SDS of cas: 123-11-5. In 2021 EUR J MED CHEM published article about DRUG DISCOVERY; LEISHMANIA; DESIGN; DOCKING; ANTIBACTERIAL; METHOTREXATE; SYSTEM; TARGET in [Bibi, Maria; Farooq, Umar; Ullah, Azmat; Khan, Farhan A.; Rashid, Umer] COMSATS Univ Islamabad, Dept Chem, Abbottabad Campus, Abbottabad 22060, Khyber Pakhtunk, Pakistan; [Qureshi, Naveeda Akhter; Shaheen, Nargis] Quaid I Azam Univ, Dept Anim Sci, Islamabad 45320, Pakistan; [Sadiq, Abdul] Univ Malakand, Fac Biol Sci, Dept Pharm, Dir L 18000, KP, Pakistan; [Hassan, Abbas] Quaid I Azam Univ, Dept Chem, Islamabad 45320, Pakistan; [Asghar, Irfa; Umer, Duaa] COMSATS Univ Islamabad, Dept Biotechnol, Abbottabad Campus, Abbottabad 22060, Khyber Pakhtunk, Pakistan; [Salman, Muhammad] Natl Inst Hlth NIH, Dept Microbiol, Islamabad 45320, Pakistan; [Bibi, Ahtaram] Kohat Univ Sci & Technol, Fac Phys Sci, Dept Chem, Kohat 26000, Kp, Pakistan in 2021, Cited 42. The Name is 4-Methoxybenzaldehyde. Through research, I have a further understanding and discovery of 123-11-5.
To tackle leishmaniasis, search for efficient therapeutic drug targets should be pursued. Dihydrofolate reductase (DHFR) is considered as a key target for the treatment of leishmaniasis. In current study, we are interested in the design and synthesis of selective antifolates targeting DHFR from L. major. We focused on the development of new antifolates based on 3,4-dihydropyrimidine-2-one and 5-(3,5-dimethoxybenzyl)pyrimidine-2,4-diamine motif. Structure activity relationship (SAR) studies were performed on 4-phenyl ring of dihydropyrimidine (26-30) template. While for 5-(3,5-dimethoxybenzyl) pyrimidine-2,4-diamine, the impact of different amino acids (valine, tryptophan, phenylalanine, and glutamic acid) and two carbon linkers were explored (52-59). The synthesized compounds were assayed against LmDHFR. Compound 59 with the IC50 value of 0.10 mu M appeared as potent inhibitors of L. major. Selectivity for parasite DHFR over human DHFR was also determined. Derivatives 55-59 demonstrated excellent selectivity for LmDHFR. Highest selectivity for LmDHFR was shown by compounds 56 (SI = 84.5) and 58 (SI = 87.5). Compounds Antileishmanial activity against L. major and L. donovani promastigotes was also performed. To explore the interaction pattern of the synthesized compounds with biological macromolecules, the docking studies were carried out against homology modelled LmDHFR and hDHFR targets. (C) 2020 Elsevier Masson SAS. All rights reserved.
SDS of cas: 123-11-5. Welcome to talk about 123-11-5, If you have any questions, you can contact Bibi, M; Qureshi, NA; Sadiq, A; Farooq, U; Hassan, A; Shaheen, N; Asghar, I; Umer, D; Ullah, A; Khan, FA; Salman, M; Bibi, A; Rashid, U or send Email.
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