title: Synthesis and evaluation of novel triazoles and mannich bases functionalized 1,4-dihydropyridine as angiotensin converting enzyme (ACE) inhibitors.
abstract: A series of novel diethyl 2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate embedded triazole and mannich bases were synthesized, and evaluated for their angiotensin converting enzyme (ACE) inhibitory activity. Screening of above synthesized compounds for ACE inhibition showed that triazoles functionalized compounds have better ACE inhibitory activity compared to that of mannich bases analogues. Among all triazoles we found 6 h, 6 i and 6 j to have good ACE inhibition activity with IC50 values 0.713 μM, 0.409 μM and 0.653 μM, respectively. Among mannich bases series compounds, only 7c resulted as most active ACE inhibitor with IC50 value of 0.928 μM.
authors.affiliation: Fluoroorganic Division, CSIR-Indian Institute of Chemical Technology, Hyderabad 500607, India. Electronic address: kumbhare@iict.res.in.
authors.forename: Ravindra M
authors.initials: RM
authors.lastname: Kumbhare
authors.affiliation: Fluoroorganic Division, CSIR-Indian Institute of Chemical Technology, Hyderabad 500607, India.
authors.forename: Umesh B
authors.initials: UB
authors.lastname: Kosurkar
authors.affiliation: Medicinal Chemistry and Pharmacology Division, CSIR-Indian Institute of Chemical Technology, Hyderabad 500607, India; Present Address: Drug Discovery Research Center (DDRC), Translational Health Science and Technology Institute (THSTI), Gurgaon 122016, India.
authors.forename: Pankaj K
authors.initials: PK
authors.lastname: Bagul
authors.affiliation: Medicinal Chemistry and Pharmacology Division, CSIR-Indian Institute of Chemical Technology, Hyderabad 500607, India; Present Address: Drug Discovery Research Center (DDRC), Translational Health Science and Technology Institute (THSTI), Gurgaon 122016, India.
authors.forename: Abhinav
authors.initials: A
authors.lastname: Kanwal
authors.affiliation: Fluoroorganic Division, CSIR-Indian Institute of Chemical Technology, Hyderabad 500607, India.
authors.forename: K
authors.initials: K
authors.lastname: Appalanaidu
authors.affiliation: Fluoroorganic Division, CSIR-Indian Institute of Chemical Technology, Hyderabad 500607, India.
authors.forename: Tulshiram L
authors.initials: TL
authors.lastname: Dadmal
authors.affiliation: Medicinal Chemistry and Pharmacology Division, CSIR-Indian Institute of Chemical Technology, Hyderabad 500607, India; Present Address: Drug Discovery Research Center (DDRC), Translational Health Science and Technology Institute (THSTI), Gurgaon 122016, India. Electronic address: skbanerjee@thsti.res.in.
authors.forename: Sanjay Kumar
authors.initials: SK
authors.lastname: Banerjee
mesh_terms: D000806:Angiotensin-Converting Enzyme Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D004095:Dihydropyridines / Q000737:chemistry; D004789:Enzyme Activation / Q000187:drug effects; D057809:HEK293 Cells; D006801:Humans; D008352:Mannich Bases / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D007703:Peptidyl-Dipeptidase A / Q000737:chemistry* / Q000378:metabolism; D011485:Protein Binding; D014230:Triazoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology
chemical_list: D000806:Angiotensin-Converting Enzyme Inhibitors; D004095:Dihydropyridines; D008352:Mannich Bases; D014230:Triazoles; C038806:1,4-dihydropyridine; D007703:Peptidyl-Dipeptidase A
keywords: 1,4-Dihydropyridine; Angiotensin converting enzyme; Inhibitors; Mannich bases; Triazole