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Synthesis and Characterization of 3β -Substituted Amides of 17a-Aza-Dhomo- 4-androsten-17-one as Potent 5 α-Reductase Inhibitors and Antimicrobial Agents

[ Vol. 13 , Issue. 16 ]

Author(s):

Manav Malhotra, Rajiv Sharma, Ravindra K. Rawal, Hemraj Heer and T. R. Bhardwaj   Pages 2047 - 2061 ( 15 )

Abstract:


We herein report the synthesis of 3 β-substituted amides of 17a-aza-D-homo-4-androsten-17-one (11a-11r) from commercially available Diosgenin as the starting material. The structures of newly synthesized compounds were confirmed by IR, 1H NMR, 13C NMR and mass spectrometry. All the synthesized analogues were tested for their 5 α- reductase inhibitory and antimicrobial activity, some of them exhibit moderate to potent activity comparable to the reference drugs. Among the synthesized derivatives the analogue (11r) 3 β-(indonlylbutanamido)-17a-aza-D-homo-4- androsten-17-one was found to be active against both 5 -reductase enzyme and microbial strains, whereas the analogue (11i) 3β -(3,4-dimethoxy-benzamido)-17a-aza-D-homo-4-androsten-17-one was found to be the least active. The detailed 5 -reductase inhibitors and antimicrobial activities of the synthesized compounds were reported.

Keywords:

5 α-Reductase, Antibacterial, Antifungal, Dutasteride, Ciprofloxacin, Voriconazole.

Affiliation:

Department of Pharmaceutical Chemistry, Indo-Soviet Friendship (ISF) College of Pharmacy, Ferozepur Road, Moga-142 001, India.



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