180613-20-1Relevant articles and documents
New isoniazid derivatives with improved pharmaco-toxicological profile: Obtaining, characterization and biological evaluation
Dragostin, Ionut,Dragostin, Oana M.,Samal, Sangram Keshari,Dash, Saumya,Tatia, Rodica,Dragan, Maria,Confederat, Lumini?a,Ghiciuc, Cristina M.,Diculencu, Daniela,Lupu?oru, C?t?lina E.,Zamfir, Carmen L.
, (2019)
Tuberculostatic drugs are the most common drug groups with global hepatotoxicity. Awareness of potentially severe hepatotoxic reactions is vital, as hepatic impairment can be a devastating and often fatal condition. The treatment problems that may arise, within this class of medicines, are mainly of two types: adverse reactions (collateral, toxic or hypersensitive reactions) and the initial or acquired resistance of Mycobacterium tuberculosis to one or more antituberculosis drugs. Prevention of adverse reactions, increase treatment adherence and success rates, providing better control of tuberculosis (TB). In this regard, obtaining new drugs with low toxicity and high tuberculostatic potential is essential. Thus, in this work, we have designed or synthesized new derivatives of isoniazid (INH), such as new Isonicotinoylhydrazone (INH-a, INH-b and INH-c). These derivatives demonstrated good biocompatibility, antimicrobial property similar to that of parent isoniazid and last but not least, a significantly improved Pharmacotoxicological profile compared to that of isoniazid.
Antimicrobial activities of synthetic arylidine nicotinic and isonicotinic hydrazones
Hayat, Muhammad,Khan, Khalid Mohammed,Saeed, Sumayya,Salar, Uzma,Khan, Momin,Baig, Taimoor,Ahmad, Aqeel,Parveen, Shahnaz,Taha, Muhammad
, p. 1057 - 1067 (2018/10/31)
Background: Despite availability of variety of antibacterial agents, re-emergance of pathogenic bacteria is still a serious medical concern. Identification of new, safer, and selective antibacterial agents is the key interest in the medicinal chemistry research. Methods: A library of synthetic arylidene nicotinic and isonicotinic hydrazones (1-63) were investigated for antimicrobial activities. Results: A number of derivatives showed significant to moderate antimicrobial activities against Gram positive and Gram negative bacterial cultures. Few compounds also showed antifungal activity against fungal cultures. Minimum Inhibitory Concentration (MIC) was calculated for the most active compounds 1, 7, 11, 19, 34, 46, 50, 51, and 55 against gram positive and gram negative cultures. Conclusion: Newly identified compounds may serve as lead for future research in order to get the more powerful antibacterial agents.
An efficient alkynylation of 4-thiazolidinone with terminal alkyne under C-H functionalisation
Shaikh, Mohammed Umar M.,Mudaliar, Sulochana S.,Chikhalia, Kishor H.
, p. 50780 - 50785 (2016/06/09)
A method of palladium catalysed efficient alkynylation through the cross coupling reaction of terminal alkynes with the slightly more acidic C-H bonds of 4-thiazolidinone has been developed. This method allows the direct introduction of an ethynyl group into the 4-thiazolidinone moiety. Mild reaction conditions involving aerial oxidation and one pot synthesis make this reaction more efficient for the formation of sp3(C)-sp(C) bond.