An article Synthesis, Biological Evaluation, Structure-Activity Relationship, and Mechanism of Action Studies of Quinoline-Metronidazole Derivatives Against Experimental Visceral Leishmaniasis WOS:000471834500027 published article about POTENTIAL ORAL TREATMENT; PROGRAMMED CELL-DEATH; REACTIVE OXYGEN; NITRIC-OXIDE; ANTILEISHMANIAL ACTIVITY; DRUG-RESISTANCE; OXIDATIVE STRESS; DONOVANI; THERAPY; ACTIVATION in [Upadhyay, Akanksha; Gupta, Sampa; Kushwaha, Pragati; Sashidhara, Koneni V.] CSIR Cent Drug Res Inst, Med & Proc Chem Div, BS-10-1,Sect 10,Jankipuram Extens,Sitapur Rd, Lucknow 226031, Uttar Pradesh, India; [Chandrakar, Pragya; Parmar, Naveen; Kar, Susanta] CSIR Cent Drug Res Inst, Div Parasitol, BS-10-1,Sect 10,Jankipuram Extens,Sitapur Rd, Lucknow 226031, Uttar Pradesh, India; [Singh, Sandeep Kumar; Rashid, Mamunur; Wahajuddin, Muhammad] CSIR Cent Drug Res Inst, Pharmacokinet & Metab Div, BS-10-1,Sect 10,Jankipuram Extens,Sitapur Rd, Lucknow 226031, Uttar Pradesh, India; [Upadhyay, Akanksha; Chandrakar, Pragya; Gupta, Sampa; Parmar, Naveen; Singh, Sandeep Kumar; Rashid, Mamunur; Kushwaha, Pragati; Wahajuddin, Muhammad; Sashidhara, Koneni V.; Kar, Susanta] Acad Sci & Innovat Res AcSIR, Anusandhan Bhawan, New Delhi 110025, India in 2019.0, Cited 69.0. HPLC of Formula: C8H8O2. The Name is 4′-Hydroxyacetophenone. Through research, I have a further understanding and discovery of 99-93-4
In our efforts to identify novel chemical scaffolds for the development of antileishmanial agents, a series of quinoline metronidazole hybrid compounds was synthesized and tested against the murine model of visceral leishmaniasis. Among all synthesized derivatives, 15b and 15i showed significant antileishmanial efficacy against both extracellular promastigote (IC50 9.54 and 5.42 mu M, respectively) and intracellular amastigote (IC50 9.81 and 3.75 mu M, respectively) forms of Leishmania donovani with negligible cytotoxicity toward the host 0774 macrophages, Vero cells). However, compound 15i effectively inhibited the parasite burden in the liver and spleen (>80%) of infected BALB/c mice. Mechanistic studies revealed that 15i triggers oxidative stress which induces bioenergetic collapse and apoptosis of the parasite by decreasing ATP production and mitochondrial membrane potential. Structure activity analyses and pharmacokinetic studies suggest 15i as a promising antileishmanial lead and emphasize the importance of quinoline metronidazole series as a suitable platform for the future development of antileishmanial agents.
Welcome to talk about 99-93-4, If you have any questions, you can contact Upadhyay, A; Chandrakar, P; Gupta, S; Parmar, N; Singh, SK; Rashid, M; Kushwaha, P; Wahajuddin, M; Sashidhara, KV; Kar, S or send Email.. HPLC of Formula: C8H8O2
Reference:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
,Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles