PMID- 26188621 OWN - NLM STAT- MEDLINE DCOM- 20160524 LR - 20150818 IS - 1768-3254 (Electronic) IS - 0223-5234 (Linking) VI - 101 DP - 2015 Aug 28 TI - Chalcone scaffolds as anti-infective agents: structural and molecular target perspectives. PG - 496-524 LID - S0223-5234(15)30131-8 [pii] LID - 10.1016/j.ejmech.2015.06.052 [doi] AB - In recent years, widespread outbreak of numerous infectious diseases across the globe has created havoc among the population. Particularly, the inhabitants of tropical and sub-tropical regions are mainly affected by these pathogens. Several natural and (semi) synthetic chalcones deserve the credit of being potential anti-infective candidates that inhibit various parasitic, malarial, bacterial, viral, and fungal targets like cruzain-1/2, trypanopain-Tb, trans-sialidase, glyceraldehyde-3-phosphate dehydrogenase (GAPDH), fumarate reductase, falcipain-1/2, beta-hematin, topoisomerase-II, plasmepsin-II, lactate dehydrogenase, protein kinases (Pfmrk and PfPK5), and sorbitol-induced hemolysis, DEN-1 NS3, H1N1, HIV (Integrase/Protease), protein tyrosine phosphatase A/B (Ptp-A/B), FtsZ, FAS-II, lactate/isocitrate dehydrogenase, NorA efflux pump, DNA gyrase, fatty acid synthase, chitin synthase, and beta-(1,3)-glucan synthase. In this review, a comprehensive study (from Jan. 1982 to May 2015) of the structural features of anti-infective chalcones, their mechanism of actions (MOAs) and structure activity relationships (SARs) have been highlighted. With the knowledge of molecular targets, structural insights and SARs, this review may be helpful for (medicinal) chemists to design more potent, safe, selective and cost effective anti-infective agents. CI - Copyright (c) 2015 Elsevier Masson SAS. All rights reserved. FAU - Mahapatra, Debarshi Kar AU - Mahapatra DK AD - Institute of Pharmaceutical Sciences, Guru Ghasidas Vishwavidyalaya (A Central University), Bilaspur 495009, Chhattisgarh, India. FAU - Bharti, Sanjay Kumar AU - Bharti SK AD - Institute of Pharmaceutical Sciences, Guru Ghasidas Vishwavidyalaya (A Central University), Bilaspur 495009, Chhattisgarh, India. Electronic address: skbharti.ggu@gmail.com. FAU - Asati, Vivek AU - Asati V AD - Institute of Pharmaceutical Sciences, Guru Ghasidas Vishwavidyalaya (A Central University), Bilaspur 495009, Chhattisgarh, India. LA - eng PT - Journal Article PT - Review DEP - 20150710 PL - France TA - Eur J Med Chem JT - European journal of medicinal chemistry JID - 0420510 RN - 0 (Anti-Infective Agents) RN - 0 (Enzymes) RN - 5S5A2Q39HX (Chalcone) SB - IM MH - Animals MH - Anti-Infective Agents/chemical synthesis/*chemistry/*pharmacology MH - Chalcone/chemical synthesis/*chemistry/*pharmacology MH - *Drug Design MH - Enzymes/*metabolism MH - Humans MH - Molecular Structure MH - Structure-Activity Relationship OTO - NOTNLM OT - Anti-malarial OT - Anti-parasitic OT - Chalcone OT - Mechanism of actions OT - Molecular targets OT - Structure activity relationships EDAT- 2015/07/21 06:00 MHDA- 2016/05/25 06:00 CRDT- 2015/07/20 06:00 PHST- 2015/03/17 00:00 [received] PHST- 2015/05/27 00:00 [revised] PHST- 2015/06/28 00:00 [accepted] PHST- 2015/07/20 06:00 [entrez] PHST- 2015/07/21 06:00 [pubmed] PHST- 2016/05/25 06:00 [medline] AID - S0223-5234(15)30131-8 [pii] AID - 10.1016/j.ejmech.2015.06.052 [doi] PST - ppublish SO - Eur J Med Chem. 2015 Aug 28;101:496-524. doi: 10.1016/j.ejmech.2015.06.052. Epub 2015 Jul 10.