Literature DB >> 8496910

Novel heterocyclic analogues of the new potent class of calcium entry blockers: 1-[[4-(aminoalkoxy)phenyl]sulfonyl]indolizines.

J Gubin1, H de Vogelaer, H Inion, C Houben, J Lucchetti, J Mahaux, G Rosseels, M Peiren, M Clinet, P Polster.   

Abstract

Several heterocyclic analogues of the potent 1-[[4-(aminoalkoxy)phenyl]sulfonyl]indolizines were synthesized and evaluated for their antagonistic calcium activities in comparison with the 1-sulfonylindolizine SR 33557 and the usual calcium antagonist references verapamil, cis-(+)-diltiazem, and nifedipine. The bicyclic nine-membered rings were, in general, more potent than the bicyclic 10-membered or five-membered rings. Among the bicyclic nine-membered rings, the indole nucleus appeared to be extremely favorable to support the calcium antagonistic activity. In particular, compound 36, with an IC50 value for the inhibition of [3H]nitrendipine equal to 0.072 nM, is among the most potent calcium antagonist known. This compound has been selected for clinical development.

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Year:  1993        PMID： 8496910     DOI： 10.1021/jm00062a015

Source DB:  PubMed          Journal:  J Med Chem        ISSN： 0022-2623            Impact factor:   7.446


  6 in total

1.  Synthesis of 2,3-disubstituted benzo[b]furans by the palladium-catalyzed coupling of o-iodoanisoles and terminal alkynes, followed by electrophilic cyclization.

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Journal:  J Org Chem       Date:  2005-12-09       Impact factor: 4.354

Review 2.  Molecular pharmacology of high voltage-activated calcium channels.

Authors:  Clinton J Doering; Gerald W Zamponi
Journal:  J Bioenerg Biomembr       Date:  2003-12       Impact factor: 2.945

3.  [3 + 2]-Annulation of pyridinium ylides with 1-chloro-2-nitrostyrenes unveils a tubulin polymerization inhibitor.

Authors:  Alexander V Aksenov; Nikolai A Arutiunov; Nikita K Kirilov; Dmitrii A Aksenov; Igor Yu Grishin; Nicolai A Aksenov; Huifen Wang; Liqin Du; Tania Betancourt; Stephen C Pelly; Alexander Kornienko; Michael Rubin
Journal:  Org Biomol Chem       Date:  2021-08-13       Impact factor: 3.890

4.  Benzofuranyl Esters: Synthesis, Crystal Structure Determination, Antimicrobial and Antioxidant Activities.

Authors:  C S Chidan Kumar; Li Yee Then; Tze Shyang Chia; Siddegowda Chandraju; Yip-Foo Win; Shaida Fariza Sulaiman; Nurul Shafiqah Hashim; Kheng Leong Ooi; Ching Kheng Quah; Hoong-Kun Fun
Journal:  Molecules       Date:  2015-09-11       Impact factor: 4.411

5.  Crystallography, Molecular Modeling, and COX-2 Inhibition Studies on Indolizine Derivatives.

Authors:  Katharigatta N Venugopala; Sandeep Chandrashekharappa; Christophe Tratrat; Pran Kishore Deb; Rahul D Nagdeve; Susanta K Nayak; Mohamed A Morsy; Pobitra Borah; Fawzi M Mahomoodally; Raghu Prasad Mailavaram; Mahesh Attimarad; Bandar E Aldhubiab; Nagaraja Sreeharsha; Anroop B Nair; Osama I Alwassil; Michelyne Haroun; Viresh Mohanlall; Pottathil Shinu; Rashmi Venugopala; Mahmoud Kandeel; Belakatte P Nandeshwarappa; Yasmine F Ibrahim
Journal:  Molecules       Date:  2021-06-10       Impact factor: 4.411

6.  Novel Series of Methyl 3-(Substituted Benzoyl)-7-Substituted-2-Phenylindolizine-1-Carboxylates as Promising Anti-Inflammatory Agents: Molecular Modeling Studies.

Authors:  Katharigatta N Venugopala; Omar H A Al-Attraqchi; Christophe Tratrat; Susanta K Nayak; Mohamed A Morsy; Bandar E Aldhubiab; Mahesh Attimarad; Anroop B Nair; Nagaraja Sreeharsha; Rashmi Venugopala; Michelyne Haroun; Meravanige B Girish; Sandeep Chandrashekharappa; Osama I Alwassil; Bharti Odhav
Journal:  Biomolecules       Date:  2019-10-28
  6 in total

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