Discovery of hydrazone containing thiadiazoles as Mycobacterium tuberculosis growth and enoyl acyl carrier protein reductase (InhA) inhibitors
 
Yazarlar (8)
Öğr. Gör. Hilal Doğan Erciyes Üniversitesi, Türkiye
Prof. Dr. Şengül Dilem Doğan Erciyes Üniversitesi, Türkiye
Prof. Dr. Miyase Gözde Gündüz Hacettepe Üniversitesi, Türkiye
Vagolu Siva Krishna
Birla Institute Of Technology And Science, Pilani, Hindistan
Christian Lherbet Laboratoire De Synthèse Et Physico-Chimie De Molécules D’Intérêt Biologique, Fransa
Dharmarajan Sriram
Birla Institute Of Technology And Science, Pilani, Hindistan
Prof. Dr. Onur ŞAHİN Sinop Üniversitesi, Türkiye
Prof. Dr. Emin Sarıpınar Erciyes Üniversitesi, Türkiye
Makale Türü Özgün Makale (SSCI, AHCI, SCI, SCI-Exp dergilerinde yayınlanan tam makale)
Dergi Adı European Journal of Medicinal Chemistry (Q1)
Dergi ISSN 0223-5234 Dergi Bilgileri (2020)
Dergi Tarandığı Indeksler SCI-Expanded
Makale Dili İngilizce Basım Tarihi 02-2020
Kabul Tarihi Yayınlanma Tarihi 01-02-2020
Cilt / Sayı / Sayfa 188 / 1 / 112035–0 DOI 10.1016/j.ejmech.2020.112035
Makale Linki https://linkinghub.elsevier.com/retrieve/pii/S0223523420300027
UAK Araştırma Alanları
Yoğun Madde Fiziği
Özet
Tuberculosis, caused by Mycobacterium tuberculosis, is a serious infectious disease and remains a global health problem. There is an increasing need for the discovery of novel therapeutic agents for its treatment due to the emerging multi-drug resistance. Herein, we present the rational design and the synthesis of eighteen new thiadiazolylhidrazones (TDHs) which were synthesized by intramolecular oxidative N–S bond formation reaction of 2-benzylidene-N-(phenylcarbamothioyl)hydrazine-1-carboximidamide derivatives by phenyliodine(III) bis(trifluoroacetate) (PIFA) under mild conditions. The compounds were characterized by various spectral techniques including FTIR, 1H NMR, 13C NMR and HRMS. Furthermore, the proposed structure of TDH12 was resolved by single-crystal X-ray analysis. The compounds were evaluated for their in vitro antitubercular activity against M. tuberculosis H37Rv. Among them …
Anahtar Kelimeler
Hydrazone | InhA | Molecular modeling | Synthesis | Thiadiazole | Tuberculosis