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HTN (ARBS (Losartan, (Its Metabolite is 40times more active), Candesertan…
HTN
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SYMPATHOLYTICS
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a & BB
Labetalol
2 Chiral Center R(OH),R(CH3) is the active β – blocker
the R(OH),S(CH3) a1 blocker. The S,R & S,S are Inactive
Carvedilol
1-Chiral center: Its S(-) enantiomer is both an a1 and nonselective β -blocker, whereas its R( +) enantiomer is an a1- blocker.
CCB
1,4-DIHYDROPYRIDINES
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SAR -> pyridine instead of benzene= Toxic Non Planer cycle is Inactive the benzene subs must be on M or O position e state doesn't matter ( para or Non subs benzene= inactive) This perpendicular conformation is essential for the activity in Pyridine ring the position 3&5 is E.W= CC Opener Chirality is better for activity due to stereo-selectivity
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