An article Design and synthesis of leucine-linked quinazoline-4(3H)-one-sulphonamide molecules distorting malarial reductase activity in the folate pathway WOS:000478950800001 published article about DRUG-RESISTANCE; IONIC LIQUID; DIHYDROFOLATE-REDUCTASE; SULFONAMIDE; INHIBITORS; ANTICANCER; EFFICIENT; PARASITE; PREDICT; COMFA in [Patel, Tarosh S.; Dixit, Bharat C.] Sardar Patel Univ, VP&RPTP Sci Coll, Chem Dept, Vallabh Vidyanagar 388120, Gujarat, India; [Bhatt, Jaimin D.] Sardar Patel Univ, VP&RPTP Sci Coll, Ind Chem Dept, Vallabh Vidyanagar, Gujarat, India; [Dixit, Ritu B.] Ashok & Rita Patel Inst Integrated Studies & Res, Pharmaceut Chem Dept, New Vallabh Vidyanagar, Gujarat, India; [Chudasama, Chaitanya J.] Sardar Patel Univ, Shree Alpesh N Patel PG Inst, Dept Biochem, Anand, Gujarat, India; [Patel, Bhavesh D.] Sardar Patel Univ, VP&RPTP Sci Coll, Microbiol Dept, Vallabh Vidyanagar, Gujarat, India in 2019.0, Cited 60.0. SDS of cas: 100-83-4. The Name is 3-Hydroxybenzaldehyde. Through research, I have a further understanding and discovery of 100-83-4
Optimization of a modified Grimmel’s method for N-heterocyclization of a leucine-linked sulfonamide side-arm at position 2 leading to 2,3-disustituted-4-quinazolin-(3H)-ones was accomplished. Further, 22 hybrid quinazolinone motifs (4a-v) were synthesized by N-heterocyclization reaction under microwave irradiation using the ionic liquid [Bmim][BF4]-H2O as green solvent as well as the catalyst. The in vitro screening of the hybrid entities against the malarial species Plasmodium falciparum yielded five potent molecules 4l, 4n, 4o, 4t, and 4u owning antimalarial activity comparable to those of the reference drugs. In continuation, an in silico study was carried out to obtain a pharmacophoric model and quantitative structure-activity relationship. We also built a 3D-QSAR model to procure more information that could be applied to design new molecules with more potent Pf-DHFR inhibitory activity. The designed pharmacophore was recognized to be more potent for the selected molecules, exhibiting five pharmacophoric features. The active scaffolds were further evaluated for enzyme inhibition efficacy against alleged receptor Pf-DHFR computationally and in vitro, proving their candidature as lead dihydrofolate reductase inhibitors, and the selectivity of the test candidates was ascertained by toxicity study against Vero cells. Good oral bioavailability was also proved by studying pharmacokinetic properties.
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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