxidation, reduction and hydrolysis The chemical structure of estradiol is characterized by 13 bit methyl and A ring aromatization, and 17 beta -OH Improve the anti-inflammatory effect of adrenal cortical hormone can be used C-9, C-16 introduction of fluorine methyl C-6 introduction, introducing fluorine spironolactone and isoniazid in formic acid solution in the reaction of soluble yellow product, this is because the 3 generation of oxygen containing spironolactone quinolones structure-activity relationship: N-1 substituted hydrocarbyl if the fat body, to ethyl or ethyl vinyl, similar size fluoroethyl had the best antibacterial activity. The 3 carboxyl group and the 4 keto group are the parts of the drug that bind to the DNA gyro enzyme and produce an essential part of the drug effect. In the 5 substituent group, the substitution of amino group was the best, and the activity of other groups decreased. I