Ursolic acid derivatives for pharmaceutical use

a patent review (2012-2016)

Hidayat Hussain, Ivan R. Green, Iftikhar Ali, Ikhlas A. Khan, Zulfiqar Ali, Abdullah M. Al-Sadi, Ishtiaq Ahmed

Research output: Contribution to journalReview article

19 Citations (Scopus)

Abstract

Introduction: Ursolic acid (UA), belongs to a group of pentacyclic triterpenoids and is known to possess some very interesting biological properties. Protocols have been developed in order to synthesize bioactive UA analogs which have resulted in numerous ursolic acid analogs being synthesized during the period 2012–2016. Ursolic acid and its analogues can be employed to treat various cancers, inflammatory diseases, diabetes, Parkinson’s disease, Alzheimer’s disease, hepatitis B, hepatitis C and AIDS to mention but a few. Areas covered: This review covers patents on therapeutic activities of ursolic acid (UA) and its synthetic derivatives published during the four year period 2012–2016. A discussion about structure-activity relationships (SAR) of these analogs is also included. Expert opinion: Ursolic acid and its synthetic derivatives demonstrated excellent anticancer, antidiabetic, antiarrhythmic, anti-hyperlipidemic, antimicrobial, anti-hypercholesterolemic, and anti-cardiovascular properties. Additionally, various ursolic acid analogues have been synthesized through modification at positions C2-OH, C3-OH and C17-CO2H. It is noteworthy that the C-17 amide and amino analogs of UA possessed better anticancer activity compared to the parent compound (UA). Most importantly, UA has the potential to conjugate with other anticancer drugs or be transformed into its halo derivatives since this will greatly facilitate scientists to get lead compounds in cancer drug discovery.

Original languageEnglish
Pages (from-to)1061-1072
Number of pages12
JournalExpert Opinion on Therapeutic Patents
Volume27
Issue number9
DOIs
Publication statusPublished - Sep 2 2017

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Pharmaceutical Preparations
ursolic acid
Patents
Expert Testimony
Drug Discovery
Structure-Activity Relationship
Hepatitis C
Hepatitis B
Hypoglycemic Agents
Amides
Parkinson Disease
Neoplasms
Alzheimer Disease
Acquired Immunodeficiency Syndrome
Therapeutics

Keywords

  • anti-inflammatory
  • anticancer
  • diabetes
  • in vitro
  • in vivo
  • Ursolic acid

ASJC Scopus subject areas

  • Pharmacology
  • Drug Discovery

Cite this

Ursolic acid derivatives for pharmaceutical use : a patent review (2012-2016). / Hussain, Hidayat; Green, Ivan R.; Ali, Iftikhar; Khan, Ikhlas A.; Ali, Zulfiqar; Al-Sadi, Abdullah M.; Ahmed, Ishtiaq.

In: Expert Opinion on Therapeutic Patents, Vol. 27, No. 9, 02.09.2017, p. 1061-1072.

Research output: Contribution to journalReview article

Hussain, Hidayat ; Green, Ivan R. ; Ali, Iftikhar ; Khan, Ikhlas A. ; Ali, Zulfiqar ; Al-Sadi, Abdullah M. ; Ahmed, Ishtiaq. / Ursolic acid derivatives for pharmaceutical use : a patent review (2012-2016). In: Expert Opinion on Therapeutic Patents. 2017 ; Vol. 27, No. 9. pp. 1061-1072.
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