Sulfonamide-1,2,4-thiadiazole derivatives as antifungal and antibacterial agents: synthesis, biological evaluation, lipophilicity, and conformational studies

Chemical & Pharmaceutical Bulletin
Charalabos CamoutsisMaria Zervou

Abstract

A series of thirteen new thiadiazole compounds were synthesized and evaluated for in vitro antifungal and antibacterial activity. All compound tested showed significant antifungal activity against all the micromycetes, compared to the commercial fungicide bifonazole. Differences in their activity depend on the substitution of different reactive groups. More specifically, best antifungal activity was shown for the synthetic analogue with methylpiperazine reactive group. Furthermore, it is apparent that different compounds reacted on different ways against bacteria. An effort was made to correlate the above mentioned differences in activity with lipophilicity studies. Furthermore, NMR and molecular modelling were used to obtain the main conformational features of a potent analogue, for future in silico studies.

References

Jan 1, 1968·Advances in Heterocyclic Chemistry·J Sandström
Aug 29, 2001·Clinical Infectious Diseases : an Official Publication of the Infectious Diseases Society of America·F C Tenover
Aug 29, 2001·Clinical Infectious Diseases : an Official Publication of the Infectious Diseases Society of America·D C Hooper
Jan 5, 2002·Current Opinion in Pharmacology·I Chopra
Aug 17, 2002·Antimicrobial Agents and Chemotherapy·Roland Leclercq, Patrice Courvalin
Jan 25, 2003·Antimicrobial Agents and Chemotherapy·Brunello OlivaIan Chopra
Apr 12, 2003·The Journal of Biological Chemistry·Jerry R ColcaAlexander S Mankin
May 23, 2003·Antimicrobial Agents and Chemotherapy·Anthony E ChoudhryKapila Ratnam
Jul 25, 2003·Antimicrobial Agents and Chemotherapy·Marc GalimandThierry Lambert
Nov 20, 2003·Chemistry and Physics of Lipids·P ZoumpoulakisT Mavromoustakos
Oct 1, 1995·Journal of Food Protection·Rasha K DaoukElsa J Sattout

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Citations

Mar 5, 2013·Chemical Biology & Drug Design·Abhishek Kumar JainRam Kishore Agrawal
Feb 13, 2015·Frontiers in Plant Science·Yasemin Bektas, Thomas Eulgem
Dec 5, 2012·ChemMedChem·Yijing LiGuisen Zhao
Mar 9, 2019·Anti-inflammatory & Anti-allergy Agents in Medicinal Chemistry·Dinesh K MehtaKamal Dua
Dec 7, 2018·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Ahmet Çağrı KaraburunZafer Asım Kaplancıklı
Feb 2, 2019·Current Topics in Medicinal Chemistry·Christophe TratratMarina Soković
Nov 26, 2020·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Sewara J MohammedKarzan A Abdalkarim

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